User:Meodipt/backup

#1

Pharmacological Profile of Selected Agents in the Dopamine, Norepinephrine and 5-HT Release and Uptake Inhibition Assays:

Test Drug	Release NET EC₅₀ (nM ± SD)	NE Uptake K_i (nM ± SD)	Release DAT EC₅₀ (nM ± SD)	DA Uptake K_i (nM ± SD)	Release SERT EC₅₀ (nM ± SD)	5-HT Uptake K_i (nM ± SD)
Appetite Suppressants and their Metabolites
Phentermine	39.4 ± 6.6	-	262 ± 21	-	3,511 ± 253	-
(+)-Amphetamine	7.07 ± 0.95	-	24.8 ± 3.5	-	1,765 ± 94	-
(–)-Ephedrine	43.1 ± 4.0	-	236 ± 9	-	>10,000	>50,000
(+)-Ephedrine	218 ± 14	-	2,104 ± 68	-	-	-
Diethylpropion	>10,000	>10,000	>10,000	>10,000	>10,000	>10,000
N-Ethylpropion	99.3 ± 6.6	-	-	1,014 ± 80	2,118 ± 98	-
N,N-Diethylnorpseudoephedrine	>10,000	>10,000	>10,000	>10,000	>10,000	>10,000
Phendimetrazine	8,300 ± 445	>10,000	19,000 ± 537	>10,000	>100,000	>100,000
Phenmetrazine	50.4 ± 5.4	-	131 ± 11	-	7,765 ± 610	-
(±)-Pseudophenmetrazine	514 ± 52	-	-	2,630 ± 198	>10,000	>10,000
(+)-Pseudophenmetrazine	349 ± 28	-	1,457 ± 138	-	>10,000	>10,000
(–)-Pseudophenmetrazine	2,511 ± 561	-	-	2,691 ± 176	>10,000	>10,000
Appetite Suppressants Removed from Clinical Use
(±)-Fenfluramine	739 ± 57	-	-	23,700 ± 1,300	79.3 ± 11.5	-
(+)-Fenfluramine	302 ± 20	-	-	22,000 ± 1,100	51.7 ± 6.1	-
(–)-Fenfluramine	-	7,187 ± 559	>10,000	>20,000	147 ± 19	-
(±)-Norfenfluramine	168 ± 17	-	1,925 ± 295	-	104 ± 5	-
(+)-Norfenfluramine	72.7 ± 5.4	-	924 ± 112	-	59.3 ± 2.4	-
(–)-Norfenfluramine	474 ± 40	-	-	19,194 ± 1,048	287 ± 14	-
Aminorex	26.4 ± 2.8	-	49.4 ± 7.5	-	193 ± 23	-
Chlorphentermine	-	451 ± 66	2,650 ± 273	-	30.9 ± 5.4	-
Abused Stimulants
(+)-Methamphetamine	12.3 ± 0.7	-	24.5 ± 2.1	-	736 ± 45	-
(–)-Methamphetamine	28.5 ± 2.5	-	416 ± 20	-	4,640 ± 243	-
(±)-MDMA	110 ± 10	-	278 ± 7	-	72 ± 3	-
(+)-MDMA	136 ± 9	-	142 ± 4	-	74 ± 3	-
(–)-MDMA	560 ± 4	-	3,700 ± 100	-	340 ± 20	-
(±)-MDA	108 ± 7	-	190 ± 6	-	160 ± 7	-
(+)-MDA	50 ± 5	-	98 ± 4	-	100 ± 4	-
(–)-MDA	290 ± 10	-	900 ± 30	-	310 ± 10	-
Benzylpiperazine	62 ± 6.5	-	175 ± 13	-	6,050 ± 835	-
Endogenous Substrates
Tyramine	40.6 ± 3.5	-	119 ± 11	-	2,775 ± 234	-
Norepinephrine	164 ± 13	-	869 ± 51	-	>10,000	>50,000
Dopamine	66.2 ± 5.4	-	86.9 ± 9.7	-	-	6,489 ± 200
Serotonin	>10,000	3,013 ± 266	1,960 ± 147	-	44.4 ± 5.3	-
Transporter Inhibitors
GBR-12,935	-	277 ± 23	-	4.90 ± 0.30	-	289 ± 29
GBR-12,909 (Vanoxerine)	-	79.2 ± 4.9	-	4.3 ± 0.3	-	73.2 ± 1.5
Cocaine	-	779 ± 30	-	478 ± 25	-	304 ± 10
Mazindol	2.88 ± 0.17	-	25.9 ± 0.56	-	272 ± 11	-
Methylphenidate	-	118 ± 12	-	90.2 ± 7.9	-	-
Desipramine	-	8.32 ± 1.19	-	5,946 ± 193	-	350 ± 13
Fluoxetine	-	688 ± 39	-	>5,000	-	9.58 ± 0.88
Citalopram	-	4,332 ± 295	-	20,485 ± 923	-	2,40 ± 0.09
RTI-55 (β-CIT; Iometopane)	-	5.89 ± 0.53	-	0.83 ± 0.09	-	1.00 ± 0.03
Indatraline	-	12.6 ± 0.5	-	1.90 ± 0.05	-	3.10 ± 0.09
Miscellaneous Agents
Nantenine	>10,000	>10,000	>10,000	>10,000	>10,000	>10,000
Tramadol	>10,000	2,770 ± 250	>10,000	>10,000	>10,000	1,820 ± 100
JDTic	>10,000	1,756 ± 100	>10,000	3,620 ± 230	>10,000	-

Source: Rothman RB, Baumann MH. (2006) Therapeutic Potential of Monoamine Transporter Substrates. Current Topics in Medicinal Chemistry. 6(17), 1845-1859. Pubmed Link.

#2

Pharmacological Profile of Selected Agents in the DA, NE and 5-HT Release and Uptake Inhibition Assays:

Compound	NE Release	NE Reuptake	5-HT Release	5-HT Reuptake	DA Release	DA Reuptake
Aminorex	26.4 ± 2.8	54.5 ± 4.8	193 ± 23	1,244 ± 106	49.4 ± 7.5	216 ± 7
(+)-Amphetamine	7.07 ± 0.95	38.9 ± 1.8	1,765 ± 94	3,830 ± 170	24.8 ± 3.5	34 ± 6
Chlorphentermine	>10,000	451 ± 66	30.9 ± 5.4	388 ± 6	2,650 ± 273	3,940 ± 110
Dopamine	66.2 ± 5.4	40.3 ± 4.4	>10,000	6,489 ± 200	86.9 ± 9.7	38.3 ± 1.6
(–)-Ephedrine	72.4 ± 10.2	225 ± 36	>10,000	>50,000	1,350 ± 124	4,398 ± 213
(±)-Fenfluramine	739 ± 57	1,987 ± 205	79.3 ± 11.5	269 ± 7	>10,000	23,700 ± 1,300
(+)-Fenfluramine	302 ± 20	1,290 ± 152	51.7 ± 6.1	150 ± 5	>10,000	22,000 ± 1,100
(-)-Fenfluramine	>10,000	?	147 ± 19	?	>10,000	?
mCPP	38.1 ± 4.6	?	>10,000	?	>10,000	?
MDMA	77.4 ± 3.4	462 ± 18	56.6 ± 2.1	238 ± 13	376 ± 16	1,572 ± 59
(+)-Methamphetamine	12.3 ± 0.7	48.0 ± 5.1	736 ± 45	2,137 ± 98	24.5 ± 2.1	114 ± 11
(–)-Methamphetamine	28.5 ± 2.5	234 ± 14	4,640 ± 243	14,000 ± 644	416 ± 20	4,840 ± 178
Norepinephrine	164 ± 13	63.9 ± 1.6	>10,000	>50,000	869 ± 51	357 ± 27
Phentermine	39.4 ± 6.6	244 ± 15	3,511 ± 253	13,900 ± 510	262 ± 21	1,580 ± 80
Serotonin	>10,000	3,013 ± 266	44.4 ± 5.3	16.7 ± 0.9	>10,000	2,703 ± 79
Tyramine	40.6 ± 3.5	72.5 ± 5.0	2,775 ± 234	1,556 ± 95	119 ± 11	106 ± 6.0

Source(s):

Rothman RB, Baumann MH, Dersch CM; et al. (January 2001). "Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin". Synapse (New York, N.Y.). 39 (1): 32–41. doi:10.1002/1098-2396(20010101)39:1<32::AID-SYN5>3.0.CO;2-3. PMID 11071707. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link) PDF

Rothman RB, Baumann MH (July 2002). "Therapeutic and adverse actions of serotonin transporter substrates". Pharmacology & Therapeutics. 95 (1): 73–88. doi:10.1016/s0163-7258(02)00234-6. PMID 12163129.{{cite journal}}: CS1 maint: date and year (link) PDF

#3

Effect of Test Agents on Biogenic Amine Release or Uptake [EC₅₀ (nM ± S.D.)]:

Compound	NE Release	DA Release	5-HT Release
(+)-Amphetamine	7.07 ± 0.95	24.8 ± 3.5	1,765 ± 94
(+)-Methamphetamine	12.3 ± 0.7	24.5 ± 2.1	736 ± 45
(–)-Cathinone	12.4 ± 0.7	18.5 ± 0.3	2,366 ± 138
(–)-Methcathinone	13.1 ± 0.6	14.8 ± 0.4	1772 ± 160
(–)-Ephedrine	43.1 ± 4.0	236 ± 9	-
(+)-Ephedrine	218 ± 14	2,104 ± 68	-
(–)-Norephedrine	42.1 ± 4.3	302 ± 10	-
(+)-Norephedrine	137 ± 8.9	1,371 ± 50	-
(–)-Pseudoephedrine	4,092 ± 432	9,125 ± 480	-
(+)-Pseudoephedrine	224 ± 14	1,988 ± 50	-
(–)-Pseudonorephedrine	30.1 ± 2.2	294 ± 8	-
(+)-Pseudonorephedrine (Cathine)	15.0 ± 4.7	68.3 ± 2.4	-

Source: Rothman RB, Vu N, Partilla JS, Roth BL, Hufeisen SJ, Compton-Toth BA, Birkes J, Young R, Glennon RA. (2003) In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates. J Pharmacol Exp Ther. 307(1), 138-145. Pubmed Link, PDF Link.

#4

In Vitro Potency as Releasers of Monoamine Neurotransmitters:

Compound	[³H]NE	[³H]DA	[³H]5-HT
d-Amphetamine	7.2 ± 0.44	8.0 ± 0.43	1756 ± 94
3-Fluoroamphetamine (PAL-353)	16.1 ± 1.7	24.2 ± 1.1	1,937 ± 202
4-Fluoroamphetamine (PAL-303)	28.0 ± 1.8	51.5 ± 1.7	939 ± 76
3-Methylamphetamine (PAL-314)	18.3 ± 1.4	33.3 ± 1.3	218 ± 22
4-Methylamphetamine (PAL-313)	22.2 ± 1.3	44.1 ± 2.6	53.4 ± 0.83

Source: Wee S, Anderson KG, Baumann MH, Rothman RB, Blough BE, Woolverton WL. (2005) Relationship between the serotonergic activity and reinforcing effects of a series of amphetamine analogs. J Pharmacol Exp Ther. 313(2), 848-854. 15677348 Pubmed Link, PDF Link.

#5

Comparison of the K_i (μM) Values of Five Psychostimulants to Inhibit Human and Mouse Monoamine Transporters:

Transporter	Cocaine	Methylphenidate	d-Amphetamine	d-Methamphetamine	MDMA
Human
hDAT	0.23 ± 0.03	0.06 ± 0.01	0.64 ± 0.14	0.46 ± 0.06	8.29 ± 1.67
hNET	0.48 ± 0.05	0.10 ± 0.01	0.07 ± 0.01	0.11 ± 0.01	1.19 ± 0.13
hSERT	0.74 ± 0.03	132.43 ± 10.71	38.46 ± 3.84	31.74 ± 2.40	2.41 ± 0.73
Mouse
mDAT	0.49 ± 0.04	0.26 ± 0.03	0.56 ± 0.11	0.47 ± 0.08	4.87 ± 0.65
mNET	0.46 ± 0.06	0.17 ± 0.03	0.12 ± 0.02	0.19 ± 0.05	1.75 ± 0.51
mSERT	0.73 ± 0.12	114.37 ± 7.61	23.82 ± 1.71	9.28 ± 0.86	0.64 ± 0.05

Source: Han DD, Gu HH. (2006) Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs. BMC Pharmacol. 6(6). Pubmed Link, PDF Link.

#6

Antidepressants: Equilibrium Dissociation Constants (K_D (nM) ± S.E.M.) for the Receptors of Human Brain Frontal Cortex or Caudate Nucleus:

Compound	5-HT_1A	5-HT_2A	D₂	α₁-adrenergic	α₂-adrenergic	H₁	mACh
Amitriptyline	190 ± 40	29 ± 8	1,000 ± 100	27 ± 4	940 ± 320	1.1 ± 0.4	18 ± 1
Amoxapine	220 ± 50	0.6 ± 0.2	160 ± 60	50 ± 3	2,600 ± 150	25 ± 3	1,000 ± 150
Bupropion	170,000 ± 50,000	90,000 ± 20,000	?	4,600 ± 500	81,000 ± 8,000	6,600 ± 400	48,000 ± 9,000
Butriptyline	7,000 ± 2,000	380 ± 80	?	570 ± 110	4,800 ± 910	1.1 ± 0.1	35 ± 6
Clomipramine	7,000 ± 2,000	27 ± 7	190 ± 30	38 ± 6	3,200 ± 310	31 ± 6	37 ± 4
Clovoxamine	21,000 ± 5,000	4,000 ± 1,000	?	2,200 ± 20	11,000 ± 1,300	16,000 ± 1,000	26,000 ± 5,000
Desipramine	10,000 ± 3,000	280 ± 20	3,300 ± 300	130 ± 40	7,200 ± 1,400	110 ± 30	198 ± 14
Dothiepin	2,300 ± 800	258 ± 8	?	470 ± 20	2,400 ± 500	3.6 ± 0.2	25 ± 4
Doxepin	290 ± 50	25 ± 8	2,400 ± 300	24 ± 7	1,100 ± 200	0.24 ± 0.02	80 ± 6
Fluoxetine	24,000 ± 4,000	210 ± 40	?	5,900 ± 400	13,000 ± 700	6,200 ± 600	2,000 ± 400
Fluvoxamine	16,000 ± 2,000	5,600 ± 900	?	7,500 ± 1,000	15,000 ± 3,500	109,000 ± 20,000	24,000 ± 4,000
Imipramine	9,500 ± 800	80 ± 20	2,000 ± 200	90 ± 30	3200 ± 240	11 ± 1	90 ± 3
Iprindole	2,800 ± 700	280 ± 60	?	2,300 ± 400	8,600 ± 120	130 ± 20	2,100 ± 350
Maprotiline	12,000 ± 4,000	120 ± 20	350 ± 10	90 ± 20	9,400 ± 140	2.0 ± 0.4	570 ± 120
Mianserin	190 ± 20	7 ± 2	2,100 ± 200	34 ± 7	73 ± 6	0.40 ± 0.10	820 ± 110
Nisoxetine	20,500 ± 900	400 ± 100	?	5,300 ± 500	6,700 ± 550	4,200 ± 200	3,200 ± 50
Nomifensine	800 ± 200	900 ± 100	?	850 ± 80	6,500 ± 700	21,000 ± 2,000	250,000
Nortriptyline	310 ± 20	44 ± 8	1,200 ± 100	60 ± 10	2,500 ± 200	10 ± 2	150 ± 30
Oxaprotiline	67,000 ± 9,000	2,400 ± 600	?	620 ± 80	42,000 ± 7,000	21 ± 1	2,900 ± 600
Protriptyline	3,800 ± 500	70 ± 10	2,300 ± 600	130 ± 40	6,600 ± 390	25 ± 5	25 ± 1
Trazodone	60 ± 20	7 ± 2	3,800 ± 1,000	36 ± 2	490 ± 110	350 ± 60	324,000
Trimipramine	8,000 ± 2,000	32 ± 2	180 ± 50	24 ± 2	680 ± 120	0.27 ± 0.04	58 ± 12
Viloxazine	11,000 ± 2,000	31,000 ± 8,000	?	14,000 ± 2,000	44,000 ± 7,000	18,000 ± 2,000	54,000 ± 7,000
Zimelidine	18,000 ± 3,000	800 ± 200	?	1,500 ± 50	790 ± 40	4,000 ± 300	13,000 ± 2,500

Source(s):

Richelson E, Nelson A (July 1984). "Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro". The Journal of Pharmacology and Experimental Therapeutics. 230 (1): 94–102. PMID 6086881.{{cite journal}}: CS1 maint: date and year (link)

Wander TJ, Nelson A, Okazaki H, Richelson E (December 1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro". European Journal of Pharmacology. 132 (2–3): 115–21. doi:10.1016/0014-2999(86)90596-0. PMID 3816971.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#7

Equilibrium Dissociation Constants (K_D (nM) ± S.E.M.) for Antidepressants at Human Brain Receptors:

Compound	5-HT_1A	5-HT_2A	D₂	α₁-adrenergic	α₂-adrenergic	H₁	mACh
Adinazolam	>35,000	17,400 ± 500	>35,000	>35,000	>35,000	>35,000	>35,000
Amitriptyline	450 ± 20	18 ± 1	1,460 ± 90	24 ± 2	690 ± 20	0.95 ± 0.03	9.6 ± 0.3
Bupropion	>35,000	>35,000	>35,000	4,200 ± 300	>35,000	11,800 ± 600	>35,000
Desipramine	6,400 ± 300	350 ± 20	3,500 ± 200	100 ± 10	5,500 ± 200	60 ± 1	66 ± 2
Desmethylsertraline	>35,000	4,800 ± 300	11,000 ± 2,000	1,200 ± 100	7,800 ± 200	9,000 ± 2,000	1,430 ± 30
Doxepin	276 ± 4	27 ± 4	360 ± 60	23.5 ± 0.9	1,270 ± 40	0.17 ± 0.03	23 ± 2
Etoperidone	85 ± 2	36 ± 3	2,300 ± 400	38 ± 1	570 ± 10	3,100 ± 400	>35,000
Femoxetine	2,285 ± 4	130 ± 10	590 ± 30	650 ± 30	1,970 ± 60	4,200 ± 200	184 ± 4
Fluoxetine	32,400 ± 900	280 ± 50	12,000 ± 1,000	3,800 ± 300	13,900 ± 200	5,400 ± 500	5,90 ± 70
Imipramine	5,800 ± 500	150 ± 2	620 ± 90	32 ± 5	3,100 ± 100	37 ± 4	46 ± 2
Lofepramine	4,600 ± 200	200 ± 40	2,000 ± 400	100 ± 3	2,700 ± 100	360 ± 40	67 ± 1
Nefazodone	80 ± 20	26 ± 2	910 ± 40	48 ± 2	640 ± 30	24,000 ± 1,000	11,000 ± 2,000
Norfluoxetine	13,700 ± 400	600 ± 60	16,000 ± 1,000	3,900 ± 300	19,000 ± 700	11,000 ± 1,000	810 ± 40
Nortriptyline	294 ± 4	41 ± 4	2,570 ± 50	55 ± 2	2,030 ± 30	6.3 ± 0.9	37 ± 1
Paroxetine	>35,000	19,000 ± 1,000	32,000 ± 4,000	4,600 ± 500	17,000 ± 400	22,000 ± 4,000	108 ± 5
Sertraline	>35,000	9,900 ± 1,000	10,700 ± 800	380 ± 50	4,100 ± 200	24,000 ± 5,000	630 ± 30
Tomoxetine	10,900 ± 100	940 ± 70	>35,000	3,800 ± 200	8,800 ± 100	5,500 ± 900	2,060 ± 50
Trazodone	96 ± 5	25 ± 0.7	3,500 ± 600	42 ± 3	320 ± 10	1,100 ± 200	>35,000
Venlafaxine	>35,000	>35,000	>35,000	>35,000	>35,000	>35,000	>35,000

Source:

Cusack B, Nelson A, Richelson E (May 1994). "Binding of antidepressants to human brain receptors: focus on newer generation compounds". Psychopharmacology. 114 (4): 559–65. doi:10.1007/BF02244985. PMID 7855217.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link) PDF

#8

Affinities (K_i (nM) ± S.E.M.) of Typical and Atypical Antidepressants for the Cloned Rat 5-HT_2A and 5-HT_2C Receptors (and SERT for comparison):

Compound	5-HT_2A	5-HT_2C	SERT
Amitriptyline	4.3 ± 2.4	4.3 ± 0.8	17.6
Amoxapine	1.0 ± 0.5	2.0 ± 0.3	290
Citalopram	>1,000	269 ± 57	0.65
Clomipramine	15 ± 1	22 ± 7	0.14
Clorgyline	>1,000	>1,000	?
Desipramine	121 ± 9	244 ± 59	152
Doxepin	26 ± 10	8.8 ± 2.0	126
Fluoxetine	708 ± 6	42.6 ± 4.2	1.96
Imipramine	160 ± 7	94 ± 26	14.2
Iprindole	217 ± 8	206 ± 14	>1,000
Maprotiline	51 ± 11	122 ± 24	>1,000
Mianserin	1.0 ± 0.2	0.4 ± 0.1	>1,000
Nomifensine	>1,000	>1,000	>1,000
Norfluoxetine	>1,000	157 ± 19	3.15
Nortriptyline	5.0 ± 0.3	8.5 ± 3.7	60.8
Sertraline	>1,000	>1,000	0.047
Trazodone	6.0 ± 0.8	192 ± 64	243
Zimelidine	>1,000	>1,000	67.6

Source:

Pälvimäki EP, Roth BL, Majasuo H; et al. (August 1996). "Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor". Psychopharmacology. 126 (3): 234–40. doi:10.1007/BF02246453. PMID 8876023. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#9

Antidepressants: Equilibrium Dissociation Constants (K_D (nM) ± S.E.M.) and Selectivity for the Human Serotonin, Norepinephrine and Dopamine Transporters:

Antidepressants
Compound	SERT	NET	DAT
Amitriptyline	4.30 ± 0.12	35 ± 2	3,250 ± 20
Amoxapine	58 ± 2	16.0 ± 0.3	4,310 ± 10
Bupropion	9,100 ± 300	52,000 ± 1,000	520 ± 20
Butriptyline	1,360 ± 50	5,100 ± 400	3,940 ± 40
Citalopram	1.16 ± 0.01	4,070 ± 80	28,100 ± 700
Clomipramine	0.28 ± 0.01	38 ± 1	2,190 ± 40
Desipramine	17.6 ± 0.7	0.83 ± 0.05	3,190 ± 40
Desmethylcitalopram	3.6 ± 0.2	1,820 ± 40	18,300 ± 500
Desmethylsertraline	3.0 ± 0.2	390 ± 10	129 ± 2
Dothiepin	8.6 ± 0.4	46 ± 1	5,310 ± 30
Doxepin	68 ± 1	29.5 ± 0.8	12,100 ± 400
Etoperidone	890 ± 40	20,000 ± 2,000	52,000 ± 4,000
Femoxetine	11.0 ± 0.3	760 ± 40	2,050 ± 40
Fluoxetine	0.81 ± 0.02	240 ± 10	3,600 ± 100
Fluvoxamine	2.2 ± 0.2	1,300 ± 30	9,200 ± 200
Imipramine	1.40 ± 0.03	37 ± 2	8,500 ± 100
Iprindole	1,620 ± 40	1,262 ± 7	6,530 ± 20
Iproniazid	>100,000	>100,000	>100,000
Lofepramine	70 ± 4	5.4 ± 0.4	18,000 ± 1,000
Maprotiline	5,800 ± 200	11.1 ± 0.3	1,000 ± 20
Mianserin	4,000 ± 300	71 ± 2	9,400 ± 200
Mirtazapine, (±)-	>100,000	4,600 ± 300	>100,000
Mirtazapine, (+)-	>100,000	2,900 ± 200	>100,000
Mirtazapine, (-)-	>100,000	26,000 ± 3,000	>100,000
Nefazodone	200 ± 20	360 ± 40	360 ± 10
Nomifensine	1,010 ± 30	15.6 ± 0.4	56 ± 3
Norfluoxetine	1.47 ± 0.06	1,426 ± 9	420 ± 20
Nortriptyline	18 ± 1	4.37 ± 0.07	1,140 ± 30
Oxaprotiline	3,900 ± 100	4.9 ± 0.2	4,340 ± 30
Paroxetine	0.13 ± 0.01	40 ± 2	490 ± 20
Phenelzine	>100,000	49,000 ± 5,000	8,400 ± 200
Protriptyline	19.6 ± 0.5	1.41 ± 0.02	2,100 ± 60
Sertraline	0.29 ± 0.01	420 ± 20	25 ± 2
Tomoxetine	8.9 ± 0.3	2.03 ± 0.06	1,080 ± 50
Tranylcypromine	39,000 ± 2,000	5,900 ± 200	5,100 ± 200
Trazodone	160 ± 20	8,500 ± 300	7,400 ± 300
Trimipramine	149 ± 6	2,450 ± 30	3,780 ± 10
Venlafaxine	8.9 ± 0.3	1,060 ± 40	9,300 ± 50
Viloxazine	17,300 ± 500	155 ± 8	>100,000
Zimelidine	152 ± 6	9,400 ± 100	11,700 ± 400

The Related Compounds: Equilibrium Dissociation Constants (K_D (nM) ± S.E.M.) for the Human Serotonin, Norepinephrine and Dopamine Transporters:

Benzodiazepines
Compound	SERT	NET	DAT
Alprazolam	>100,000	>100,000	>100,000
Clonazepam	>100,000	>100,000	>100,000

Mood Stabilizers
Compound	SERT	NET	DAT
Acetazolamide	>100,000	>100,000	>100,000
Carbamazepine	32,000 ± 500	>100,000	>100,000
Lithium Carbonate	>100,000	>100,000	>100,000
Valproic Acid	>100,000	>100,000	>100,000

Hormones
Compound	SERT	NET	DAT
Estrone	50,000 ± 3,000	>100,000	13,500 ± 600
T₃	>100,000	>100,000	81,000 ± 300

Calcium Channel Blockers
Compound	SERT	NET	DAT
Nifedipine	>100,000	>100,000	>100,000
Verapamil	246 ± 6	48,000 ± 1,000	20,000 ± 300

Antihypertensives
Compound	SERT	NET	DAT
Reserpine	1,460 ± 60	15,200 ± 900	41,000 ± 2,000

Psychostimulants
Compound	SERT	NET	DAT
Amfonelic Acid	?	?	207 ± 5
Amphetamine, (+)-	>100,000	530 ± 40	2,900 ± 200
Cocaine	340 ± 20	1,420 ± 50	220 ± 9
Mazindol	39 ± 1	0.45 ± 0.03	8.1 ± 0.4
Methamphetamine, (+)-	>100,000	660 ± 20	2,800 ± 100
Methylphenidate	44,000 ± 1,000	234 ± 9	24 ± 1
Vanoxerine	940 ± 20	310 ± 10	27.2 ± 0.2

Antihistamines
Compound	SERT	NET	DAT
Chlorpheniramine	15.2 ± 0.8	1,440 ± 50	1,060 ± 4
Diphenhydramine	3,800 ± 400	960 ± 30	2,200 ± 100

Neurotransmitters
Compound	SERT	NET	DAT
Dopamine	>100,000	32,000 ± 3,000	2,400 ± 100
Norepinephrine	>100,000	2,200 ± 30	16,200 ± 500
Serotonin	2,100 ± 100	>100,000	>100,000

Source:

Tatsumi M, Groshan K, Blakely RD, Richelson E (December 1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters". European Journal of Pharmacology. 340 (2–3): 249–58. doi:10.1016/s0014-2999(97)01393-9. PMID 9537821.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link) PDF

#10

Affinty of Antipsychotic Drugs for Human Neurotransmitter Receptors (K_i, nM):

Compound	D₁	D₂	D₃	D₄	5-HT_1A	5-HT_1D^*	5-HT_2A	5-HT_2C	5-HT₆	5-HT₇	α₁-adrenegic	α₂-adrenergic	H₁	mACh
Aripiprazole	410	0.52	9.1	260	?	?	20	?	160	15	57	?	?	?
Clozapine	290	130	240	47	140	1,700	8.9	17	11	66	4.0	33	1.8	1.8
Haloperidol	120	1.4	2.5	3.3	3,600	>5,000	120	4,700	6,000	1,100	4.7	1,200	440	1,600
Iloperidone	320	6.3	7.1	25	93	?	5.6	43	63	110	1.4	160	470	?
Olanzapine	52	20	50	50	2,100	530	3.3	10	10	250	54	170	2.8	4.7
Quetiapine	1,300	180	940	2,200	230	>5,100	220	1,400	4,100	1,800	15	1,000	8.7	100
Risperidone	580	2.2	9.6	8.5	210	170	0.29	10	2,000	3.0	1.4	5.1	19	2,800
Volinanserin	1,800	1,800	?	?	>4,700	>5,100	0.3	68	7,400	2,000	68	2,200	83	?
Ziprasidone	130	3.1	7.2	32	2.5	2.0	0.39	0.72	76	9.3	13	310	47	5,100

Note: 5-HT_1D values are for bovine tissue.

Source(s):

Duncan GE, Zorn S, Lieberman JA (September 1999). "Mechanisms of typical and atypical antipsychotic drug action in relation to dopamine and NMDA receptor hypofunction hypotheses of schizophrenia". Molecular Psychiatry. 4 (5): 418–28. doi:10.1038/sj.mp.4000581. PMID 10523814.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link) PDF

Smith, Gerard C.; American College of Neuropsychopharmacology; Davis, Kenneth Rexton; Geary, Nori (2002). Neuropsychopharmacology: the fifth generation of progress: an official publication of the American College of Neuropsychopharmacology. Hagerstwon, MD: Lippincott Williams & Wilkins. ISBN 0-7817-2837-1.{{cite book}}: CS1 maint: multiple names: authors list (link)

#11

Neuroleptics: Equilibrium Dissociation Constants (K_D (nM) ± S.E.M.) for the Receptors of Human Brain Frontal Cortex or Caudate Nucleus:

Compound	5-HT_1A	5-HT_2A	D₂	α₁-adrenergic	α₂-adrenergic	H₁	mACh
Butaclamol	800 ± 300	0.4 ± 0.1	0.86 ± 0.06	56 ± 8	310 ± 40	390 ± 70	12,000 ± 3,000
Chlorpromazine	3,200 ± 800	1.4 ± 0.4	19 ± 2	2.6 ± 0.3	750 ± 50	9 ± 3	70 ± 6
Chlorprothixene	230 ± 20	0.43 ± 0.08	8 ± 2	?	?	?	?
Clozapine	1,800 ± 300	1.6 ± 0.4	180 ± 5	9 ± 3	160 ± 20	2.8 ± 0.8	12 ± 4
Fluphenazine	40,000 ± 10,000	19 ± 5	0.8 ± 0.1	9 ± 2	1,550 ± 20	21 ± 4	1,900 ± 500
Haloperidol	2,800 ± 600	36 ± 5	4 ± 1	6.1 ± 0.8	3,800 ± 400	1,900 ± 300	24,000 ± 9,000
Loxapine	2,900 ± 400	1.7 ± 0.4	70 ± 10	28 ± 6	2,400 ± 600	4.9 ± 0.8	450 ± 80
Mesoridazine	500 ± 100	4.8 ± 0.3	19 ± 3	2.0 ± 0.5	1,600 ± 100	1.8 ± 0.1	69 ± 2
Molindone	1,200 ± 300	5,000 ± 1,000	120 ± 40	2,500 ± 600	640 ± 100	124,000 ± 12,000	390,000 ± 90,000
Perphenazine	3,600 ± 400	5.6 ± 0.6	1.4 ± 0.2	10 ± 2	510 ± 20	8 ± 1	1,500 ± 30
Prochlorperazine	5,900 ± 700	15 ± 2	7 ± 1	24 ± 7	1,700 ± 100	19 ± 0.2	540 ± 120
Promazine	12,000 ± 2,000	16 ± 4	160 ± 5	6 ± 2	900 ± 100	2.0 ± 0.1	150 ± 30
Spiperone	320 ± 90	0.38 ± 0.05	0.16 ± 0.02	1.2 ± 0.2	660 ± 20	480 ± 70	2,700 ± 800
Thioridazine	350 ± 70	22 ± 8	26 ± 8	5 ± 1	800 ± 100	16 ± 3	18 ± 1
Thiothixene	1,400 ± 400	130 ± 30	0.45 ± 0.08	11 ± 1	200 ± 20	6 ± 2	2,900 ± 100
Trifluoperazine	23,000 ± 1,000	14 ± 1	2.6 ± 0.3	24 ± 3	2,600 ± 200	62 ± 7	660 ± 40
Triflupromazine	23,000 ± 5,000	4 ± 1	2.8 ± 0.5	?	?	?	?

Source(s):

Richelson E, Nelson A (August 1984). "Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro". European Journal of Pharmacology. 103 (3–4): 197–204. doi:10.1016/0014-2999(84)90478-3. PMID 6149136.{{cite journal}}: CS1 maint: date and year (link)
Wander TJ, Nelson A, Okazaki H, Richelson E (November 1987). "Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro". European Journal of Pharmacology. 143 (2): 279–82. doi:10.1016/0014-2999(87)90544-9. PMID 2891550.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#12

Binding Data (K_i (nM)) for Typical and Atypical Antipsychotic Drugs as Used in This Study:

Compound	5-HT_1A	5-HT_2A	5-HT_2C	5-HT₆	5-HT₇	D₂	α_1A-adrenergic	α_2A-adrenergic	α_2B-adrenergic	α_2C-adrenergic	H₁	M₃
Aripiprazole	5.57	8.7	22.4	783.2	9.6	26	74	102	37	0.66	29.7	4677
Chlorpromazine	116.4	8	25	20.1	35.8	0.28	184	27	46	4	6	47
Clozapine	104.8	5.4	17	17	17.9	1.64	142	26	34	256	1.2	25
Fluphenazine	145.7	30	1386	38	8	6.5	314.1	81.6	28.8	0.54	21	1441
Haloperidol	1202	53	>10000	3666	377.2	12	1130	480	550	4	1800	>10000
Loxapine	2456	7.7	9.5	32.9	87.2	31	150.8	107.6	79.9	12	7	122
Molindone	3797	320	>10000	1008	3053	2612	1097	557.8	172.6	63	2130	>10000
Olanzapine	2063	2	6.8	6.28	105.4	115	314.1	81.6	28.8	34	2	105
Perphenazine	421	5.6	132	17	23	10	810.5	104.9	85.2	1.4	8	1848
Pimozide	650	19	3350	71	0.5	197.7	1593	821.1	376.5	0.65	692	1955
Quetiapine	431.6	101	2502	1865	307.2	22	3630	746.6	28.7	245	11	>10000
Risperidone	427.5	0.17	35	1188	6.6	5	150.8	107.6	1.3	6.5	15	>10000
Sertindole	280	0.58	0.9	5.4	28	1.8	640	450	450	9.1	130	2692
Thioridazine	180.7	10	60	57.1	99	5	134.3	341.3	74.8	11	19	43
Thiothixene	410.4	50	1400	208.4	15.5	11	79.9	50.2	51.9	0.63	4	>10000
Trifluoperazine	950	13	378	118	290.8	24	653.7	163.6	391.5	1.3	63	1001
Ziprasidone	76	0.3	13	60.9	6.62	18	160	48	59	9.7	43	>10000

Source:

Kroeze WK, Hufeisen SJ, Popadak BA; et al. (March 2003). "H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs". Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 28 (3): 519–26. doi:10.1038/sj.npp.1300027. PMID 12629531. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#13

Equilibrium Dissociation Constants (K_D (nM) ± S.E.M.) for Antipsychotic Drugs at Human Brain Receptors:

Compound	α₁-adrenegic	α₂-adrenergic	D₂	H₁	mACh	5-HT_1A	5-HT_1D	5-HT_2A	5-HT_2C
Asenapine	1.1 ± 0.1	16 ± 1	2.0 ± 0.3	9.3 ± 0.8	7,000 ± 300	15 ± 2	10.2 ± 0.7	0.77 ± 0.03	0.27 ± 0.03
Clozapine	6.8 ± 0.8	15.0 ± 0.6	210 ± 30	3.1 ± 0.5	9 ± 1	160 ± 20	130 ± 10	2.59 ± 0.01	4.8 ± 0.4
Haloperidol	17 ± 1	600 ± 100	2.6 ± 0.5	260 ± 20	>10,000	1,800 ± 300	40 ± 4	61 ± 3	4,700 ± 400
Iloperidone	0.31 ± 0.02	3.0 ± 0.2	3.3 ± 0.1	12.3 ± 0.9	6,000 ± 300	33 ± 2	15 ± 2	0.20 ± 0.02	14 ± 1
Melperone	180 ± 20	150 ± 20	180 ± 20	580 ± 50	>10,000	2,200 ± 200	3,400 ± 100	102 ± 3	2,100 ± 200
Olanzapine	44 ± 4	280 ± 30	20 ± 3	0.087 ± 0.005	36 ± 5	610 ± 80	150 ± 20	1.48 ± 0.05	4.1 ± 0.2
Paliperidone	10.1 ± 0.8	80 ± 10	2.8 ± 0.3	3.4 ± 0.4	8,800 ± 600	480 ± 40	19 ± 1	1.21 ± 0.06	48 ± 5
Pimozide	76 ± 5	650 ± 40	29 ± 4	25 ± 3	800 ± 100	88 ± 6	3,100 ± 300	14.3 ± 0.1	570 ± 40
Quetiapine	8.1 ± 0.9	80 ± 10	770 ± 30	19 ± 1	1,400 ± 200	300 ± 20	560 ± 90	31 ± 4	3,500 ± 500
Risperidone	2.7 ± 0.3	8 ± 1	3.77 ± 0.04	5.2 ± 0.5	34,000 ± 3,000	190 ± 20	3.9 ± 0.5	0.15 ± 0.02	32 ± 4
Sertindole	3.9 ± 0.2	190 ± 30	2.7 ± 0.2	320 ± 30	5,000 ± 1,000	1,050 ± 40	20 ± 1	0.14 ± 0.01	6 ± 1
Ziprasidone	2.6 ± 0.3	154 ± 9	2.6 ± 0.1	4.6 ± 0.4	2,440 ± 80	1.9 ± 0.1	2.4 ± 0.1	0.12 ± 0.01	0.9 ± 0.1
Zotepine	7.3 ± 0.3	180 ± 8	8.1 ± 1	3.3 ± 0.4	330 ± 80	280 ± 20	80 ± 10	2.6 ± 0.1	3.2 ± 0.3

Source:

Richelson E, Souder T (November 2000). "Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds". Life Sciences. 68 (1): 29–39. doi:10.1016/s0024-3205(00)00911-5. PMID 11132243.{{cite journal}}: CS1 maint: date and year (link) PDF

#14

Neuroleptics: Equilibrium Dissociation Constants (K_D (nM) ± S.E.M.) for the Human Serotonin, Norepinephrine, and Dopamine Transporters:

Compound	SERT	NET	DAT
Bromperidol	2,200 ± 100	8,600 ± 400	1,660 ± 60
Carpipramine	1,370 ± 30	5,100 ± 200	1,300 ± 100
Chlorpromazine	30 ± 2	19 ± 2	1,750 ± 40
Chlorprothixene	110 ± 10	21 ± 1	1,690 ± 50
Clocapramine	560 ± 10	3,200 ± 200	370 ± 30
Clozapine	1,330 ± 50	2,700 ± 300	>10,000
Fluperlapine	30 ± 4	128 ± 3	>100,000
Fluphenazine	400 ± 30	4,600 ± 100	1,690 ± 20
Haloperidol	3,000 ± 100	6,500 ± 300	2,400 ± 70
Levomepromazine	2,800 ± 100	>10,000	4,100 ± 200
Loxapine	2,400 ± 100	380 ± 30	9,000 ± 200
Melperone	>10,000	>10,000	>10,000
Mesoridazine	>100,000	>10,000	>10,000
Molindone	>100,000	>100,000	>100,000
Moperone	2,680 ± 80	7,690 ± 60	>10,000
Olanzapine	1,310 ± 40	4,500 ± 100	>10,000
Oxypertine	>10,000	4,000 ± 200	630 ± 320
Perazine	3,200 ± 100	1,540 ± 80	5,800 ± 100
Perphenazine	610 ± 30	740 ± 20	1,290 ± 30
Pimozide	74 ± 8	370 ± 10	69 ± 3
Prochlorperazine	940 ± 30	510 ± 10	590 ± 20
Promazine	190 ± 20	25 ± 2	8,400 ± 100
Quetiapine	>10,000	>10,000	>10,000
Risperidone	>10,000	>10,000	>10,000
Sertindole	1,200 ± 200	640 ± 40	200 ± 20
Spiperone	7,500 ± 300	>10,000	4,200 ± 300
Sulpiride	>100,000	>100,000	>10,000
Sultopride	>100,000	>100,000	>10,000
Thioridazine	650 ± 30	1,620 ± 70	1,130 ± 30
Thiothixene	3,190 ± 40	30,000 ± 2000	3,600 ± 100
Tiapride	>100,000	>100,000	>10,000
Timiperone	>100,000	>10,000	5,400 ± 300
Tiospirone	2,200 ± 200	1,900 ± 300	460 ± 20
Trifluoperazine	810 ± 10	3,000 ± 100	570 ± 50
Triflupromazine	24 ± 1	110 ± 4	1,830 ± 40
Ziprasidone	39 ± 3	59 ± 7	76 ± 5
Zotepine	45 ± 3	20 ± 3	2,350 ± 80

Source:

Tatsumi M, Jansen K, Blakely RD, Richelson E (March 1999). "Pharmacological profile of neuroleptics at human monoamine transporters". European Journal of Pharmacology. 368 (2–3): 277–83. doi:10.1016/s0014-2999(99)00005-9. PMID 10193665.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link) PDF

#15

Inhibition of Opioid Binding and Neurotransmitter Uptake:

Compound	μ-OR	δ-OR	κ-OR	SERT	NET
DAMGO	0.365	85	210	>100,000	>100,000
DPDPE	380	4.45	11,700	>100,000	>100,000
U-69,593	1,000	3,750	6.65	>100,000	>100,000
Codeine	160	5,130	5,970	>100,000	>100,000
Oxycodone	8.69	901	1,350	>100,000	>100,000
Hydrocodone	11.1	962	501	>300,000	>300,000
Morphine, (-)-	1.24	145	23.4	>100,000	>100,000
Morphine, (+)-	>10,000	>100,000	>300,000	>300,000	>300,000
Buprenorphine	4.18	25.8	12.9	>100,000	>100,000
Naloxone, (-)-	0.559	36.5	4.91	>100,000	>100,000
Naloxone, (+)-	3,550	122,000	8,950	>100,000	>100,000
Naltrexone	0.0825	8.02	0.509	>100,000	>100,000
Levorphanol	0.42	3.61	4.2	86.3	1,210
Dextrorphan	420	34,700	5,950	401	340
Levomethorphan	11.2	249	225	35.8	179
Dextromethorphan	1,280	11,500	7,000	23	240
Levallorphan	0.213	2.18	1,100	7,950	19,100
Dextrallorphan	1,140	2,600	34.6	27,700	804
Methadone, (±)-	1.7	435	405	?	?
Methadone, (R)-(-)-	0.945	371	1,860	14.1	702
Methadone, (S)-(+)-	19.7	960	1,370	992	12,700
Levacetylmethadol	9.86	169	1,020	1,440	67,400
Dextropropoxyphene	34.5	380	1,220	30,000	10,000
Tramadol, (±)-	2,120	57,700	42,700	992	785
Tramadol, (+)-	1,330	62,400	54,000	528	2,510
Tramadol, (-)-	24,800	213,000	53,500	2,350	432

Source:

Codd EE, Shank RP, Schupsky JJ, Raffa RB (September 1995). "Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception". The Journal of Pharmacology and Experimental Therapeutics. 274 (3): 1263–70. PMID 7562497.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#16

The K_i Values of Drugs for Sigma-1, Sigma-2 and NMDA (PCP site) Receptors in Rat Brain Membranes:

Compound	σ₁	σ₂	NMDA (PCP)
Alazocine	45 ± 4	13,694 ± 4,849	587 ± 108
Dextromethorphan	205 ± 42	11,060 ± 1,320	7,253 ± 302
Dextrorphan	144 ± 37	11,325 ± 1,395	906 ± 77
Dimemorfan	151 ± 17	4,421 ± 277	16,978 ± 488
Dizocilpine	33,756 ± 1,999	51,111 ± 7,630	8.2 ± 1.6
Haloperidol	13 ± 4	148 ± 31	63,951 ± 3,858
Tenocyclidine	?	?	36.3 ± 0.2

Source:

Chou YC, Liao JF, Chang WY, Lin MF, Chen CF (March 1999). "Binding of dimemorfan to sigma-1 receptor and its anticonvulsant and locomotor effects in mice, compared with dextromethorphan and dextrorphan". Brain Research. 821 (2): 516–9. doi:10.1016/s0006-8993(99)01125-7. PMID 10064839.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#17

Antiparkinsonian Agents at Dopamine Receptors
Compound	D₁	D_2S	D_2L	D₃	D₄	D₅
Apomorphine	372	35	83	26	4.4	15
Bromocriptine	692	5.0	15	6.8	372	537
Cabergoline	214	0.62	0.95	0.80	56	22
Lisuride	65	0.34	0.66	0.28	4.6	3.5
Pergolide	339	32	26	5.5	59	33
Piribedil	>10,000	132	174	234	302	>10,000
Pramipexole	>10,000	955	1,698	10	129	>10,000
Quinelorane	>10,000	316	708	5.4	19	>10,000
Quinpirole	>10,000	891	1,445	42	34	>10,000
Ropinirole	>10,000	676	933	37	851	>10,000
Roxindole	468	2.8	4.4	1.2	5.9	191
Talipexole	>10,000	617	977	68	331	3,467
Terguride	28	0.81	1.1	1.0	8.1	23
TL99	2,692	7.2	68	2.5	58	78

Antiparkinsonian Agents at Serotonin Receptors
Compound	5-HT_1A	5-HT_1B	5-HT_1D	5-HT_2A	5-HT_2B	5-HT_2C
Apomorphine	117	2,951	1,230	120	132	102
Bromocriptine	13	355	11	107	56	741
Cabergoline	20	479	8.7	6.2	1.2	692
Lisuride	0.15	19	0.98	2.8	1.3	6.6
Pergolide	1.9	282	13	8.3	7.1	295
Piribedil	447	>10,000	>10,000	>10,000	1,202	>10,000
Pramipexole	692	8,318	1,660	>10,000	>10,000	>10,000
Quinelorane	>10,000	>10,000	>10,000	>10,000	>10,000	2,630
Quinpirole	1,698	>10,000	>10,000	>10,000	>10,000	>10,000
Ropinirole	288	>10,000	1,380	>10,000	3,802	>10,000
Roxindole	0.11	1,445	63	6.6	31	309
Talipexole	1,698	>10,000	>10,000	>10,000	>10,000	>10,000
Terguride	3.5	257	16	4.8	7.1	48
TL99	3,802	>10,000	1,950	2,344	2,042	2,291

Ropinirole at Additional Serotonin Receptors
Compound	5-HT₃	5-HT₄	5-HT_5A	5-HT₆	5-HT₇
Ropinirole	>10,000	>10,000	>10,000	>10,000	1,514

Antiparkinsonian Agents at Adrenergic Receptors
Compound	α_1A	α_1B	α_1D	α_2A	α_2B	α_2C	α_2D	β₁	β₂
Apomorphine	1,995	676	65	141	66	36	324	>10,000	>10,000
Bromocriptine	4.2	1.4	1.1	11	35	28	68	589	741
Cabergoline	288	60	166	12	72	22	3.6	>10,000	>10,000
Lisuride	5.5	17	3.0	0.055	0.13	0.13	0.79	68	7.9
Pergolide	1,047	692	295	50	32	68	692	>10,000	>10,000
Piribedil	813	6,166	219	89	288	69	437	>10,000	>10,000
Pramipexole	>10,000	>10,000	>10,000	1,698	631	>10,000	5,495	>10,000	>10,000
Quinelorane	>10,000	>10,000	>10,000	>10,000	>10,000	>10,000	>10,000	>10,000	>10,000
Quinpirole	>10,000	>10,000	>10,000	>10,000	2,512	>10,000	>10,000	>10,000	>10,000
Ropinirole	>10,000	>10,000	>10,000	1,862	759	1,202	4,467	>10,000	>10,000
Roxindole	2.6	2.8	1.3	6.2	4.6	1.8	28	2,692	933
Talipexole	>10,000	3,890	1,259	37	81	43	162	>10,000	>10,000
Terguride	3.5	35	3.9	0.30	0.45	0.76	1.5	661	20
TL99	>10,000	>10,000	>10,000	42	52	6.0	47	>10,000	>10,000

Antiparkinsonian Agents at Histamine and Muscarinic Acetylcholine Receptors
Compound	H₁	M₁
Apomorphine	>10,000	>10,000
Bromocriptine	>10,000	>10,000
Cabergoline	1,380	>10,000
Lisuride	35	>10,000
Pergolide	1,698	>10,000
Piribedil	>10,000	>10,000
Pramipexole	>10,000	>10,000
Quinelorane	1,047	>10,000
Quinpirole	1,047	>10,000
Ropinirole	2,951	>10,000
Roxindole	129	>10,000
Talipexole	>10,000	>10,000
Terguride	339	>10,000
TL99	776	>10,000

All values are for human receptors except for α_2D-adrenergic which is for the rat receptor (due to this receptor not being present in humans and only in rodents). Also the ropinirole values for 5-HT3 and 5-HT4 are for house and guinea pig receptors, respectively.

Source(s):

Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes". The Journal of Pharmacology and Experimental Therapeutics. 303 (2): 791–804. doi:10.1124/jpet.102.039867. PMID 12388666.{{cite journal}}: CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)
Newman-Tancredi A, Cussac D, Audinot V; et al. (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor". The Journal of Pharmacology and Experimental Therapeutics. 303 (2): 805–14. doi:10.1124/jpet.102.039875. PMID 12388667. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)
Newman-Tancredi A, Cussac D, Quentric Y; et al. (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes". The Journal of Pharmacology and Experimental Therapeutics. 303 (2): 815–22. doi:10.1124/jpet.102.039883. PMID 12388668. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)
Millan MJ, Cussac D, Gobert A; et al. (June 2004). "S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole". The Journal of Pharmacology and Experimental Therapeutics. 309 (3): 903–20. doi:10.1124/jpet.103.062398. PMID 14978194. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#18

Affinities of Tandospirone, Buspirone, Ipsapirone, and Gepirone for Neurotransmitter Receptor Binding Sites:

Receptor	Buspirone	Gepirone	Ipsapirone	Tandospirone
5-HT_1A	20 ± 3	70 ± 10	7.9 ± 2	27 ± 5
5-HT_1B	> 100,000	> 100,000	> 100,000	> 100,000
5-HT_1D	> 100,000	> 100,000	33,000 ± 8,000	> 100,000
5-HT_2A	1,300 ± 400	3,000 ± 50	6,400 ± 4,000	1,300 ± 200
5-HT_2C	1,100 ± 200	5,000 ± 700	5,000 ± 1,000	2,600 ± 60
SERT	–	–	–	> 100,000
α₁-Adrenergic	1,000 ± 400	2,300 ± 300	40 ± 7	1,600 ± 80
α₂-Adrenergic	6,000 ± 700	1,600 ± 200	1,900 ± 500	1,900 ± 400
β-Adrenergic	8,800 ± 1,000	> 100,000	> 100,000	> 100,000
D₁	33,000 ± 1,000	> 100,000	15,000 ± 2,000	41,000 ± 10,000
D₂	240 ± 50	2,200 ± 200	1,900 ± 200	1,700 ± 300
BDZ	> 100,000	> 100,000	> 100,000	> 100,000
mACh	38,000 ± 5,000	> 100,000	49,000 ± 5,000	> 100,000

Source: Hamik A, Oksenberg D, Fischette C, Peroutka SJ. (1990) Analysis of Tandospirone (SM-3997) Interactions With Neurotransmitter Receptor Binding Sites. Biol Psychiatry. 28(2), 99-109. Pubmed Link

#19

K_i Values of Test Drugs at 5-HT₂ Receptors:

Compound	5-HT_2A (rat)	5-HT_2B (human)	5-HT_2C (rat)
(±)-Fenfluramine	5216 ± 2.5	4134 ± 753	3183 ± 374
(+)-Fenfluramine	11107 ± 1354	5099 ± 690	6245 ± 514
(-)-Fenfluramine	5463 ± 352	5713 ± 1344	3415 ± 542
(±)-Norfenfluramine	2316 ± 163	52.1 ± 12.3	557 ± 36
(+)-Norfenfluramine	1516 ± 88	11.2 ± 4.3	324 ± 7.1
(-)-Norfenfluramine	3841 ± 361	47.8 ± 18.0	814 ± 58

Values are mean ± SEM (n=3). Units are nanomolar (nM).

Source: Rothman RB, Baumann MH, Savage JE; et al. (December 2000). "Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications". Circulation. 102 (23): 2836–41. doi:10.1161/01.cir.102.23.2836. PMID 11104741. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: date and year (link) CS1 maint: multiple names: authors list (link)

#20

Binding profiles of opioids (Codd et al., 1995)
Drug	MORTooltip mu-Opioid receptor	DORTooltip delta-Opioid receptor	KORTooltip kappa-Opioid receptor	SERTTooltip Serotonin transporter	NETTooltip Norepinephrine transporter
Buprenorphine	4.18	25.8	12.9	>100,000	>100,000
Codeine	160	5,130	5,970	>100,000	>100,000
DAMGO	0.365	85	210	>100,000	>100,000
Dextropropoxyphene	34.5	380	1,220	30,000	10,000
DPDPE	380	4.45	11,700	>100,000	>100,000
Hydrocodone	11.1	962	501	>300,000	>300,000
Levacetylmethadol	9.86	169	1,020	1,440	67,400
Levallorphan	0.213	2.18	1,100	7,950	19,100
Levomethorphan	11.2	249	225	35.8	179
Levorphanol	0.42	3.61	4.2	86.3	1,210
Methadone	1.7	435	405	ND	ND
Dextromethadone	19.7	960	1,370	992	12,700
Levomethadone	0.945	371	1,860	14.1	702
Morphine, (–)-	1.24	145	23.4	>100,000	>100,000
Morphine, (+)-	>10,000	>100,000	>300,000	>300,000	>300,000
Naloxone, (–)-	0.559	36.5	4.91	>100,000	>100,000
Naloxone, (+)-	3,550	122,000	8,950	>100,000	>100,000
Naltrexone	0.0825	8.02	0.509	>100,000	>100,000
Oxycodone	8.69	901	1,350	>100,000	>100,000
Tramadol	2,120	57,700	42,700	992	785
U-69,593	1,000	3,750	6.65	>100,000	>100,000
Values are K_i (nM). The smaller the value, the more strongly the drug binds to the site. Assays were done with rat brain membranes.

Source: Codd EE, Shank RP, Schupsky JJ, Raffa RB (1995). "Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception". J. Pharmacol. Exp. Ther. 274 (3): 1263–70. PMID 7562497.

#21

Binding profiles of opioids (Tam, 1985)
Drug	MORTooltip mu-Opioid receptor	DORTooltip delta-Opioid receptor	KORTooltip kappa-Opioid receptor	σ₁
(–)-Alazocine	3.0	15	4.7	1,800–2,400
(+)-Alazocine	1,900	19,000	1,600	48–66
Bremazocine	0.9	2.9	0.67	195
Butorphanol	1.7	13	7.4	2,300
Cyclazocine	0.45	6.3	5.9	36–42
DADLE	150	1.8	>10,000	>100,000
Dynorphin	31	12	0.98	>10,000
(–)-Ethylketazocine	2.3	5.2	2.2	15,000–19,000
(+)-Ethylketazocine	2,500	>10,000	1,600	55–76
Morphine	38	510	1,900	>100,000
Nalbuphine	6.3	163	61	>100,000
Nalorphine	4.5	49	31	80,000
Naloxone	1.1	16	12	>100,000
Oxymorphone	15	145	725	>100,000
Pentazocine	39	467	87	18–29
Sufentanil	5.3	41	140	94
Tifluadom	32	189	2.1	6,600
U-50488H	825	21,000	15	696
Values are K_i (nM). The smaller the value, the more strongly the drug binds to the site. Assays were done with guinea pig brain membranes.

Source: Tam SW (1985). "(+)-[3H]SKF 10,047, (+)-[3H]ethylketocyclazocine, mu, kappa, delta and phencyclidine binding sites in guinea pig brain membranes". Eur. J. Pharmacol. 109 (1): 33–41. doi:10.1016/0014-2999(85)90536-9. PMID 2986989.

#22

Binding and activation profiles of opioids (Gharagozlou et al., 2002, 2003, 2006)
Drug	MORTooltip mu-Opioid receptor			DORTooltip delta-Opioid receptor			KORTooltip kappa-Opioid receptor
Drug	K_i	IC₅₀	I_max	K_i	IC₅₀	I_max	K_i	EC₅₀	I_max	IA
β-Endorphin	ND	526	71%	ND	ND	ND	ND	ND	ND	ND
Alazocine	1.15	ANT	–	ND	184	68%	0.4	24	38%	0.66
Butorphanol	ND	3	58%	ND	61	64%	2.5	57	33%	0.57
Cyclazocine	0.22	21	37%	ND	6	53%	0.1	2	39%	0.67
DAMGO	2.65	35	58%	ND	ND	ND	ND	ND	ND	ND
Dezocine	ND	1.3	43%	ND	477	39%	24.5	ANT	–	ANT
Etorphine	ND	0.6	60%	ND	0.2	67%	ND	0.4	52%	0.90
Fentanyl	ND	8.4	69%	242.5	2,039	71%	233	1,677	58%	1.00
Hydromorphone	ND	0.8	67%	ND	54	65%	55	279	55%	0.95
Lofentanil	ND	3.8	56%	ND	0.8	62%	8.2	153	58%	1.00
Met-enkephalin	ND	ND	ND	ND	22	49%	ND	ND	ND	ND
Metazocine	ND	2.0	41%	ND	159	77%	24	56	47%	0.81
Morphine	2.2	17	48%	68.5	1,101	39%	26	213	55%	0.95
Nalbuphine	ND	11	49%	77	545	55%	6	2,550	27%	0.47
Nalorphine	ND	2.7	50%	38.5	ANT	–	1.6	483	55%	0.95
Naltrexone	0.74	ANT	–	ND	ANT	–	0.3	ANT	–	ANT
Quadazocine	0.99	ANT	–	2.6	40	54%	0.5	ANT	–	ANT
Xorphanol	0.25	3.4	29%	1.0	8	76%	0.4	3.3	49%	0.84
Values are nM. The smaller the value (aside from the percentages), the more strongly the drug inter- acts with the site. Assays were done with cloned mouse receptors transfected in HEK293 cells.

Sources:

Gharagozlou P, Demirci H, David Clark J, Lameh J (2003). "Activity of opioid ligands in cells expressing cloned mu opioid receptors". BMC Pharmacol. 3: 1. doi:10.1186/1471-2210-3-1. PMC 140036. PMID 12513698.{{cite journal}}: CS1 maint: unflagged free DOI (link)
Gharagozlou P, Demirci H, Clark JD, Lameh J (2002). "Activation profiles of opioid ligands in HEK cells expressing delta opioid receptors". BMC Neurosci. 3: 19. doi:10.1186/1471-2202-3-19. PMC 137588. PMID 12437765.{{cite journal}}: CS1 maint: unflagged free DOI (link)
Gharagozlou P, Hashemi E, DeLorey TM, Clark JD, Lameh J (2006). "Pharmacological profiles of opioid ligands at kappa opioid receptors". BMC Pharmacol. 6: 3. doi:10.1186/1471-2210-6-3. PMC 1403760. PMID 16433932.{{cite journal}}: CS1 maint: unflagged free DOI (link)

User:Meodipt/backup

#1

#2

#3

#4

#5

#6

#7

#8

#9

#10

#11

#12

#13

#14

#15

#16

#17

#18

#19

#20

#21

#22

Navigation menu

Search