Various release, reuptake, and binding affinities for stims.

There is a lot of talk in comparing various stims, barring subjective reports, I thought it would be nice to have some numerical comparisons.

IMPORTANT NOTE ON READING THIS CHART

The values above are expressed as equilibrium dissociation constants (K^i (nM)). Lower values correspond to higher binding at the site, or in other words, less is more.

DATA

Table 1

Drug	NE Release	NE Uptake	5-HT Release	5-HT Uptake	DA Release	DA Uptake
(+)-Amphetamine	7.07	38.9	1,765	3,830	24.8	34
(-)-Methamphetamine	28.5	234	4,640	14,000	416	4,840
(+)-Methamphetamine	12.3	48.0	736	2,137	24.5	114
(-)-Ephedrine	72.4	225	>10,000	>50,000	1,350	4,398
(+/-)-MDMA	77.4	462	56.6	238	376	1,572
Cocaine	>10,000	779	>10,000	304	>10,000	478
RTI-55	>10,000	5.89	>10,000	1	>10,000	0.83
RTI-229	>10,000	19.5	>10,000	362	>10,000	2.15

Source: Amphetamine-Type Central Nervous System Stimulants Release Norepinephrine More Potently Than They Release Dopamine and Serotonin, Rothman et. al.

Measurement: IC^50 (nM) for release / K^i (nM) for uptake

Table 2

Drug	NE Release	DA Release	5-HT Release
4-FA	28	51.5	939
4-MA	22.2	44.1	53.4
(d)-Amphetamine	7.1	110.3	1,765
Benzylpiperazine	62	175	6,050
Cathine	15.0	68.3	-
(l)-Cathinone	1,206.2	18.5	2,366
(l)-ephedrine	43.1	236	>10,000
(d)-ephedrine	218	2,104	>10,000
(d)-Methamphetamine	489	24.5	736
(l)-Methamphetamine	234	4,480	>10,000
(l)-Methcathinone	707	14.8	1772
MDA	108	190	160
MDMA	110	278	72
Phenmetrazine	50.4	131	7,765
Psuedoephedrine	3112	1988	>10,000

Source: Releasing Agents - Release Affinities of Selected Compounds, References 4-9

Measurement: K^i (nM) for release

Table 3

Drug	NE Uptake	DA Uptake	NET Binding	DAT Binding
(d)-methylphenidate	46	28	408	139
(d/l)-methylphenidate	31	24	1,560	105
(d)-ethylphenidate	247	24	2,479	276
(d/l)-ethylphenidate	408	82	4,824	382

Source: Ethylphenidate - Pharmacodynamics, References 7-9

Measurement: K^i (nM) for transporter binding, IC^50 for uptake

Posted Jan 27, 2014, 2:52 AM UTC · edited

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