Some amphetamine affinities

Doktor DynaSoar targeting at OMCL.mil
Sat Feb 14 08:30:51 EST 2004


On Sat, 14 Feb 2004 04:56:21 GMT, BilZ0r
<BilZ0r at TAKETHISOUThotmail.com> wrote:

} Not that I'm really asking anyone here to do research for me, but no one 
} here would happen to be close to some information which says what affinity,  
} methamphetamine, mdma and mda have for the serotonin and dopamine reuptake 
} carrier, would they?

I like to start with Cooper, Bloom and Roth's "Biochemical basis of
neurophramacology" for this stuff (if they don't have the answer
there, they at least talk about it), but they're maddeningly
insensitive to placing references in the text, and it's hard to tell
just from the titles who said what.

IIRC, the transporters are essentially the same -- Na+ dependent
monoamine transporters. But I'd check here for the real deal:

Barker EL and Blakely RD (1995). Norepinephrine and serotonin
transporters: molecular targets of antidepressant drugs, in
Psychopharmacology: The Fourth Generation of Progress (Bloom FE and
Kupfer DJ eds) pp 321–334, Raven Press, New York. 

Here's AMP/DAT:

J Neurosci. 2001 Aug 15;21(16):5916-24. 
Amphetamine distorts stimulation-dependent dopamine overflow: effects
on D2 autoreceptors, transporters, and synaptic vesicle stores.
Schmitz Y, Lee CJ, Schmauss C, Gonon F, Sulzer D.

"To evaluate carefully AMPH effects on release and uptake, we recorded
stimulated DA overflow in striatal slices by using continuous
amperometry and cyclic voltammetry. Recordings were fit by a random
walk simulation of DA diffusion, including uptake with
Michaelis-Menten kinetics, that provided estimates of DA concentration
and uptake parameters. AMPH (10 microm) promoted the overflow of
synaptically released DA by decreasing the apparent affinity for DA
uptake (K(m) increase from 0.8 to 32 microm)."

There's probably more on all 3 and trasnporters here:
Synapse. 2000 Mar 1;35(3):222-7.
Neurochemical neutralization of methamphetamine with high-affinity
nonselective inhibitors of biogenic amine transporters: a
pharmacological strategy for treating stimulant abuse. Rothman RB,
Partilla JS, Baumann MH, Dersch CM, Carroll FI, Rice KC.


Everyone talks about it in the cocaine literature, but nobody puts in
in the abstracts. Have to read the articles just to find out if it's
in there. Here's some stuff on cocaine/DAT:

Pharmacol Biochem Behav. 1997 Jul;57(3):505-12.
Relations between heterogeneity of dopamine transporter binding and
function and the behavioral pharmacology of cocaine. Katz JL, Newman
AH, Izenwasser S.

Whew. PubMed is your friend, but the people who write the abstract
aren't necessarily. Then again, they're abstracts, not text books.
Check the references as well as doing some of your own poking around
for various combinations of the terms, just like Googling. Depending
on where you're doing it from, you'll have anywhere from some to a
whole bunch of access to the electronic versions of the articles,
which will really help when the abstract teases you but that's all.




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