Some amphetamine affinities
BilZ0r at TAKETHISOUThotmail.com
Mon Feb 16 00:12:11 EST 2004
Well the problem I find is that, different papers report different
affinities. I've found MDMA for SERT many times, and they are all
different, sometimes by nearly a factor of 10. I was hoping to find a
paper that gave all of them, so that they were standerdized.
I'm trying to buy a copy of the 5th generation of progress from amazon in
the next couple of days.
Doktor DynaSoar <targeting at OMCL.mil> wrote in
news:hv6s20pikfjbimskpnqjhbvjtv3aimbbsn at 4ax.com:
> 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 321334, 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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