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Titolo:
Neurochemical neutralization of methamphetamine with high-affinity nonselective inhibitors of biogenic amine transporters: A pharmacological strategyfor treating stimulant abuse
Autore:
Rothman, RB; Partilla, JS; Baumann, MH; Dersch, CM; Carroll, FI; Rice, KC;
Indirizzi:
NIDA, Clin Psychopharmacol Sect, Intramural Res Program, DIR,NIH, Baltimore, MD 21224 USA NIDA Baltimore MD USA 21224 Res Program, DIR,NIH, Baltimore, MD 21224 USA Res Triangle Inst, Res Triangle Pk, NC 27709 USA Res Triangle Inst Res Triangle Pk NC USA 27709 Triangle Pk, NC 27709 USA NIDDK, Med Chem Lab, NIH, Bethesda, MD 20892 USA NIDDK Bethesda MD USA 20892 DK, Med Chem Lab, NIH, Bethesda, MD 20892 USA
Titolo Testata:
SYNAPSE
fascicolo: 3, volume: 35, anno: 2000,
pagine: 222 - 227
SICI:
0887-4476(20000301)35:3<222:NNOMWH>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
DOPAMINE; AMPHETAMINE; SEROTONIN; REUPTAKE; MONKEYS;
Keywords:
dopamine; serotonin; norepinephrine; transporters; methamphetamine; MDMA;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
12
Recensione:
Indirizzi per estratti:
Indirizzo: Rothman, RB NIDA, Clin Psychopharmacol Sect, Intramural Res Program, DIR,NIH, 5500 Nathan Shock Dr, Baltimore, MD 21224 USA NIDA 5500 Nathan Shock DrBaltimore MD USA 21224 MD 21224 USA
Citazione:
R.B. Rothman et al., "Neurochemical neutralization of methamphetamine with high-affinity nonselective inhibitors of biogenic amine transporters: A pharmacological strategyfor treating stimulant abuse", SYNAPSE, 35(3), 2000, pp. 222-227

Abstract

The abuse of methamphetamine (METH) and other amphetamine-like stimulants is a growing problem in the United States. METH is a substrate for the 12-transmembrane proteins which function as transporters for the biogenic amines dopamine (DA), serotonin (5-HT), and norepinephrine (NE). Increased release of CNS DA is thought to mediate the addictive effects of METH, whereas increased release of NE in both the peripheral and CNS is thought to mediateits cardiovascular effects. The neurotoxic effects of METH on both dopaminergic and serotonergic nerves requires the transport of METH into the nerveterminals. Thus, transport of METH into nerve terminals is the crucial first step in the production of METH-associated pharmacological and toxicological effects. A single molecular entity which would block the transport of METH at all three biogenic amine transporters might function to neurochemically neutralize METH. This agent would ideally be a high-affinity slowly dissociating agent at all three transporters, and also be amenable to formulation as a long-acting depot medication, such as has been accomplished with an analog of GBR12909. As a first step towards developing such an agent, we established an in vitro assay which selectively detects transporter substrates and used this assay to profile the ability of a lead compound, indatraline, to block the releasing effects of METH and MDMA at the DA, 5-HT, and NE transporters. The major finding reported here is that indatraline blocks the ability of METH and MDMA to release these neurotransmitters. (C) Published 2000 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 12/07/20 alle ore 08:50:54