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Titolo:
Inhibition of plasma membrane monoamine transporters by beta-ketoamphetamines
Autore:
Cozzi, NV; Sievert, MK; Shulgin, AT; Jacob, P; Ruoho, AE;
Indirizzi:
E Carolina Univ, Sch Med, Dept Pharmacol, Greenville, NC 27858 USA E Carolina Univ Greenville NC USA 27858 armacol, Greenville, NC 27858 USA Univ Wisconsin, Sch Med, Dept Pharmacol, Madison, WI 53706 USA Univ Wisconsin Madison WI USA 53706 Dept Pharmacol, Madison, WI 53706 USA Univ Calif San Francisco, Dept Med, San Francisco, CA 94110 USA Univ CalifSan Francisco San Francisco CA USA 94110 ancisco, CA 94110 USA Univ Calif San Francisco, Dept Psychiat, San Francisco, CA 94110 USA Univ Calif San Francisco San Francisco CA USA 94110 ancisco, CA 94110 USA
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 1, volume: 381, anno: 1999,
pagine: 63 - 69
SICI:
0014-2999(19990917)381:1<63:IOPMMT>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
SEROTONIN TRANSPORTERS; METHCATHINONE; RELEASE; AMPHETAMINE; ANALOGS; MECHANISM; DOPAMINE; POTENT; AGENT; MDMA;
Keywords:
methcathinone; MDMA (3,4-methylenedioxymethamphetamine); methamphetamine; monoamine transporter; 5-HT (5-hydroxytryptamine, serotonin); vesicle transporter (VMAT2);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Cozzi, NV E Carolina Univ, Sch Med, Dept Pharmacol, Greenville, NC 27858 USA E Carolina Univ Greenville NC USA 27858 reenville, NC 27858 USA
Citazione:
N.V. Cozzi et al., "Inhibition of plasma membrane monoamine transporters by beta-ketoamphetamines", EUR J PHARM, 381(1), 1999, pp. 63-69

Abstract

Methcathinone and methylone, the beta-ketone analogues of methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA), respectively, were tested forneurotransmitter uptake inhibition in vitro. The beta-ketones were threefold less potent than the nonketo drugs at inhibiting platelet serotonin accumulation, with IC50's of 34.6 +/- 4.8 mu M and 5.8 +/- 0.7 mu M, respectively. Methcathinone and methylone were similar in potency to methamphetamine and MDMA at catecholamine transporters individually expressed in transfected glial cells. For dopamine uptake, IC50's were 0.36 +/- 0.06 mu M and 0.82+/- 0.17 mu M, respectively; for noradrenaline uptake, IC50 values were 0.51 +/- 0.10 mu M and 1.2 +/- 0.1 mu M, respectively. In chromaffin granules, IC50's for serotonin accumulation were 112 +/- 8.0 mu M for methcathinoneand 166 +/- 12 mu M for methylone, 10-fold higher than the respective values for methamphetamine and MDMA. Our results indicate that methcathinone and methylone potently inhibit plasma membrane catecholamine transporters butonly weakly inhibit the vesicle transporter. (C) 1999 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 13:27:51