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Titolo:
Pharmacological profile of neuroleptics at human monoamine transporters
Autore:
Tatsumi, M; Jansen, K; Blakely, RD; Richelson, E;
Indirizzi:
Mayo Clin Jacksonville, Jacksonville, FL 32224 USA Mayo Clin JacksonvilleJacksonville FL USA 32224 cksonville, FL 32224 USA Showa Univ, Sch Med, Dept Psychiat, Tokyo 142, Japan Showa Univ Tokyo Japan 142 niv, Sch Med, Dept Psychiat, Tokyo 142, Japan Vanderbilt Univ, Sch Med, Dept Pharmacol, Nashville, TN 37232 USA Vanderbilt Univ Nashville TN USA 37232 Pharmacol, Nashville, TN 37232 USA
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 2-3, volume: 368, anno: 1999,
pagine: 277 - 283
SICI:
0014-2999(19990305)368:2-3<277:PPONAH>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN DOPAMINE TRANSPORTER; HUMAN SEROTONIN TRANSPORTER; RAT-BRAIN SYNAPTOSOMES; BIOGENIC-AMINE UPTAKE; NOREPINEPHRINE UPTAKE; BINDING; ANTIDEPRESSANTS; COCAINE; IMIPRAMINE; PIMOZIDE;
Keywords:
5-HT (5-hydroxy-hyptamine, serotonin), human; norepinephrine transporter, human; dopamine transporter, human; neuroleptic; radioligand binding assay;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
37
Recensione:
Indirizzi per estratti:
Indirizzo: Richelson, E Mayo Clin Jacksonville, 4500 San Pablo Rd, Jacksonville, FL 32224 USA Mayo Clin Jacksonville 4500 San Pablo Rd Jacksonville FL USA 32224
Citazione:
M. Tatsumi et al., "Pharmacological profile of neuroleptics at human monoamine transporters", EUR J PHARM, 368(2-3), 1999, pp. 277-283

Abstract

Using radioligand binding techniques, we determined the equilibrium dissociation constants (K-D) for 37 neuroleptics and one metabolite of a neuroleptic (haloperidol metabolite) for the human serotonin, norepinephrine, and dopamine transporters with [H-3]imipramine, [H-3]nisoxetine, and [H-3]WIN35428, respectively. Among neuroleptics, the four most potent compounds at thehuman serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K-D 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K-D 19-25 nM). At the human dopamine transporter, only pimozide (K-D = 69 +/- 3) ziprasidone (K-D = 76 +/- 5) had notable potency. These data may be useful in predicting therapeutic and adverse effects, including drug interactions of neuroleptics. (C) 1999 Elsevier Science B.V. All rights reserved.

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Documento generato il 06/07/20 alle ore 05:57:52