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Titolo:
Comparison of antipsychotic activity and discriminative stimulus effects of the novel acylprolyltyrosine containing compound, GZR-123, and sulpiride
Autore:
Asmakova, LS; Kalinina, TS; Ostrovskaya, RU; Gudasheva, TA; Zaitseva, NI; Bondarenko, NA; Voronina, TA; Seredenin, SB;
Indirizzi:
Russian Acad Med Sci, Inst Pharmacol, Moscow 125315, Russia Russian Acad Med Sci Moscow Russia 125315 armacol, Moscow 125315, Russia
Titolo Testata:
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
fascicolo: 2, volume: 64, anno: 1999,
pagine: 359 - 362
SICI:
0091-3057(199910)64:2<359:COAAAD>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
DOPAMINE; NEUROTENSIN;
Keywords:
antipsychotics; acylprolyltyrosines; GZR-123; sulpiride; antidopamine activity; drug discrimination;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
14
Recensione:
Indirizzi per estratti:
Indirizzo: Asmakova, LS Russian Acad Med Sci, Inst Pharmacol, Baltiyskaga Str 8, Moscow 125315, Russia Russian Acad Med Sci Baltiyskaga Str 8 Moscow Russia 125315
Citazione:
L.S. Asmakova et al., "Comparison of antipsychotic activity and discriminative stimulus effects of the novel acylprolyltyrosine containing compound, GZR-123, and sulpiride", PHARM BIO B, 64(2), 1999, pp. 359-362

Abstract

The present experiment has been performed to determine the pharmacologicalprofile of a newly synthesized systematically active prolyltyrosine containing compound, caproyl-L-Pro-L-Tyr methyl ester (GZR-123), and to compare it with that of the standard atypical benzamide neuroleptic, sulpiride. GZR-123 demonstrated antagonistic activity on apomorphine-induced climbing and on L-DOPA-dependent extrapolatory behavior in dose ranging between 0.4-4.0 mg/kg IP. It did not provoke a cataleptogenic effect or lethality, even at doses much higher than those causing antidopamine effects (more than 500 mg/kg). The effective doses of sulpiride in the above-listed antidopamine tests were shown to be 17.5 and 16.0 mg/kg IP correspondingly. Although these doses of sulpiride did not demonstrate cataleptogenic effects, an increase of the dose level to 120 mg/kg induced pronounced catalepsy. Both GZR-123 (6 mg/kg) and sulpiride (40 and 60 mg/kg) were investigated by training ratsto discriminate each of them from saline in a two-lever, water-reinforcement operant procedure. Both GZR-123 and sulpiride demonstrated weak discriminability in this task. GZR-123 increased drug-associated lever selection when administered in doses of 2 and 6 mg/kg, for sulpirirde these doses were demonstrated to be 25-60 mg/kg. In contrast to GZR-123, which did not provoke a sedative effect, sulpiride in higher discriminable doses caused sedation, which stems probably from the motivational, but not from the motor deficit. (C) 1999 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 15:18:26