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Titolo:
PRECLINICAL PHARMACOLOGICAL ACTIONS OF (+ YDRO-5',6'-METHYLENE-DIOXY-1'-NAPHTHALENYL)METHYL] PYRROLIDINE METHANESULFONATE (ABT-200), A POTENTIAL ANTIDEPRESSANT AGENT THAT ANTAGONIZES ALPHA-2-ADRENERGIC RECEPTORS AND INHIBITS THE NEURONAL UPTAKE OF NOREPINEPHRINE/
Autore:
HANCOCK AA; BUCKNER SA; GIARDINA WJ; BRUNE ME; LEE JY; MORSE PA; OHEIM KW; STANISIC DS; WARNER RB; KERKMAN DJ; DEBERNARDIS JF;
Indirizzi:
ABBOTT LABS,DIV PHARMACEUT PROD,DIV CARDIOVASC RES ABBOTT PK IL 60064
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 3, volume: 272, anno: 1995,
pagine: 1160 - 1169
SICI:
0022-3565(1995)272:3<1160:PPAO(Y>2.0.ZU;2-1
Fonte:
ISI
Lingua:
ENG
Soggetto:
FORCED SWIMMING TEST; ALPHA-2-ADRENOCEPTOR BLOCKADE; CLINICAL-PHARMACOLOGY; ANIMAL-MODELS; RATS; DRUGS; IDENTIFICATION; DEPRESSION; THERAPY; RELEASE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
44
Recensione:
Indirizzi per estratti:
Citazione:
A.A. Hancock et al., "PRECLINICAL PHARMACOLOGICAL ACTIONS OF (+ YDRO-5',6'-METHYLENE-DIOXY-1'-NAPHTHALENYL)METHYL] PYRROLIDINE METHANESULFONATE (ABT-200), A POTENTIAL ANTIDEPRESSANT AGENT THAT ANTAGONIZES ALPHA-2-ADRENERGIC RECEPTORS AND INHIBITS THE NEURONAL UPTAKE OF NOREPINEPHRINE/", The Journal of pharmacology and experimental therapeutics, 272(3), 1995, pp. 1160-1169

Abstract

-tetrahydro-5',6'-methylene-dioxy-1'-naphthalenyl) methyl] pyrrolidine methanesulfonate (ABT-200) was evaluated in a number of biological tests to establish its pharmacological profile of activity. ABT-200 antagonized the uptake of [H-3]-norepinephrine into synaptosomes of rat hypothalamus (IC50 = 841 nM) and blocked 4,alpha-dimethyl-m-tyramine-induced hypermotility in rats. in addition, ABT-200 potently inhibited binding of [H-3]-rauwolscine to alpha-2 adrenergic receptors with a K-ivalue in radioligand binding assays of approximately 1 nM in the rat cortex and was much less potent at other receptor binding sites. ABT-200 antagonized alpha-2 receptors in vitro in the rat vas deferens and dog saphenous vein, where pA(2) values of 7.7 and 8.2, respectively, were obtained. ABT-200 also antagonized clonidine-induced mydriasis andincreased the overflow of [H-3]-norepinephrine in guinea pig hippocampal slices, manifestations of blockade of alpha-2 adrenoceptors in thecentral nervous system. ABT-200 was active in antagonizing nocturnal hyperactivity in olfactory bulbectomized rats, a test for putative antidepressant activity. In cardiovascular studies, ABT-200 exhibited negligible activity in affecting hemodynamic parameters and was free of postural hypotensive activity, In both in vitro and in vivo tests, ABT-200 was devoid of antihistaminic or anticholinergic activity. This profile of activity of moderate inhibition of norepinephrine uptake with blockade of alpha-2 adrenoceptors suggests potential dual-action effects for ABT-200, which may represent a putative antidepressant with minimal cardiovascular side-effect liability.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/04/20 alle ore 06:39:31