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Titolo:
NOVEL HYPOTENSIVE AGENTS FROM VERBESINA-CARACASANA .2. SYNTHESIS AND PHARMACOLOGY OF CARACASANAMIDE
Autore:
DELLEMONACHE G; BOTTA B; DELLEMONACHE F; ESPINAL R; DEBONNEVAUX SC; DELUCA C; BOTTA M; CORELLI F; CARMIGNANI M;
Indirizzi:
CTR CHIM RECETTORI,LARGO F VITO 1 I-00168 ROME ITALY UNIV CARABOBO,DEPT FARMACOL CALABOZO VENEZUELA CTR ELETTROCHIM & CHIM FIS INTERFASI ROME ITALY UNIV AQUILA,DIPARTIMENTO BIOL & FISIOL CELLULARE,SEZ FARMACOL I-67010COPPITO ITALY UNIV SIENA,DIPARTIMENTO FARM CLIN TECHNOL I-53100 SIENA ITALY
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 20, volume: 36, anno: 1993,
pagine: 2956 - 2963
SICI:
0022-2623(1993)36:20<2956:NHAFV.>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
CARDIOVASCULAR REGULATION; THERAPEUTIC EFFICACY; HYPERTENSION; MECHANISMS; GUANABENZ; PINACIDIL;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
35
Recensione:
Indirizzi per estratti:
Citazione:
G. Dellemonache et al., "NOVEL HYPOTENSIVE AGENTS FROM VERBESINA-CARACASANA .2. SYNTHESIS AND PHARMACOLOGY OF CARACASANAMIDE", Journal of medicinal chemistry, 36(20), 1993, pp. 2956-2963

Abstract

Caracasanamide, one of the hypotensive agents isolated from Verbesinacaracasana, is a mixture of (Z)-1a and (E)-lb forms of )amino]-4-[(3-methyl-2-butenyl)-guanidino]butane.1 The structure of (E)-caracasanamide (1b) was confirmed by high-yielding synthesis starting from N,N'-bis(tert-butoxycarbonyl)-S-methylisothiourea. The water-soluble Z-form of 1a, assayed by iv route in anesthetized rats at doses ranging from 50 to 1600 mug/kg body weight, was found to decrease blood pressure, toincrease cardiac inotropism, respiratory frequency, and tidal volume,and to induce a very slight and not significant tachycardia. Higher doses determined respiratory depression and, in some cases, consequent cardiac arrest. The compound was shown to affect cardiovascular function by acting at the vascular level in inducing arterial vasodilation, by determining sympathetic hypotone through central neurogenic mechanisms, and by interacting with the cardiac beta1-adrenoreceptors. The respiratory effects were independent of the cardiovascular ones. In lowering blood pressure, the compound was more potent than guanethidine and not less potent than reserpine and papaverine. (Z)-Caracasanamide may therefore be useful in the treatment of arterial hypertension of moderate degree.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/10/20 alle ore 09:57:59