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Titolo:
EFFECTS OF CATECHOL RING FLUORINATION ON CARDIOVASCULAR AND RENAL ACTIVITIES OF FENOLDOPAM ENANTIOMERS
Autore:
KINTER LB; MANN WA; WEINSTOCK J; RUFFOLO RR;
Indirizzi:
STERLING WINTHROP INC,DEPT LAB ANIM RESOURCES,POB 5000 COLLEGEVILLE PA 19426 SK&F LABS,DEPT PHARMACOL SWEDELAND PA 00000 SK&F LABS,DEPT MED CHEM SWEDELAND PA 00000
Titolo Testata:
Chirality
fascicolo: 5, volume: 6, anno: 1994,
pagine: 446 - 455
SICI:
0899-0042(1994)6:5<446:EOCRFO>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
DOPAMINE RECEPTOR AGONIST; CONSCIOUS DOGS; RENIN RELEASE; F 82526; ANTAGONIST; VASODILATOR; STIMULATION; ARTERIOLES; BLOCKADE;
Keywords:
BLOOD PRESSURE; RENAL VASODILATION; DOPAMINE AGONISTS; RENAL FUNCTION; RENAL BLOOD FLOW; DIURESIS; RENIN ANGIOTENSIN ALDOSTERONE SYSTEM;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
40
Recensione:
Indirizzi per estratti:
Citazione:
L.B. Kinter et al., "EFFECTS OF CATECHOL RING FLUORINATION ON CARDIOVASCULAR AND RENAL ACTIVITIES OF FENOLDOPAM ENANTIOMERS", Chirality, 6(5), 1994, pp. 446-455

Abstract

SK&F 87516 is a potent DA1 receptor agonist with demonstrated renal vasodilator activity. SK&F 87516 is the 6-fluoro analog of another DA1 agonist/renal vasodilator agent, fenoldopam. SK&F 87516 is a racemic mixture of two enantiomers, SK&F(R)-87516 and SK&F(S)-87516, and like fenoldopam, the (R)-enantiomer is responsible for the biological activities of the racemate. SK&F(R)-87516 is diuretic in spontaneously hypertensive rats and in dogs, whereas its enantiomer, SK&F(S)-87516 is inactive. SK&F(R)-87516 increases glomerular filtration rate, an effect which may account, in part, for its diuretic activity. Unlike fenoldopam, SK&F(R)-87516 is not associated with acute hypotensive activity, tachycardia, or stimulation of the renin-angiotensin-aldosterone system. The activity differences between SK&F(R)-87516 and fenoldopam are notrelated to differences in DA1 agonist potency. The activity differences may be due to the differing effects of fluorine and chlorine on theelectron distribution in the catechol ring, resulting in an enhanced effect of SK&F(R)-87516 at alpha2-adrenoceptors. (C) 1994 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/06/20 alle ore 23:59:53