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Titolo:
STRUCTURE-ACTIVITY-RELATIONSHIPS OF TRANS-3,4-DIMETHYL-4-(3-HYDROXYPHENYL)PIPERIDINE ANTAGONISTS FOR MU-OPIOID AND KAPPA-OPIOID RECEPTORS
Autore:
ZIMMERMAN DM; LEANDER JD; CANTRELL BE; REEL JK; SNODDY J; MENDELSOHN LG; JOHNSON BG; MITCH CH;
Indirizzi:
ELI LILLY & CO,LILLY RES LAB,DIV CNS INDIANAPOLIS IN 46285
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 20, volume: 36, anno: 1993,
pagine: 2833 - 2841
SICI:
0022-2623(1993)36:20<2833:SOT>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
NALORPHINE-LIKE DRUGS; CHRONIC SPINAL DOG; INCREASED URINATION; MORPHINE-LIKE; PEPTIDES; PICENADOL; AGONISTS; LIGAND; RAT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
D.M. Zimmerman et al., "STRUCTURE-ACTIVITY-RELATIONSHIPS OF TRANS-3,4-DIMETHYL-4-(3-HYDROXYPHENYL)PIPERIDINE ANTAGONISTS FOR MU-OPIOID AND KAPPA-OPIOID RECEPTORS", Journal of medicinal chemistry, 36(20), 1993, pp. 2833-2841

Abstract

A series of racemic N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines were evaluated for opioid agonist and antagonist activity at mu and kappa receptors. Several highly potent mu and kappa antagonists were discovered; however, no compounds with high selectivity for either the mu or kappa receptor were identified. Importantly, no derivative was found to have significant opioid agonist activity. Two derivatives were resolved, and the activities of the enantiomers were investigated. Only a limited stereochemical effect on opioid receptor selectivities was observed. The structure-activity relationships described establish the existence of an important lipophilic binding site distal to the nitrogen for both mu and kappa receptors and confirm the pure opioid antagonist pharmacophore nature of the trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine structure.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 22:34:12