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Titolo:
ANTINOCICEPTIVE ACTION OF DBO-17 AND DBO-11 IN MICE - 2 3,8-DIAZABICYCLO(3.2.1.)OCTANE DERIVATES WITH SELECTIVE MU-OPIOID RECEPTOR AFFINITY
Autore:
FADDA P; BARLOCCO D; TRONCI S; CIGNARELLA G; FRATTA W;
Indirizzi:
UNIV CAGLIARI,BB BRODIE DEPT NEUROSCI,VIA PORCELL 4 I-09124 CAGLIARI ITALY UNIV CAGLIARI,BB BRODIE DEPT NEUROSCI I-09124 CAGLIARI ITALY CNR,CTR STUDIO NEUROFARMACOL I-09124 CAGLIARI ITALY UNIV MODENA,DIPARTIMENTO SCI FARMACEUT I-41100 MODENA ITALY UNIV MILAN,IST CHIM FARMACEUT & TOSSICOL I-20131 MILAN ITALY
Titolo Testata:
Naunyn-Schmiedeberg's archives of pharmacology
fascicolo: 5, volume: 356, anno: 1997,
pagine: 596 - 602
SICI:
0028-1298(1997)356:5<596:AAODAD>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
NALORPHINE-LIKE DRUGS; CHRONIC SPINAL DOG; OPIATE RECEPTORS; MORPHINE-LIKE; DEPENDENCE; TOLERANCE; BRAIN;
Keywords:
3,8 DIAZABICYCLO (3.2.1.) OCTANE DERIVATES; ANTINOCICEPTION; TOLERANCE; DEPENDENCE; MICE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
20
Recensione:
Indirizzi per estratti:
Citazione:
P. Fadda et al., "ANTINOCICEPTIVE ACTION OF DBO-17 AND DBO-11 IN MICE - 2 3,8-DIAZABICYCLO(3.2.1.)OCTANE DERIVATES WITH SELECTIVE MU-OPIOID RECEPTOR AFFINITY", Naunyn-Schmiedeberg's archives of pharmacology, 356(5), 1997, pp. 596-602

Abstract

Two 3,8 diazabicyclo (3.2.1.) octane derivates, namely DBO 17 and DBO11, were studied for the opioidlike activity. In the rat brain membrane preparation binding studies, DBO 17 and DBO 11 showed a high affinity and selectivity for the mu opioid receptor (K-i's: 5.1 and 25 nM, respectively). DBO 17 and DBO 11 inhibited the nociceptive response in the hot-plate test of mice with ED50 values of 0.16 mg/kg and 0.44 mg/kg, respectively. The antinociceptive action of both DBO 17 and DBO 11was blocked by naloxone. Tolerance to the antinociceptive ac tion of DBO 17 and DBO 11 was present after 13 and 7 days of repeated treatment, respectively. Both DBO 17 and DBO 11 were ineffective in morphine-tolerant mice and vice versa. Chronic treatments (three times daily forseven consecutive days) of DBO 17 and DBO 11 induced a naloxone-precipitated withdrawal syndrome in DBO 17 treated mice similar to that in morphine treated mice, whereas in DBO 11 treated mice abstinence signswere virtually absent. These results indicate an interesting pharmacological profile that suggests these compounds as possible new candidates for the clinical treatment of pain.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 22:46:09