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Titolo:
PHARMACOLOGICAL CHARACTERIZATION OF BUPRENORPHINE, A MIXED AGONIST-ANTAGONIST WITH KAPPA(3) ANALGESIA
Autore:
PICK CG; PETER Y; SCHREIBER S; WEIZMAN R;
Indirizzi:
TEL AVIV UNIV,SACKLER FAC MED,DEPT ANAT & ANTHROPOL IL-69978 RAMAT AVIV TEL AVIV ISRAEL HADASSAH UNIV HOSP,DEPT PSYCHIAT EIN KEREM JERUSALEM ISRAEL TEL AVIV UNIV,TEL AVIV COMMUNITY MENTAL HLTH CTR IL-69978 RAMAT AVIV TEL AVIV ISRAEL
Titolo Testata:
Brain research
fascicolo: 1, volume: 744, anno: 1997,
pagine: 41 - 46
SICI:
0006-8993(1997)744:1<41:PCOBAM>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
NALOXONE BENZOYLHYDRAZONE; ANTINOCICEPTION; RECEPTORS; MORPHINE; MICE;
Keywords:
ANALGESIA; BUPRENORPHINE; NALOXONE BENZOYLHYDRAZONE; OPIATE RECEPTOR (MIXED AGONIST/ANTAGONIST);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
18
Recensione:
Indirizzi per estratti:
Citazione:
C.G. Pick et al., "PHARMACOLOGICAL CHARACTERIZATION OF BUPRENORPHINE, A MIXED AGONIST-ANTAGONIST WITH KAPPA(3) ANALGESIA", Brain research, 744(1), 1997, pp. 41-46

Abstract

Buprenorphine is a mixed opioid agonist/antagonist analgesic. This study was designed to determine the role of opioid receptor subtypes, especially kappa(3), in buprenorphine-induced analgesia in mice. Buprenorphine, when injected systemically, revealed a potent analgesic effectby taiIflick assay, with a biphasic dose-response curve, which was reversed by naloxone. The presence of analgesic cross-tolerance between buprenorphine and naloxone benzoylhydrazone (NalBzoH) and morphine indicated a role for kappa(3) and mu receptor subtype in buprenorphine analgesia. Additional studies with selective opioid antagonists indicated kappa(1) mechanisms of action. We did not detect any involvement of the delta receptor subtype. Low doses of buprenorphine antagonized morphine analgesia, while high doses of buprenorphine coadministered withmorphine elicited increasing analgesia in a dose-dependent manner. These findings suggest that buprenorphine elicits analgesia through an interaction with kappa(3) receptors and to a lesser extent with kappa(1) as well as its activity as partial mu receptor agonist.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/07/20 alle ore 21:29:37