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Titolo:
THE IN-VITRO PHARMACOLOGICAL CHARACTERIZATION OF NALOXONE BENZOYLHYDRAZONE
Autore:
BERZETEIGURSKE IP; WHITE A; POLGAR W; DECOSTA BR; PASTERNAK GW; TOLL L;
Indirizzi:
SRI INT,DEPT NEUROSCI,BLDG LA,ROOM 105,333 RAVENSWOOD AVE MENLO PK CA94025 NIDDK,MED CHEM LAB BETHESDA MD 20892 MEM SLOAN KETTERING CANC CTR,DEPT NEUROL & PHARMACOL NEW YORK NY 10021
Titolo Testata:
European journal of pharmacology
fascicolo: 2-3, volume: 277, anno: 1995,
pagine: 257 - 263
SICI:
0014-2999(1995)277:2-3<257:TIPCON>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG BRAIN; KAPPA-OPIOID RECEPTOR; BINDING; LIGAND; OPIATE; ANTAGONIST; MULTIPLICITY; MORPHINE; AGONISTS; INVIVO;
Keywords:
NALOXONE BENZOYLHYDRAZONE; ILEUM, GUINEA PIG; KAPPA-OPIOID RECEPTOR; RECEPTOR BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
23
Recensione:
Indirizzi per estratti:
Citazione:
I.P. Berzeteigurske et al., "THE IN-VITRO PHARMACOLOGICAL CHARACTERIZATION OF NALOXONE BENZOYLHYDRAZONE", European journal of pharmacology, 277(2-3), 1995, pp. 257-263

Abstract

On the basis of its in vivo activity and binding affinity, naloxone benzoylhydrazone has been characterized as a kappa(3)-opioid receptor agonist and a mu-opioid receptor antagonist. This paper continues its pharmacological characterization with the help of isolated tissue preparations. Naloxone benzoylhydrazone was found to have partial agonist activity in the guinea pig ileum longitudinal muscle/myenteric plexus preparation. As an antagonist, naloxone benzoylhydrazone is similar to naloxone, with pA(2) values of 8.8, 7.8, and 7.8 for mu-, delta-, and kappa(1)-opioid receptors, respectively. Its agonist activity in the guinea pig ileum preparation was not influenced by beta-funaltrexamine treatment but was reversed by the selective kappa-opioid receptor antagonist nor-binaltorphimine and by the irreversible kappa(1)-opioid receptor blocker UPHIT rans-2-isothiocyanato-4,5-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl] benzeneacetamide. The presence of kappa(3)-opioid receptors could not be demonstrated by [H-3]naloxone benzoylhydrazone binding in the guinea pig ileum longitudinal muscle/myentericplexus preparation. From these studies it is concluded that the partial agonist activity of naloxone benzoylhydrazone in this bioassay is probably due to the activation of the kappa(1)-opioid receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/07/20 alle ore 12:33:54