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Titolo:
PHARMACOLOGICAL CHARACTERIZATION OF THE CLONED KAPPA-OPIOID RECEPTOR AS A KAPPA(1B) SUBTYPE
Autore:
LAI J; MA SW; ZHU RH; ROTHMAN RB; LENTES KU; PORRECA F;
Indirizzi:
UNIV ARIZONA,ARIZONA HLTH SCI CTR,DEPT PHARMACOL TUCSON AZ 85724 UNIV ARIZONA,ARIZONA HLTH SCI CTR,DEPT PHARMACOL TUCSON AZ 85724 NIDA,ADDICT RES CTR BALTIMORE MD 21224 MAX PLANCK INST BIOPHYS CHEM GOTTINGEN GERMANY
Titolo Testata:
NeuroReport
fascicolo: 16, volume: 5, anno: 1994,
pagine: 2161 - 2164
SICI:
0959-4965(1994)5:16<2161:PCOTCK>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG BRAIN; BINDING-SITES; NALOXONE BENZOYLHYDRAZONE; DIFFERENTIAL ANTAGONISM; OPIATE RECEPTOR; MULTIPLICITY; DRUGS; ANTINOCICEPTION; FEDOTOZINE; PEPTIDES;
Keywords:
RECEPTORS; OPIOID; KAPPA SUBTYPES; CLONED KAPPA RECEPTOR; MOUSE BRAIN; RADIOLIGAND BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
21
Recensione:
Indirizzi per estratti:
Citazione:
J. Lai et al., "PHARMACOLOGICAL CHARACTERIZATION OF THE CLONED KAPPA-OPIOID RECEPTOR AS A KAPPA(1B) SUBTYPE", NeuroReport, 5(16), 1994, pp. 2161-2164

Abstract

SUBSTANTIAL pharmacological evidence in vitro and in vivo has suggested the existence of subtypes of the kappa opioid receptor. Quantitative radioligand binding techniques resolved the presence of two high affinity binding sites for the kappa(1) ligand [H-3]U69,593 in mouse brain membranes, termed kappa(1a) and kappa(1b), respectively. Whereas thekappa(1a) site has high affinity for fedotozine and oxymorphindole and low affinity for bremazocine and alpha-neoendorphin, site kappa(1b) has high affinity for bremazocine and alpha-neoendorphin and low affinity for fedotozine and oxymorphindole. CI-977 and U69,593 bind equallywell at both sites. To determine the relationship between these kappa(1) receptor subtypes and the recently cloned mouse kappa(1) receptor (KOR), we examined [H-3]U69,593 binding to the KOR in stably transfected cells (KORCHN-8). Competition of [H-3]U69,593 binding to the KOR bybremazocine, alpha-neoendorphin, fedotozine and oxymorphindole resolved a single class of binding sites at which these agents had binding affinities similar to that of the kappa(1b) site present in mouse brain. These results suggest that the cloned KOR corresponds to the kappa(1) site in mouse brain defined as kappa(1b).

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Documento generato il 14/07/20 alle ore 18:44:25