Pharmacological characterization of the cloned kappa opioid receptor as a kappa(1b) subtype

J. Lai, S. W. Ma, R. H. Zhu, Frank Porreca, K. U. Lentes, F. Porreca

Research output: Contribution to journalArticle

26 Citations (Scopus)

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 κ1 ligand [3H]U69,593 in mouse brain membranes, termed κ(1a) and κ(1b) respectively. Whereas the κ(1b) site has high affinity for fedotozine and oxymorphindole and low affinity for bremazocine and (α-neoendorphin, site κ(1b) has high affinity for bremazocine and α-neoendorphin and low affinity for fedotozine and oxymorphindole. CI-977 and U69,593 bind equally well at both sites. To determine the relationship between these K1 receptor subtypes and the recently cloned mouse κ1 receptor (KOR), we examined [3H]U69,593 binding to the KOR in stably transfected cells (KORCHN-8). Competition of [3H]U69,593 binding to the KOR by bremazocine, α-neoendorphin, fedotozine and oxymorphindole resolved a single class of binding sites at which these agents had binding affinities similar to that of the κ(1b) site present in mouse brain. These results suggest that the cloned KOR corresponds to the κ1 site in mouse brain defined as κ(1b).

Original languageEnglish (US)
Pages (from-to)2161-2164
Number of pages4
JournalNeuroReport
Volume5
Issue number16
StatePublished - 1994

Fingerprint

kappa Opioid Receptor
Pharmacology
Brain
Binding Sites
Ligands
Membranes
fedotozine
bremazocine
oxymorphindole

Keywords

  • Cloned kappa receptor
  • Kappa subtypes
  • Mouse brain
  • Opioid
  • Radioligand binding
  • Receptors

ASJC Scopus subject areas

  • Neuroscience(all)

Cite this

Lai, J., Ma, S. W., Zhu, R. H., Porreca, F., Lentes, K. U., & Porreca, F. (1994). Pharmacological characterization of the cloned kappa opioid receptor as a kappa(1b) subtype. NeuroReport, 5(16), 2161-2164.

Pharmacological characterization of the cloned kappa opioid receptor as a kappa(1b) subtype. / Lai, J.; Ma, S. W.; Zhu, R. H.; Porreca, Frank; Lentes, K. U.; Porreca, F.

In: NeuroReport, Vol. 5, No. 16, 1994, p. 2161-2164.

Research output: Contribution to journalArticle

Lai, J, Ma, SW, Zhu, RH, Porreca, F, Lentes, KU & Porreca, F 1994, 'Pharmacological characterization of the cloned kappa opioid receptor as a kappa(1b) subtype', NeuroReport, vol. 5, no. 16, pp. 2161-2164.
Lai, J. ; Ma, S. W. ; Zhu, R. H. ; Porreca, Frank ; Lentes, K. U. ; Porreca, F. / Pharmacological characterization of the cloned kappa opioid receptor as a kappa(1b) subtype. In: NeuroReport. 1994 ; Vol. 5, No. 16. pp. 2161-2164.
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