The ligand-selectivity of cloned human and rat opiate mu receptors studied with [125I]IOXY-AGO

Richard B. Rothman, Heng Xu, Jia Bel Wang, John S. Partilla, Hiroshi Kayakiri, Kenner C. Rice, George R. Uhl

Research output: Contribution to journalArticlepeer-review

Abstract

The recent molecular cloning of μ, δ and κ opiate receptors (1-5) has created new opportunities for the study of opiate receptors. The recent cloning of the human μ receptor (6) has shown that there is a high homology between the predicted human and rat μ receptor sequences, but also some differences in sequence. We therefore sought significant changes in the ligand-selectivity profile of these two receptors expressed in the COS and CHO cell lines under identical assay conditions. We used the novel agonist ligand [125I]IOXY-AGO (6β-[125Iodo]-3,14-dihydroxy-17-methyl-4,5α-epoxymorphinan) since its high specific activity (2200 Ci/mmol) and high affinity for μ opioid receptors generated a high signal-to-noise ratio with use of relatively few expressing cells. (7). The results indicate substantial similarities in ligand-selectivity profile of the human and rat μ receptors, but also modest differences.

Original languageEnglish (US)
Pages (from-to)249-250
Number of pages2
JournalRegulatory Peptides
Volume54
Issue number1
DOIs
StatePublished - Nov 10 1994
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Neuroscience(all)

Fingerprint Dive into the research topics of 'The ligand-selectivity of cloned human and rat opiate mu receptors studied with [<sup>125</sup>I]IOXY-AGO'. Together they form a unique fingerprint.

Cite this