Cloning and functional comparison of κ and δ opioid receptors from mouse brain

Kazuki Yasuda, Karen Raynor, Haeyoung Kong, Christopher D. Breder, Jun Takeda, Terry Reisine, Graeme I. Bell

Research output: Contribution to journalArticlepeer-review

590 Scopus citations


While trying to identify new members of the somatostatin receptor family of G protein-coupled receptors, we isolated cDNAs from a mouse brain library encoding two related receptor-like proteins, designated msl-1 and msl-2, of 380 and 372 amino acids, respectively. There was 61% identity and 71% similarity between the sequences of msl-1 and msl-2. Among members of the G protein-coupled receptor superfamily, the sequences of both msl-1 and msl-1 were most closely related to those of the somatostatin receptors (SSTRs), having ≈35% identity with the sequence of SSTR1. Transient expression in COS-1 cells showed that msl-1 and msl-2 did not bind somatostatin. Rather they bound opioids selectively and with high affinity and had the pharmacological properties of κ and δ opioid receptors, respectively. Indeed, the sequence of msl-2 was identical to that of a δ opioid receptor recently cloned by other workers. Functional characterization of κ/msl-1 and δ/msl-2 opioid receptors showed that they were coupled to G proteins and mediated opioid receptor class-specific agonist inhibition of forskolin-stimulated cAMP formation. RNA blotting studies and in situ hybridization histochemistry showed that κ opioid receptor mRNA was expressed at high levels in brain in the neocortex, hippocampus, amygdala, medial habenula, hypothalamus (arcuate and paraventricular nuclei), locus ceruleus, and parabrachial nucleus, suggesting that this receptor may play a role in arousal and regulation of autonomic and neuroendocrine functions.

Original languageEnglish (US)
Pages (from-to)6736-6740
Number of pages5
JournalProceedings of the National Academy of Sciences of the United States of America
Issue number14
StatePublished - Jul 15 1993
Externally publishedYes


  • Cyclic AMP
  • Dynorphin
  • Enkephalin
  • G protein-coupled receptor
  • Neuropeptide

ASJC Scopus subject areas

  • General


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