kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system

Proc Natl Acad Sci U S A. 1995 Jul 18;92(15):7006-10. doi: 10.1073/pnas.92.15.7006.


Using the mouse delta-opioid receptor cDNA as a probe, we have isolated genomic clones encoding the human mu- and kappa-opioid receptor genes. Their organization appears similar to that of the human delta receptor gene, with exon-intron boundaries located after putative transmembrane domains 1 and 4. The kappa gene was mapped at position q11-12 in human chromosome 8. A full-length cDNA encoding the human kappa-opioid receptor has been isolated. The cloned receptor expressed in COS cells presents a typical kappa 1 pharmacological profile and is negatively coupled to adenylate cyclase. The expression of kappa-opioid receptor mRNA in human brain, as estimated by reverse transcription-polymerase chain reaction, is consistent with the involvement of kappa-opioid receptors in pain perception, neuroendocrine physiology, affective behavior, and cognition. In situ hybridization studies performed on human fetal spinal cord demonstrate the presence of the transcript specifically in lamina II of the dorsal horn. Some divergences in structural, pharmacological, and anatomical properties are noted between the cloned human and rodent receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenylyl Cyclases
  • Aged
  • Amino Acid Sequence
  • Base Sequence
  • Central Nervous System / chemistry*
  • Central Nervous System / physiology
  • Chromosome Mapping
  • Chromosomes, Human, Pair 8 / genetics*
  • Cloning, Molecular
  • DNA, Complementary / genetics
  • Exons / genetics
  • Genomic Library
  • Humans
  • In Situ Hybridization
  • Ligands
  • Middle Aged
  • Molecular Sequence Data
  • RNA, Messenger / isolation & purification
  • Receptors, Opioid, kappa / genetics*
  • Receptors, Opioid, kappa / isolation & purification
  • Receptors, Opioid, kappa / metabolism
  • Receptors, Opioid, mu / genetics*
  • Receptors, Opioid, mu / isolation & purification
  • Receptors, Opioid, mu / metabolism
  • Recombinant Proteins / metabolism
  • Sequence Homology, Amino Acid
  • Signal Transduction
  • Tissue Distribution


  • DNA, Complementary
  • Ligands
  • RNA, Messenger
  • Receptors, Opioid, kappa
  • Receptors, Opioid, mu
  • Recombinant Proteins
  • Adenylyl Cyclases

Associated data

  • GENBANK/U17298