Molecular biology and pharmacology of cloned opioid receptors

R. J. Knapp, E. Malatynska, N. Collins, L. Fang, J. Y. Wang, Victor J Hruby, William R Roeske, H. I. Yamamura

Research output: Contribution to journalArticle

206 Citations (Scopus)

Abstract

The cloning and expression of DNA for the three major opioid receptor types (μ, δ, and κ) present new research opportunities for the characterization of opioid drugs and their interactions with these receptors. Genomic and cDNA clones for opioid receptors exist for several animal species including mouse, rat, guinea pig, and human. These include clones for all three human opioid receptor types. The receptor proteins consist of about 400 amino acids and have the characteristic seven transmembrane domain structure of G-protein-coupled receptors. There is about 60% amino acid identity between opioid receptor types and about 90% identity between a receptor type cloned from different animal species. All opioid receptor types mediate the inhibition of adenylyl cyclase in response to agonist binding. Radioligand binding and functional studies using the cloned receptors tend to support current conclusions on opioid drug receptor selectivity and activity. Investigations of opioid receptor chimeras and single amino acid mutants are providing information on the ligand recognition sites of these receptors and essential support for the development of computational opioid receptor models. A molecular model of the human δ opioid receptor is included in this review.

Original languageEnglish (US)
Pages (from-to)516-525
Number of pages10
JournalFASEB Journal
Volume9
Issue number7
StatePublished - 1995

Fingerprint

Molecular biology
narcotics
Opioid Receptors
pharmacology
molecular biology
Molecular Biology
Pharmacology
receptors
Amino Acids
Opioid Analgesics
Animals
Clone Cells
Drug Receptors
Cloning
Molecular Models
amino acids
G-Protein-Coupled Receptors
Adenylyl Cyclases
Drug Interactions
Rats

Keywords

  • adenylyl cylase
  • antisense oligonucleotides
  • cAMP formation
  • cDNA
  • cloning
  • endorphin receptors
  • expression
  • G-protein
  • molecular modeling
  • site-directed mutagenesis

ASJC Scopus subject areas

  • Agricultural and Biological Sciences (miscellaneous)
  • Biochemistry, Genetics and Molecular Biology(all)
  • Biochemistry
  • Cell Biology

Cite this

Knapp, R. J., Malatynska, E., Collins, N., Fang, L., Wang, J. Y., Hruby, V. J., ... Yamamura, H. I. (1995). Molecular biology and pharmacology of cloned opioid receptors. FASEB Journal, 9(7), 516-525.

Molecular biology and pharmacology of cloned opioid receptors. / Knapp, R. J.; Malatynska, E.; Collins, N.; Fang, L.; Wang, J. Y.; Hruby, Victor J; Roeske, William R; Yamamura, H. I.

In: FASEB Journal, Vol. 9, No. 7, 1995, p. 516-525.

Research output: Contribution to journalArticle

Knapp, RJ, Malatynska, E, Collins, N, Fang, L, Wang, JY, Hruby, VJ, Roeske, WR & Yamamura, HI 1995, 'Molecular biology and pharmacology of cloned opioid receptors', FASEB Journal, vol. 9, no. 7, pp. 516-525.
Knapp RJ, Malatynska E, Collins N, Fang L, Wang JY, Hruby VJ et al. Molecular biology and pharmacology of cloned opioid receptors. FASEB Journal. 1995;9(7):516-525.
Knapp, R. J. ; Malatynska, E. ; Collins, N. ; Fang, L. ; Wang, J. Y. ; Hruby, Victor J ; Roeske, William R ; Yamamura, H. I. / Molecular biology and pharmacology of cloned opioid receptors. In: FASEB Journal. 1995 ; Vol. 9, No. 7. pp. 516-525.
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