Science · 1992 · 1.2K citations · 23 references
MedicineMolecular BiologyPharmacologyCell SignalingNeuropharmacologySignal TransductionDrug-receptor InteractionsLigand BindingNeurotransmitter ReceptorsOpioid AnalgesicsReceptor BindingReceptor-ligand InteractionsComplementary Dna (Cdna) CloningG Protein-coupled Neuropeptide ReceptorsG-protein-coupled ReceptorsMolecular CharacterizationOpioid Receptor BindingTransient ExpressionTransient Expression SystemsTransient Gene Expression
Opiate drugs are potent analgesics and addictive agents that act on receptors also responsive to endogenous opioid peptides, yet the molecular identity of these opioid receptors had remained elusive. The authors identified a cDNA clone encoding a functional δ opioid receptor by transiently expressing it in COS cells and screening with an iodinated enkephalin analog, and the sequence shows homology to G protein‑coupled receptors such as those for somatostatin, angiotensin, and interleukin‑8.
Opiate drugs have potent analgesic and addictive properties. These drugs interact with receptors that also mediate the response to endogenous opioid peptide ligands. However, the receptors for opioids have eluded definitive molecular characterization. By transient expression in COS cells and screening with an iodinated analog of the opioid peptide enkephalin, a complementary DNA clone encoding a functional δ opioid receptor has been identified. The sequence shows homology to G protein-coupled receptors, in particular the receptors for somatostatin, angiotensin, and interleukin-8.
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Identification of two related pentapeptides from the brain with potent opiate agonist activity
Joel W. Hughes, Terry Smith, H. W. Kosterlitz et al. · Nature · 1975 · 3.8K citations
Endogenous opioid peptides: multiple agonists and receptors
John A.H. Lord, Angela A. Waterfield, John Hughes et al. · Nature · 1977 · 2.5K citations
Opiate Receptor: Demonstration in Nervous Tissue
Candace B. Pert, Solomon H. Snyder · Science · 1973 · 2.4K citations
Medicine, Neuroscience, Pharmacology +10