TYPE 1 AND TYPE 2 OPIATE RECEPTORS: A SUBCLASSIFICATION SCHEME BASED UPON GTP'S DIFFERENTIAL EFFECTS ON BINDING
作者： Candace B. Pert , Duncan Taylor
DOI: 10.1016/B978-0-08-025488-3.50027-1
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摘要: Summary We present evidence for a simple opiate receptor subclassification scheme analogous to the one recently proposed dopamine receptor. The Type 1 is GTP-sensitive, adenylate cyclase-coupled and associated with soium ionophore. 2 GTP-resistant uncoupled. find receptors predominantly in ileum most of rat brain, particularly areas which mediate analgesia; predominate limbic system, neuroblastoma-glioma cell hybrid, vas deferens , pituitary invertebrate nervous systems. are easily reversed by naloxone, while even resistant naloxone blockade. Comparisons receptor-enriched area (midbrain) (frontal cortex) revealed following ligand selectivity (in order strongest preference 1): > morphine diprenorphine ≃= N-allylnormetazocine ketocyclazocine ≃ = cyclazocine B-endorphin D-Ala-enkephalin amide met-enkephalin leu-enkephalin. Benzo-morphans generally lack but differ their relative affinity antagonist conformation (σ).
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