The opiate receptor: a model explaining structure-activity relationships of opiate agonists and antagonists.
A model of the opiate receptor is proposed which explains structure-activity relationships of opiate drugs, including (i) the unique potency of certain opiates such as etonitazene, fentanyl, phenazocine, and oripavines; (ii) the role of N-allyl substituents in conferring antagonist properties; and (iii) chemical features that afford "pure" antagonists. The model indicates mlecular mechanisms for interconversion of the opiate receptor between respective states that bind agonists or antagonists with high affinity.
D000494:Allosteric Regulation; D011431:Dextropropoxyphene; D005283:Fentanyl; D008691:Methadone; D008954:Models, Biological; D008958:Models, Molecular; D008968:Molecular Conformation; D009020:Morphine; D009269:Nalorphine; D009270:Naloxone; D009294:Narcotics / Q000378:metabolism*; D010423:Pentazocine; D010620:Phenazocine; D011487:Protein Conformation; D011957:Receptors, Opioid / Q000378:metabolism*; D013329:Structure-Activity Relationship
D009294:Narcotics; D011957:Receptors, Opioid; D009270:Naloxone; D009020:Morphine; D010620:Phenazocine; D010423:Pentazocine; D011431:Dextropropoxyphene; D009269:Nalorphine; D008691:Methadone; D005283:Fentanyl