morphinans and 18-19-dihydroetorphine

Buprenorphine is a partial agonist at the micro -opioid receptor with long duration of action and also exhibits delayed antagonist activity. Buprenorphine is finding increasing use as a treatment agent for opioid abuse, though its low efficacy is not well tolerated by all addicts. There is interest in developing a higher efficacy version of buprenorphine and in this mini-review some of the ligands recently discovered, that share with buprenorphine a profile of agonism followed by delayed antagonism, are discussed.

Topics: Analgesics, Opioid; Animals; Buprenorphine; Drug Evaluation, Preclinical; Etorphine; Humans; Hydromorphone; Ligands; Morphinans; Narcotic Antagonists; Receptors, Opioid, mu; Structure-Activity Relationship; Substance-Related Disorders

Topics: Animals; Brain Chemistry; Etorphine; Mice; Morphinans; Rabbits

Topics: Administration, Sublingual; Analgesics; Animals; Biological Availability; Etorphine; Female; Male; Mice; Morphinans

Topics: Adolescent; Analgesics, Opioid; Anesthesia; Cardiac Surgical Procedures; Child; Etorphine; Female; Fentanyl; Heart Septal Defects, Ventricular; Humans; Male; Morphinans; Nitrous Oxide

Topics: Alkaloids; Anesthesia, General; Anesthesia, Intravenous; Animals; Antipsychotic Agents; Benzilates; Berberine Alkaloids; Diazepam; Dogs; Drug Interactions; Etorphine; Female; Male; Mice; Morphinans; Piperidines; Rabbits

The respiratory inhibition caused by dihydroetorpine (DHE) was fully antagonized by pilocarpine or physostigmine, but the bradycardia was not. When atropine (icv) was combined with DHE, the respiratory inhibition was antagonized but the bradycardia persisted. However, intravenous atropine antagonized both the respiratory and cardiac inhibition caused by DHE.

Topics: Animals; Atropine; Cerebral Ventricles; Etorphine; Heart Rate; Injections, Intraventricular; Morphinans; Pilocarpine; Rabbits; Respiration

Topics: Analgesics; Animals; Dogs; Etorphine; Female; Immobilization; Male; Mice; Morphinans; Motor Activity; Nalorphine; Rabbits; Respiration

Topics: Analgesics; Animals; Etorphine; Female; Humans; Macaca mulatta; Male; Mice; Morphinans; Morphine Dependence; Opioid-Related Disorders; Substance Withdrawal Syndrome