The partial opiate receptor agonists, dezocine and ciramadol act as mu receptor antagonists at the feline ileocecal sphincter.
The effects of two novel synthetic narcotic agonist/antagonists dezocine and ciramadol were examined at the ileocecal sphincter (ICS) in the intact anesthetized cat. Changes in blood pressure were seen with higher doses of both dezocine and ciramadol. No ICS pressure changes were seen in the ICS to dezocine and an increase in ICS pressure was seen only to the highest dose of ciramadol examined (10 mg/kg). The antagonist action of the two drugs were examined against submaximal doses of the mu receptor agonist morphine sulfate, delta receptor agonist methionine enkephalin and the k-receptor agonist dynorphin. Both drugs inhibit the ICS response to morphine sulfate. No inhibition of the responses to methionine enkephalin or dynorphin were seen with dezocine and only partial inhibition of the ICS response to dynorphin was seen with ciramadol.
Ouyang
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A
Gastrointestinal Section, Hospital of the University of Pennsylvania, Philadelphia 19104-4283.
D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D001596:Benzylamines / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002415:Cats; D003516:Cycloparaffins / Q000494:pharmacology*; D004399:Dynorphins / Q000037:antagonists & inhibitors / Q000494:pharmacology; D004744:Enkephalin, Methionine / Q000494:pharmacology; D007080:Ileocecal Valve / Q000187:drug effects*; D008297:Male; D009020:Morphine / Q000494:pharmacology; D009119:Muscle Contraction / Q000187:drug effects; D009292:Narcotic Antagonists; D011312:Pressure; D017450:Receptors, Opioid, mu; D013764:Tetrahydronaphthalenes
D000700:Analgesics; D001596:Benzylamines; D019086:Bridged Bicyclo Compounds, Heterocyclic; D003516:Cycloparaffins; D009292:Narcotic Antagonists; D017450:Receptors, Opioid, mu; D013764:Tetrahydronaphthalenes; D004744:Enkephalin, Methionine; D004399:Dynorphins; D009020:Morphine; C018273:ciramadol; C010827:dezocine