Benextramine and nifedipine distinguish between sub-classes of alpha 1-adrenoceptors.
The effects of benextramine and nifedipine were examined on the dose-diastolic pressure response to methoxamine in pithed normotensive rats. Benextramine (3, 6 and 12 mg/Kg) displaced the dose-response curve to methoxamine to the right. Maximum response was reduced after the administration of 12 mg/Kg benextramine. Nifedipine (0.1 and 0.3 mg/Kg) also caused the dose-response curve to methoxamine to be displaced to the right with reduction in maximum response. Nifedipine effects were additive with an increase in the EC50 values as well as reduction in the maximum response after pretreatment with benextramine (3 and 6 mg/Kg). However, at the highest dose of benextramine the effects of nifedipine were diminished and no longer apparent. It is concluded that benextramine may have alkylated a nifedipine sensitive site on the alpha 1-adrenoceptors.
Tabrizchi
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Division of Basic Medical Sciences, Faculty of Medicine, Memorial University of Newfoundland, St. John's, Canada.
Triggle
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D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001831:Body Temperature; D003538:Cystamine / Q000494:pharmacology / Q000031:analogs & derivatives; D003655:Decerebrate State; D003971:Diastole / Q000187:drug effects; D008297:Male; D008729:Methoxamine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D009543:Nifedipine / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000145:classification / Q000187:drug effects*
D011942:Receptors, Adrenergic, alpha; C029998:benextramine; D008729:Methoxamine; D009543:Nifedipine; D003538:Cystamine