Abstract:
:1 The presynaptic alpha-adrenoceptor blocking activity of the newly synthesized alpha-adrenoceptor blocking drug, benextramine, was evaluated in the isolated left atrium of the guinea-pig heart. 2 High-voltage stimulation increased the force of contraction of electrically driven atrial strips, presumably by releasing noradrenaline from sympathetic nerve endings. Like phentolamine, benextramine increased the effect of high-voltage stimulation, presumably by blocking presynaptic alpha-adrenoceptors. 3 Clonidine reduced the effect of high-voltage stimulation, presumably by stimulating presynaptic alpha-adrenoceptors. The inhibitory effect of clonidine was antagonized noncompetitively by benextramine and competitively by phentolamine. 4 Combined administration of benextramine and phentolamine only resulted in the competitive phentolamine antagonism. Thus phentolamine protected the presynaptic alpha-adrenoceptors against benextramine blockade.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Belleau B,Benfey BG,Melchiorre Cdoi
10.1111/j.1476-5381.1982.tb09182.xsubject
Has Abstractpub_date
1982-04-01 00:00:00pages
617-21issue
4eissn
0007-1188issn
1476-5381journal_volume
75pub_type
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journal_title:British journal of pharmacology
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