Document Detail


Interactions of MEN 935 (adimolol), a long acting beta- and alpha-adrenolytic antihypertensive agent, with postsynaptic alpha-adrenoceptors in different isolated blood vessels--influence of angiotensin II.
MedLine Citation:
PMID:  3020439     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
MEN 935 [1-(3-[3-(1-naphthoxy)-2-hydroxypropyl) amino)-3,3-dimethylpropyl)-2-benzimidazolinone-hydrochloride monohydrate, adimolol] is a long acting antihypertensive agent with beta- and alpha-adrenolytic properties. Preliminary experiments in pithed rats had led to the suggestion that the alpha-adrenolytic activity was of the alpha 2-subtype. The alpha-adrenolytic properties of MEN 935 were now tested in isolated vascular preparations of rat aorta, rabbit vena ischiadica and rabbit vena cava inferior against the selective alpha 1-adrenergic agonist phenylephrine (PE) and the selective alpha 2-adrenergic agonist B-HT 920 [2-amino-6-allyl-5,6,7,8-tetrahydro-4H-thiazolo-(4,5-d)azepine]. The experiments were performed in absence and in presence of 5 X 10(-9) mol/l angiotensin II (A II). MEN 935 antagonized contractions to phenylephrine as well as those to B-HT 920 in each vessel. A twofold shift to the right of the concentration-response curves to both agonists was obtained with concentrations between 1.9 X 10(-8) and 1.4 X 10(-5) mol/l, depending on the vessel under investigation. A II modulated the adrenolytic properties of MEN 935 in each vessel. However, irrespective of the presence or absence of A II, no pharmacologically relevant difference between antagonism against PE or B-HT 920 could be seen. In isolated vessels, MEN 935 exerts a nonselective alpha-adrenergic antagonism. In receptor binding studies in rat cerebellar cortex, MEN 935 showed a Ki of 5.2 X 10(-7) mol/l at alpha 1-adrenoceptors and a Ki of 1.3 X 10(-5) mol/l at alpha 2-adrenoceptors.(ABSTRACT TRUNCATED AT 250 WORDS)
Authors:
R Palluk; W Hoefke; W Gaida; J Mierau; W D Bechtel
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Naunyn-Schmiedeberg's archives of pharmacology     Volume:  333     ISSN:  0028-1298     ISO Abbreviation:  Naunyn Schmiedebergs Arch. Pharmacol.     Publication Date:  1986 Jul 
Date Detail:
Created Date:  1986-10-30     Completed Date:  1986-10-30     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0326264     Medline TA:  Naunyn Schmiedebergs Arch Pharmacol     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  277-83     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Angiotensin II / pharmacology*
Animals
Azepines / pharmacology
Blood Vessels / metabolism*
Female
Male
Phenylephrine / pharmacology
Propanolamines / pharmacology*
Rabbits
Rats
Receptors, Adrenergic, alpha / drug effects*,  metabolism
Vasoconstriction / drug effects
Chemical
Reg. No./Substance:
0/Azepines; 0/Propanolamines; 0/Receptors, Adrenergic, alpha; 11128-99-7/Angiotensin II; 36085-73-1/talipexole; 59-42-7/Phenylephrine; 78459-19-5/adimolol

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