Document Detail


Studies with abanoquil (UK-52,046) a novel quinoline alpha 1-adrenoceptor antagonist: I. Effects on blood pressure, heart rate and pressor responsiveness in normotensive subjects.
MedLine Citation:
PMID:  1683249     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
1. Abanoquil (UK 52,046) is a novel, quinoline-derivative, alpha 1-adrenoceptor antagonist which, on the basis of animal studies, possesses antiarrhythmic activity at doses which have little or no effect on blood pressure. 2. In two placebo-controlled, double-blind, crossover studies the alpha 1-adrenoceptor antagonist activity (phenylephrine pressor responses) and the effects on blood pressure and heart rate (in the presence and absence of concomitant beta-adrenoceptor blockade) have been investigated in healthy, normotensive subjects following the intravenous administration (i.v.) of abanoquil. 3. In the first study, abanoquil at a dose of 0.4 micrograms kg-1 i.v. (as a bolus or by increments) produced significant alpha 1-adrenoceptor antagonism (with rightward shifts of more than two-fold in the phenylephrine pressor dose-response curves) but no significant effects on supine or erect blood pressure and heart rate. 4. In the second study, a dose of 0.5 micrograms kg-1 i.v. had no significant effect on supine or erect blood pressure but pre-treatment with atenolol promoted a small fall in erect blood pressure without causing significant orthostatic hypotension. 5. In conclusion, significant alpha 1-adrenoceptor antagonism without marked reflex tachycardia or profound postural hypotension suggest that abanoquil has a different haemodynamic profile from that of 'classical' peripheral alpha 1-adrenoceptor antagonists.
Authors:
R F Schafers; H L Elliott; C A Howie; J L Reid
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Publication Detail:
Type:  Clinical Trial; Journal Article; Randomized Controlled Trial    
Journal Detail:
Title:  British journal of clinical pharmacology     Volume:  32     ISSN:  0306-5251     ISO Abbreviation:  Br J Clin Pharmacol     Publication Date:  1991 Nov 
Date Detail:
Created Date:  1991-12-30     Completed Date:  1991-12-30     Revised Date:  2009-11-18    
Medline Journal Info:
Nlm Unique ID:  7503323     Medline TA:  Br J Clin Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  599-604     Citation Subset:  IM    
Affiliation:
University Department of Medicine and Therapeutics, Stobhill General Hospital, Glasgow.
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MeSH Terms
Descriptor/Qualifier:
Adrenergic alpha-Antagonists / pharmacology*
Adult
Aminoquinolines / administration & dosage,  pharmacology*
Atenolol / pharmacology
Blood Pressure / drug effects*
Double-Blind Method
Heart Rate / drug effects*
Humans
Injections, Intravenous
Male
Phenylephrine / antagonists & inhibitors,  pharmacology
Tetrahydroisoquinolines*
Chemical
Reg. No./Substance:
0/Adrenergic alpha-Antagonists; 0/Aminoquinolines; 0/Tetrahydroisoquinolines; 118931-00-3/abanoquil; 29122-68-7/Atenolol; 59-42-7/Phenylephrine
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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