Document Detail


Cardiovascular actions of a new selective postjunctional alpha-adrenoceptor antagonist, SK&F 104856, in normotensive and hypertensive dogs.
MedLine Citation:
PMID:  1354539     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
1. SK&F 104856 (2-vinyl-7-chloro-3,4,5,6-tetrahydro-4- methylthieno[4,3,2ef][3]benzazepine) is a novel postjunctional alpha 1- and alpha 2-adrenoceptor antagonist. 2. SK&F 104856 as well as prazosin and SK&F 86466 reduced blood pressure in the anaesthetized normotensive dog. 3. SK&F 86466 and rauwolscine but not SK&F 104856 or prazosin, produced a marked increase in myocardial contractility which corresponds with their ability to block prejunctional alpha 2-adrenoceptors. 4. Intravenous or oral administration of SK&F 104856 resulted in dose-dependent antihypertensive responses in 1-kidney, 1-clip (1-K, 1-C) Goldblatt hypertensive dogs with baseline blood pressure of approximately 140 mmHg. At 0.1 and 1 mg kg-1, i.v., mean arterial blood pressure fell by 11 +/- 5 and 23 +/- 5 mmHg, respectively. At 3 and 10 mg kg-1, p.o., blood pressure fell by 9 +/- 3 and 22 +/- 5 mmHg, respectively. At 10 mg kg-1, p.o., the antihypertensive effect of SK&F 104856 was still evident at 4 h. 5. The data indicate that SK&F 104856 shows selectivity in vivo for postjunctional versus prejunctional alpha-adrenoceptors and is a potent and long-acting antihypertensive agent in 1-K, 1-C Goldblatt hypertensive dogs.
Authors:
J P Hieble; A J Nichols; T A Fredrickson; P D DePalma; R R Ruffolo; D P Brooks
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  British journal of pharmacology     Volume:  105     ISSN:  0007-1188     ISO Abbreviation:  Br. J. Pharmacol.     Publication Date:  1992 Apr 
Date Detail:
Created Date:  1992-09-22     Completed Date:  1992-09-22     Revised Date:  2010-09-07    
Medline Journal Info:
Nlm Unique ID:  7502536     Medline TA:  Br J Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  992-6     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA.
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MeSH Terms
Descriptor/Qualifier:
Adrenergic alpha-Antagonists / pharmacology
Animals
Benzazepines / administration & dosage,  pharmacology*
Blood Pressure / drug effects
Cardiovascular Physiological Phenomena
Cardiovascular System / drug effects*
Dogs
Female
Heart Rate / drug effects
Hypertension, Renovascular / drug therapy*,  physiopathology
Male
Myocardial Contraction / drug effects
Prazosin / pharmacology
Yohimbine / pharmacology
Chemical
Reg. No./Substance:
0/Adrenergic alpha-Antagonists; 0/Benzazepines; 138194-10-2/SK&F 104856; 146-48-5/Yohimbine; 19216-56-9/Prazosin; 73943-10-9/benalfocin
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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