Document Detail


Extremely long-acting antihypertensive effects of KF-4317, a alpha- and beta 1-adrenoceptor blocker.
MedLine Citation:
PMID:  2865934     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The hypotensive effects of 4-(2-hydroxy-3-[(1-methyl-3-phenylpropyl)amino]propoxy)benzeneacetamide hydrochloride (KF-4317, a novel alpha- and beta 1-adrenoceptor blocker) were evaluated in spontaneously hypertensive rats and renal hypertensive dogs as well as in normotensive dogs, cats and rabbits, using various routes of administration. Single oral, intraduodenal and intravenous administrations of KF-4317 induced definite hypotensive effects. When intraduodenally given to anesthetized rabbits, KF-4317 elicited a much more prolonged effect on the blood pressure than labetalol, while neither atenolol nor propranolol showed hypotensive effects. Pretreatment with phentolamine abolished its depressor effect, but not its bradycardic effect, indicating that the former effect is mediated by alpha-blockade. When orally given to the conscious hypertensive rats and dogs, it exerted an extremely long-acting effect with a property of very gradual onset of action. Furthermore, KF-4317 neither showed any sign indicative of orthostatic hypotension in an experimental model nor exhibited any intrinsic sympathomimetic activity, though a very weak local anesthetic effect was observed. From these results, it could be concluded that KF-4317 possesses some pharmacological properties similar to labetalol, but in contrast to labetalol it is beta 1-selective, and it may be useful in the treatment of patients with hypertension.
Authors:
K Kubo; J Ikeda; J Nakamura; N Nakamizo
Related Documents :
2566504 - Role of ancillary properties of beta-adrenoceptor antagonists in protecting the heart f...
16618484 - Importance of extracardiac alpha1-adrenoceptor stimulation in assisting dofetilide to i...
2896274 - The conundrum of the effect of beta-blockade on myocardial oxygen consumption.
2419684 - Alpha 1-and alpha 2-adrenoceptor mediated vasoconstriction in the forearm of normotensi...
20550244 - Determination of postexcitation thresholds for single ultrasound contrast agent microbu...
704264 - Information variables in voluntary control and classical conditioning of heart rate: fi...
Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Archives internationales de pharmacodynamie et de thérapie     Volume:  277     ISSN:  0003-9780     ISO Abbreviation:  Arch Int Pharmacodyn Ther     Publication Date:  1985 Sep 
Date Detail:
Created Date:  1985-12-16     Completed Date:  1985-12-16     Revised Date:  2012-01-12    
Medline Journal Info:
Nlm Unique ID:  0405353     Medline TA:  Arch Int Pharmacodyn Ther     Country:  BELGIUM    
Other Details:
Languages:  eng     Pagination:  140-60     Citation Subset:  IM    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Adrenergic alpha-Antagonists / administration & dosage,  pharmacology*
Adrenergic beta-Antagonists / administration & dosage,  pharmacology*
Animals
Antihypertensive Agents / administration & dosage,  pharmacology*
Benzeneacetamides*
Blood Pressure / drug effects*
Cats
Dogs
Female
Guinea Pigs
Heart Rate / drug effects
Injections, Intravenous
Male
Myocardial Contraction / drug effects
Posture
Propanolamines / administration & dosage,  pharmacology*
Rats
Rats, Inbred Strains
Species Specificity
Time Factors
Chemical
Reg. No./Substance:
0/Adrenergic alpha-Antagonists; 0/Adrenergic beta-Antagonists; 0/Antihypertensive Agents; 0/Benzeneacetamides; 0/Propanolamines; 76805-48-6/KF 4317

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


Previous Document:  Mechanism of the hypotensive effect of a novel phenylpiperazine derivative, SGB-1534: antagonism at ...
Next Document:  Cholinergic involvement in the modulation of oxotremorine-tremor in mice by propranolol.