Document Detail

5-HT2-receptor antagonists: alpha 1- vs. 5-HT2-receptor blocking properties in blood vessels.
MedLine Citation:
PMID:  2459510     Owner:  NLM     Status:  MEDLINE    
LY53857, spiperone, ketanserin, and setoperone were potent and competitive 5-HT2-receptor antagonists in the rat jugular vein with equivalent affinities at 5-HT2 receptors. In the rat jugular vein, ritanserin blocked 5-HT2-mediated contractile responses with a depression of the maximum response in concentrations greater than 3 X 10(-10) M. Ketanserin, spiperone, ritanserin, and setoperone were also alpha 1-adrenergic receptor antagonists, although affinity at alpha 1-adrenergic receptors was less for ritanserin and setoperone than for ketanserin or spiperone. Of the 5-HT2-receptor antagonists examined, LY53857 was the most selective with respect to alpha 1-adrenergic receptor affinity, showing 250,000-fold selectivity as an antagonist at 5-HT2 receptors. The possibility that the dual properties of 5-HT2- and alpha 1-receptor blockade confer greater antihypertensive efficacy than alpha 1-receptor blockade alone was also examined in vivo. However, acute administration of LY53857 at doses sufficient to abolish 5-HT2-receptor activation did not enhance blood pressure reduction produced by the alpha-adrenergic receptor antagonist phentolamine in normotensive or spontaneously hypertensive rats. These data argue against an important role for 5-HT2 receptors in blood pressure regulation even in combination with alpha-adrenergic receptor blockade.
M L Cohen; K W Schenck; K D Kurz
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of cardiovascular pharmacology     Volume:  11 Suppl 1     ISSN:  0160-2446     ISO Abbreviation:  J. Cardiovasc. Pharmacol.     Publication Date:  1988  
Date Detail:
Created Date:  1988-11-17     Completed Date:  1988-11-17     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  7902492     Medline TA:  J Cardiovasc Pharmacol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  S25-9     Citation Subset:  IM    
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.
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MeSH Terms
Adrenergic alpha-Antagonists / pharmacology*
Blood Pressure / drug effects
Ergolines / pharmacology
Ketanserin / pharmacology
Muscle Contraction / drug effects
Muscle, Smooth, Vascular / drug effects*,  physiology
Phentolamine / pharmacology
Piperidines / pharmacology
Pyrimidinones / pharmacology
Rats, Inbred SHR
Rats, Inbred Strains
Receptors, Adrenergic, alpha / drug effects*,  physiology
Receptors, Serotonin / drug effects*,  physiology
Serotonin Antagonists / pharmacology*
Spiperone / pharmacology
Reg. No./Substance:
0/Adrenergic alpha-Antagonists; 0/Ergolines; 0/Piperidines; 0/Pyrimidinones; 0/Receptors, Adrenergic, alpha; 0/Receptors, Serotonin; 0/Serotonin Antagonists; 50-60-2/Phentolamine; 60634-51-7/LY 53857; 74050-98-9/Ketanserin; 749-02-0/Spiperone; 86487-64-1/setoperone; 87051-43-2/Ritanserin

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

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