Document Detail

5-HT, alpha-adrenoceptors, and blood pressure. Effects of ketanserin in essential hypertension and autonomic insufficiency.
MedLine Citation:
PMID:  6319278     Owner:  NLM     Status:  MEDLINE    
The serotonin (5-hydroxytryptamine, 5-HT) antagonist, ketanserin, has a high affinity for 5-HT2-receptors but it also binds to alpha 1-adrenoceptors. The compound (10 mg i.v.) lowered mean arterial pressure by 22% +/- 2% (mean +/- SEM, p less than 0.001) in 30 patients with essential hypertension. Measurements of heart rate, cardiac output, cardiac filling pressures, forearm blood flow, renal blood flow, and glomerular filtration rate revealed a hemodynamic pattern compatible with vasodilation of both resistance and capacitance vessels. This was accompanied by moderate reflex cardiostimulation. Ketanserin did not alter the pressor effect of bolus injections of (-)-phenylephrine hydrochloride (25, 50, 100, and 200 micrograms i.v.). Ketanserin also had a distinct hypotensive effect in four normotensive patients with autonomic insufficiency due to an efferent sympathetic lesion, who were unresponsive to phentolamine (20 mg i.v.). Thus, ketanserin in the dose we have used appears to lower blood pressure independently of alpha 1-adrenoceptor blockade. On the other hand, in patients with essential hypertension the antihypertensive effect of ketanserin was blunted by pretreatment with prazosin (12 mg/day). Therefore, a certain degree of alpha 1-adrenergic tone seems to be required for the compound to exert its full antihypertensive action. The findings are indirect evidence for a role of 5-HT in the maintenance of increased vascular resistance in essential hypertension. This may be related, at least in part, to the alleged amplifying effect of 5-HT on alpha 1-adrenoceptor-mediated vasoconstriction.
G J Wenting; A J Woittiez; A J Man in't Veld; M A Schalekamp
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Hypertension     Volume:  6     ISSN:  0194-911X     ISO Abbreviation:  Hypertension     Publication Date:    1984 Jan-Feb
Date Detail:
Created Date:  1984-03-06     Completed Date:  1984-03-06     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  7906255     Medline TA:  Hypertension     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  100-9     Citation Subset:  IM    
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MeSH Terms
Aldosterone / blood
Antihypertensive Agents / administration & dosage
Autonomic Nervous System Diseases / drug therapy,  physiopathology
Blood Pressure / drug effects*
Furosemide / administration & dosage
Hemodynamics / drug effects
Hypertension / drug therapy,  physiopathology*
Middle Aged
Norepinephrine / blood
Phenylephrine / administration & dosage
Piperidines / administration & dosage*
Prazosin / administration & dosage
Receptors, Adrenergic, alpha / drug effects*
Renal Circulation / drug effects
Renin / blood
Serotonin Antagonists / administration & dosage*
Reg. No./Substance:
0/Antihypertensive Agents; 0/Piperidines; 0/Receptors, Adrenergic, alpha; 0/Serotonin Antagonists; 19216-56-9/Prazosin; 51-41-2/Norepinephrine; 52-39-1/Aldosterone; 54-31-9/Furosemide; 59-42-7/Phenylephrine; 74050-98-9/Ketanserin; EC

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