Serotonergic receptors and drugs in hypertension

Pharmacology & Toxicology
P A van ZwietenP van Brummelen

Abstract

The possible role of 5-hydroxytryptamine (5HT) and 5HT-receptors in hypertension, already suggested by Page in 1954, has been subject to a renaissance of interest owing to the development of antihypertensive drugs which interact with 5HT-receptors. These drugs, like ketanserin, urapidil and flesinoxan are used as tools to study the role of 5HT and its receptors in hypertension. Some arguments would plead in favour of a certain role of 5HT and 5HT-receptors in the pathogenesis and maintenance of hypertension: hyperresponsiveness of blood vessels from hypertensive patients and animals to 5HT-induced constriction; the antihypertensive/vasodilator activity of the 5HT2-receptor antagonist ketanserin; enhanced sensitivity of platelets from hypertensives to 5HT. However, there are also several arguments which do not support a causal role of 5HT in hypertensive disease: 5HT is not a generally accepted pressor agent, whereas its concentration in the circulating blood is subthreshold; the 5HT2-receptor antagonist ketanserin is the only agent of this type which lowers blood pressure, other 5HT2-receptor blockers (ritanserin; LY 53587) being inactive. The various data and arguments available do not unequivocally support a relevant role of ...Continue Reading

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Related Concepts

Urapidil, 5-(14)C-labeled
Adrenergic alpha-Antagonists
Metazoa
Antihypertensive Agents
Diastolic Blood Pressure
Hypertensive Disease
R-41,468
Piperazines
Receptors, Tryptamine
Vasoactive Antagonists

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