Abstract
5-Hydroxytryptamine (5-HT; serotonin) has fascinated and confused scientists since its discovery some 40 years ago. The monoamine, released from aggregating blood platelets, has been implicated in the peripheral control of vascular tone and in the pathogenesis of hypertension and peripheral vascular disorders. Its exact role, however, has remained elusive [1]. Exogenous 5-HT causes either contraction or relaxation of vascular smooth musle depending on blood vessel type, monoamine concentration, presence of intact endothelium and experimental conditions [2]. Most isolated large blood vessels, arteries as well as veins, are constricted by 5-HT whereas arterioles may be dilated. In addition, 5-HT markedly potentiates the constrictor effects of other agonists including noradrenaline. Local factors such as hypoxia and low temperature also contribute to the vasoconstrictor effect of 5-HT. This constrictor effect is mediated by 5-HT2 receptors on vascular smooth musle [3–5].
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References
Page IH (1968): Serotonin. Chicago: Year Book Medical Publishers.
Vanhoutte PM, Luescher TF (1986): Serotonin and the blood vessel wall. J Hypertens (suppl. 1)4: S29–S35.
Leysen JE, Awouters F, Kennis L, Laduron PM, Vandenberk J, Janssen PAJ (1981): Receptor binding profile of R 41468, a novel antagonist at 5-HT2 receptors. Life Sci 28: 1015–1022.
Cohen ML, Fuller RW, Wiley KS (1981): Evidence for 5-HT2 receptors mediating contraction in vascular smooth muscle./ Pharmacol Exp Ther 218: 421–425.
Janssen PAJ (1983): 5-HT2 receptor blockade to study serotonin-induced pathology. Trends Pharmacol Sci 4:198–206.
Van Nueten JM, Janssen PAJ, Van Beek J, Xhonneux R, Verbeuren TJ, Vanhoutte PM (1981): Vascular effects of ketanserin (R 41468), a novel antagonist of 5-HT2 serotonergic receptors. J Pharmacol Exp Ther 218: 217–230.
Wenting GJ, Manin’t Veld AJ, Woittiez AJ, Boomsma F, Schalekamp MADH (1982): Treatment of hypertension with ketanserin, a new selective 5-HT2 receptor antagonist. Br Med J 284: 537–539.
Wenting GJ, Woittiez AJ, Manin’t Veld AJ, Schalekamp MADH: 5-HT, alpha- adrenoceptors and blood pressure. Effects of ketanserin in essential hypertension and autonomic insufficiency. Hypertension 6:100–109.
Woittiez AJ, Wenting GJ, Van den Meiracker AJ, Ritsema van Eck HJ, Manin’t Veld AJ, Zantvoort FA, Schalekamp MADH (1986): Chronic effect of ketanserin in mild to moderate essential hypertension. Hypertension 8: 167–173.
Vanhoutte PM, Amery AA, Birkenhager WH, Breckenridge A et al. (1988): Serotonergic mechanisms in hypertension. Focus on the effects of ketanserin. Hypertension 11: 111–133.
Reimann IW, Frolich JC (1983): Mechanism of antihypertensive action of ketanserin in man. Br Med J 287: 381–383.
Zabludowski JR, Zoccali C, Isles CG, Murray GD, Robertson JIS, Inglis GC, Fraser R, Ball SG (1984): Effect of the 5-hydroxytryptamine type 2 receptor antagonist, ketanserin, on blood pressure, the renin-angiotensin system and sympatho-adrenal function in patients with essential hypertension. Br J Clin Pharmacol 17: 309–316.
Fagard R, Fioli R, Lijnen P, Staessen J, Moerman E, De Schaepdrijver A, Amery A (1984): Haemodynamic and humoral responses to chronic ketanserin treatment in essential hypertension. Br Heart 7 51: 149–156.
Saxena PR (1989): 5-Hydroxytryptamine antagonists as antihypertensive drugs. This book.
Hosie J, Stott DJ, Robertson JIS, Ball SG (1987): Does acute serotonergic type-2 antagonism reduce blood pressure? Comparative effects of single doses of ritanserin and ketanserin in essential hypertension. J Cardiovasc Pharmacol (suppl. 3 ) 10: S86–S88.
Ramage AG (1985): The effects of ketanserin, methysergide and LY 53857 on sympathetic nerve activity. Eur J Pharmacol 113: 295–303.
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Schalekamp, M.A.D.H., Wenting, GJ. (1990). Ketanserin in hypertension and vasospastic disease: mechanism of action. In: Saxena, P.R., Wallis, D.I., Wouters, W., Bevan, P. (eds) Cardiovascular Pharmacology of 5-Hydroxytryptamine. Developments in CardioCardiovascular Pharmacology of 5-Hydroxytryptamine, vol 106. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-0479-8_25
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DOI: https://doi.org/10.1007/978-94-009-0479-8_25
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