Skip to main content

Ketanserin in hypertension and vasospastic disease: mechanism of action

  • Chapter
Cardiovascular Pharmacology of 5-Hydroxytryptamine

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].

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 39.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 54.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Page IH (1968): Serotonin. Chicago: Year Book Medical Publishers.

    Google Scholar 

  2. Vanhoutte PM, Luescher TF (1986): Serotonin and the blood vessel wall. J Hypertens (suppl. 1)4: S29–S35.

    Google Scholar 

  3. 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.

    Article  CAS  PubMed  Google Scholar 

  4. Cohen ML, Fuller RW, Wiley KS (1981): Evidence for 5-HT2 receptors mediating contraction in vascular smooth muscle./ Pharmacol Exp Ther 218: 421–425.

    CAS  Google Scholar 

  5. Janssen PAJ (1983): 5-HT2 receptor blockade to study serotonin-induced pathology. Trends Pharmacol Sci 4:198–206.

    Google Scholar 

  6. 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.

    PubMed  Google Scholar 

  7. 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.

    Article  CAS  Google Scholar 

  8. 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.

    Google Scholar 

  9. 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.

    Article  CAS  PubMed  Google Scholar 

  10. 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.

    Article  CAS  PubMed  Google Scholar 

  11. Reimann IW, Frolich JC (1983): Mechanism of antihypertensive action of ketanserin in man. Br Med J 287: 381–383.

    Article  CAS  Google Scholar 

  12. 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.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  13. 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.

    Article  Google Scholar 

  14. Saxena PR (1989): 5-Hydroxytryptamine antagonists as antihypertensive drugs. This book.

    Google Scholar 

  15. 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.

    Article  Google Scholar 

  16. Ramage AG (1985): The effects of ketanserin, methysergide and LY 53857 on sympathetic nerve activity. Eur J Pharmacol 113: 295–303.

    Article  CAS  PubMed  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1990 Springer Science+Business Media Dordrecht

About this chapter

Cite this chapter

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

Download citation

  • DOI: https://doi.org/10.1007/978-94-009-0479-8_25

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-010-6701-0

  • Online ISBN: 978-94-009-0479-8

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics