Skip to main content

Urapidil: The Role of 5-HT1A and α-Adrenergic Receptors in Blood Pressure Reduction

  • Chapter
  • First Online:
Serotonin

Part of the book series: Medical Science Symposia Series ((MSSS,volume 5))

  • 152 Accesses

Abstract

The CNS-mediated hypotensive response to urapidil is attributed to 5-HT1A receptor stimulation in anesthetized cats. This effect significantly participates in the blood pressure reduction following peripheral drug administration besides inhibition of vascular αl-adrenoceptors. In conscious dogs, the a1-antagonist effect prevents the appearance of a 5-HT syndrome, which is seen after ‘pure’ S-HT1A agonists, and contributes to the good tolerability of urapidil. It is concluded that the well-balanced properties of the hybrid molecule of urapidil make it an efficient and well-tolerable antihypertensive drug.

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 169.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 219.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 219.99
Price excludes VAT (USA)
  • Durable hardcover 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. Schoetensack, W., Bruckschen, E.G., and Zech, K. (1983) ‘Urapidil’, in A. Scriabine (ed.), New Drugs Annual: Cardiovascular Drugs, Raven Press, New York, pp. 19–48.

    Google Scholar 

  2. Jackisch, R., Kasakov, L., Feuerstein, T.J., and Hertting, G. (1987) ‘Effects of urapidil on neurotransmitter release in CNS tissuein vitro’Arch. int. Pharmacodyn. Ther. 285, 5–24.

    PubMed  CAS  Google Scholar 

  3. Sanders, K.H., Kilian, U., Kolassa, N., and Schoetensack, W. (1985) ‘Influence of urapidil on a-and 13-adrenoceptors in pithed rats’, J. Auton. Pharmac. 5, 307–316.

    Article  CAS  Google Scholar 

  4. Van Zwieten, P.A., de Jonge, A., Wilffert, B., Timmermans, P.B.M.W.M., Beckeringh, J.J., and Thoolen, M.J.M.C. (1985) ‘Cardiovascular effects and interaction with adrenoceptors of urapidil’, Arch. int. Pharmacodyn. Ther. 276, 180–201.

    PubMed  Google Scholar 

  5. Ramage, A.G. (1986) ‘A comparison of the effects of doxazosin and alfuzosin with those of urapidil on preganglionic sympathetic nerve activity in anesthetized cats’, Eur. J. Pharmacol. 129, 307–314.

    Article  CAS  Google Scholar 

  6. Fozard, J.R. and Mir, A.K. (1987) ‘Are 5-HT receptors involved in the antihypertensive effects of urapidil’, Br. J. Pharmacol. 90, 24P.

    Google Scholar 

  7. Van Zwieten, P.A. (1975) ‘Antihypertensive drugs with a central action’, Progr. Pharmacol. 1, 1–63.

    CAS  Google Scholar 

  8. Sanders, K.H., Beller, K.-D., Eltze, M., and Kolassa, N. (1989)‘Urapidil and some analogs with high affinities for serotonin-1A and a 1-adrenoceptor binding sites show potent hypotensive activity upon central administration’, Corr. Opinion Cardiol. 4 (Suppl. 4), S49–S55.

    Google Scholar 

  9. Sanders, K.H., Beller, K.-D., Bischler, P., and Kolassa, N. (1988) ‘Interaction of urapidil with brain serotonin-1A receptors increases the blood pressure reduction due to peripheral alpha-adrenoceptor inhibition’, J. Hypertension 6 (Suppl. 2), S65–S68.

    CAS  Google Scholar 

  10. Sanders, K.H., Beller, K.-D., and Kolassa, N. (1990) ‘Involvement of 5-HT1A receptors in blood pressure reduction by 8-OH-DPAT and urapidil in cats’, J. Cardiovasc. Pharmacol. 15 (Suppl. 7), S86–S93.

    Article  CAS  Google Scholar 

  11. Kolassa, N., Beller, K.-D., and Sanders, K.H. (1989) ‘Involvement of brain 5-HT1A receptors in the hypotensive response to urapidil’, Am. J. Cardiol. 64, 7D–10D.

    Article  CAS  Google Scholar 

  12. Beller, K.-D., Boer, R., Sanders, K.H., and Walter, B. (1990) ‘Is blockade of a 1-adrenoceptors favorable in hypotension induced by stimulation of serotonin-1A receptors in conscious dogs?’, Drugs 40, 38–41.

    Article  CAS  Google Scholar 

  13. Gillis, R.A., Kellar, K.J., Quest, J.A., Namath, I.J., Martino-Barrows, A., Hill, K., Gatti, P.J., and Dretchen, K. (1988) ‘Experimental studies on the neurocardiovascular effects of urapidil’, Drugs 35 (Suppl. 6), 20–33.

    Article  CAS  Google Scholar 

  14. Gross, G., Schüttler, K., Xin, X., and Hanft, G. (1990) ‘Urapidil analogues are potent ligands of the 5-HT,, receptor’, J. Cardiovasc. Pharmacol. 15 (Suppl. 7), S8–S16.

    Article  CAS  Google Scholar 

  15. Laporte, A.-M., Schechter, L.E., Bolanos, F.J., Verg, D., Hamon, M., and Gozlan, H. (1991) ‘(3H)5-Methyl-urapidil labels 5-HT1A receptors and aladrenoceptors in the rat CNS.In vitrobinding and autoradiographic studies’, Eur. J. Pharmacol. 198, 59–67.

    Article  CAS  Google Scholar 

  16. Valenta, B., Kotai, E., Weisz, E., and Singer, E.A. (1990) ‘Influence of urapidil and 8-OH-DPAT on brain 5-HT turnover and blood pressure in rats’, J. Cardiovasc. Pharmacol. 15 (Suppl. 7), S68–S74.

    Article  CAS  Google Scholar 

  17. Valenta, B. and Singer, E.A. (1990) ‘Hypotensive effects of 8-hydroxy-2-(din-propylamino)tetralin and 5-methylurapidil following stereotaxic microinjection into the ventral medulla of the rat’, Br. J. Pharmacol. 99, 713–716.

    Article  CAS  Google Scholar 

  18. Mandai, A.K., Kellar, K.J., and Gillis, R.A. (1991) ‘The role of serotonin-1A receptor activation and alpha-1 adrenoceptor blockade in the hypotensive effect of 5-methyl-urapidil’, J. Pharmacol. Exp. Ther. 257, 861–869.

    Google Scholar 

  19. Ramage, A.G. (1991) ‘The mechanism of the sympathoinhibitory action of urapidil: role of 5-HT1A receptors’, Br. J. Pharmacol. 102, 998–1002.

    Article  CAS  Google Scholar 

  20. Tricklebank, M.D., Forler, C., and Fozard, J.R. (1984) ‘The involvement of subtypes of the 5-HT1A receptor and of catecholaminergic systems in the behavioral response to 8-hydroxy-2-(di-n-propylamino)tetralin in the rat’, Eur. J. Pharmacol. 106, 271–282.

    Article  CAS  Google Scholar 

  21. Di Francesco, G.F., Petty, M.A., and Fozard, J.R. (1988) ‘Anti-hypertensiveeffectsof 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) in conscious dogs’, Eur. J. Pharmacol. 147, 287–290.

    Article  CAS  Google Scholar 

  22. Grohs, J.G., Fischer, G., and Raberger, G. (1990) ‘Cardiovascular effects of flesinoxan in anesthetized and conscious dogs’, Naunyn-Schmiedeberg’sArch. Pharmacol. 341, 472–475.

    CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1993 Springer Science+Business Media Dordrecht

About this chapter

Cite this chapter

Kolassa, N., Beller, K.D., Boer, R., Boss, H., Sanders, K.H. (1993). Urapidil: The Role of 5-HT1A and α-Adrenergic Receptors in Blood Pressure Reduction. In: Vanhoutte, P.M., Saxena, P.R., Paoletti, R., Brunello, N., Jackson, A.S. (eds) Serotonin. Medical Science Symposia Series, vol 5. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-1920-7_17

Download citation

  • DOI: https://doi.org/10.1007/978-94-011-1920-7_17

  • Published:

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-010-4849-1

  • Online ISBN: 978-94-011-1920-7

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics