Archives of Pharmacal Research

, Volume 21, Issue 4, pp 370–373 | Cite as

Studies on the effects of piperidine derivatives on blood pressure and smooth muscles contractions

  • M. Saeed
  • Z. S. Saify
  • A. H. Gilani
  • Z. Iqbal
Research Articles


Ten substituted phenacyl derivatives of 4-hydroxypiperidine were synthesized and studied for their effects on the mean arterial blood pressure (MABP) in normotensive anaesthetized rats and smooth muscles contractions of isolated rabbit jejunum. Two derivatives caused fall in blood pressure at the dose of 10≈20 mg/kg and one rise in blood pressure at the dose of 20 mg/kg. Two compounds exhibited biphasic response (hypotensive followed by hypertensive) and one gave triphasic response at 10 mg/kg dose. Rest of four derivatives were found devoid of any effect on mean arterial blood pressure up to the dose of 30 mg/kg. All the derivatives except two caused relaxant effect on the spontaneous contraction of rabbit jejunum at the dose range of 0.1≈2 mg/kg.

Key words

Piperidine Antihypertensive Smooth muscle contraction 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References Cited

  1. Archibald, J. L., Baum, T. and Childress, S. J., 1,4-Bis (2-indol-3-ylethyl)piperidines.J. Med. Chem., 13, 138–40 (1970).PubMedCrossRefGoogle Scholar
  2. Bolton, T. B., Mechanism of action of transmitters and other substances on smooth muscles.Physiol. Rev., 59, 606–718 (1979).PubMedGoogle Scholar
  3. Brading, A. F.,TIPS., How do drugs initiate contraction in smooth muscles? 2, 259–61 (1981).Google Scholar
  4. Clark, R. D., Caroon, J. M., Kluge, A. F. and Okada, M. D., Synthesis and antihypertensive activity of '4-substituted spiro(4H-3,1-benzoxazine-4, '4-piperidine)-2(1H)-ones.J. Med. Chem., 26, 657–61 (1983).PubMedCrossRefGoogle Scholar
  5. Gilani, A. H., Janbaz, K. H., Lateef, A. and Zaman, M., Calcium channel blocking activity ofArtemisia scoparia extract.Phytother Res., 8, 161–65 (1994).CrossRefGoogle Scholar
  6. Maillard, J., Delaunary, P., Langlois, M. and Vo Van, T., Spiro-heterocyclic cycloalkane compounds-IV. Synthesis of '4-piperidine-5-spiro-2-oxazolidinones.Bull. Soc. Chim. Fr., 4, 1394–98 (1970).Google Scholar
  7. Mailland, J., Langlois, M., Delaunary, P., Vo Van, T., Chenu, J., Morin, R., Benharkate, M., Manuel, C. and Motosso, F., Cycloalkane spiroheterocyclic compounds.J. Med Chem., 15, 1123–28 (1972).CrossRefGoogle Scholar
  8. Mauleon, D., Pujol, M. D. and Rosell, G., Synthesis and β-adrenergic antagonism of 2-(aryloxy)-1-(2-piperidyl)ethanols.J. Med. Chem., 31, 2122–26 (1988).PubMedCrossRefGoogle Scholar
  9. Mcleod, L. C. (1970).Pharmacological Experiments on Intact Preparations (E & S Livingstone, Edinburg) p. 63.Google Scholar
  10. Saeed, M., Ahmad, M., Saify, Z. S., Zia, A., Ahmad, V. U. and Iqbal, Z., Synthesis and analgesic activity of 4-piperidinol derivatives.Pak. J. Pharm. Pb. Univ. Lahore 9, 37–42 (1996).Google Scholar
  11. Saeed, M., Saify, Iqbal, Z. and Islam, N. Synthesis of 4-hydroxipiperidine derivatives and their screening for analgesic activity.Arch. Pharm. Res., 20, 338–341 (1997).PubMedCrossRefGoogle Scholar
  12. Saify, Z. S., Saeed, M., Khan, A. Moazzam, H., Ahmad, V. U., Zia, A. and Haleem, D. J. Synthesis of some piperidine derivatives of potential analgesic activity. Proceed.19th IUPAC Symp. on Chem. Nat. Products. Kar., Pak., 75–83 (1994a).Google Scholar
  13. Saify, Z. S., Saeed, M., Moazzam, H., Yasmeen, A., Zafar, A. and Haleem, D. J., Studies on the effect of 4-hydroxy-4-phenylpiperidine derivative (4-HPPD) on mice brain dopamine metabolism.Proceed. ISBBP, Univ. Kar., Pak., 1, 36–39 (1994b).Google Scholar
  14. Takai, H., Obase, H., Nakamizo, N., Teranishi, M., Kubo, K., Shuto, K. and Hashimoto, T., Synthesis and pharmacological evaluation of piperidine derivatives with various heterocyclic rings at the 4-position.Chem. Pharm. Bull., 33, 1104–1115 (1985a).PubMedGoogle Scholar
  15. Takai, H., Obase, H., Teranishi, M., Karasawa, A., Kubo, K., Shuto, K., Kasuya, Y., Hashikami, M., Karashima, N. and Shigenobu, K., Spiropiperidines-1. Synthesis of '1-substituted spiropiperidine derivatives and evaluation of their antihypertensive activity.Chem. Pharm. Bull., 33, 1129–39 (1985b).PubMedGoogle Scholar
  16. Weiner, N. (1985). In:Goodman and Gilman's Pharmacological Basis of Therapeutics, Gilman, A. G., Goodman, L. S., Rall, T. W., and Murad, F. ed. (MacMillan, New York), p. 145.Google Scholar

Copyright information

© The Pharmaceutical Society of Korea 1998

Authors and Affiliations

  • M. Saeed
    • 1
  • Z. S. Saify
    • 2
  • A. H. Gilani
    • 3
  • Z. Iqbal
    • 1
  1. 1.Department of PharmacyUniversity of PeshawarPeshawarPakistan
  2. 2.Department of Pharmaceutical Chemistry, Faculty of PharmacyUniversity of KarachiKarachiPakistan
  3. 3.Department of PharmacologyAga Khan Medical UniversityKarachiPakistan

Personalised recommendations