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. 1991 Nov;104(3):651–656. doi: 10.1111/j.1476-5381.1991.tb12484.x

Dicentrine, a natural vascular alpha 1-adrenoceptor antagonist, isolated from Lindera megaphylla.

C M Teng 1, S M Yu 1, F N Ko 1, C C Chen 1, Y L Huang 1, T F Huang 1
PMCID: PMC1908254  PMID: 1686739

Abstract

1. The pharmacological activity of dicentrine, isolated from Lindera megaphylla, was determined in rat isolated thoracic aorta, guinea-pig isolated trachea and human platelet-rich plasma. 2. Dicentrine was found to be a potent alpha 1-adrenoceptor blocking agent in rat thoracic aorta as revealed by its competitive antagonism of noradrenaline- (pA2 = 8.19 +/- 0.09) or phenylephrine (pA2 = 9.01 +/- 0.10)-induced vasoconstriction. These effects still persisted in denuded aorta. It was less potent than prazosin (pA2 = 10.60 +/- 0.10), but was more potent than phentolamine (pA2 = 7.53 +/- 0.10) or yohimbine (pA2 = 6.20 +/- 0.05). 3. Inositol monophosphate formation induced by noradrenaline (3 microM) in rat thoracic aorta was suppressed by dicentrine (3-10 microM) and prazosin (3 microM). 4. A high concentration of dicentrine (30 microM) did not affect the aortic contraction induced by the thromboxane receptor agonist U-46619 (1 microM), angiotensin II (1 microM), high potassium (60 mM) or carbachol (3 microM). 5. Contraction of guinea-pig trachea caused by histamine or carbachol was slightly inhibited by dicentrine (30 microM), while beta-adrenoceptor relaxation to isoprenaline in trachea was not affected. 6. Aggregation in human platelet-rich plasma induced by adrenaline (10 microM) was blocked by yohimbine (5 microM). A high concentration of dicentrine (greater than 30 microM) caused slight inhibition of aggregation, the release reaction and thromboxane formation. Complete blockade was obtained with 150 microM dicentrine. 7. It is concluded that dicentrine is a potent, selective alpha 1-adrenoceptor antagonist in vascular smooth muscle.

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Selected References

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  1. Alosachie I., Godfraind T. Role of cyclic GMP in the modulation by endothelium of the adrenolytic action of prazosin in the rat isolated aorta. Br J Pharmacol. 1986 Nov;89(3):525–532. doi: 10.1111/j.1476-5381.1986.tb11152.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Alosachie I., Godfraind T. The modulatory role of vascular endothelium in the interaction of agonists and antagonists with alpha-adrenoceptors in the rat aorta. Br J Pharmacol. 1988 Oct;95(2):619–629. doi: 10.1111/j.1476-5381.1988.tb11684.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Berridge M. J., Downes C. P., Hanley M. R. Lithium amplifies agonist-dependent phosphatidylinositol responses in brain and salivary glands. Biochem J. 1982 Sep 15;206(3):587–595. doi: 10.1042/bj2060587. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Eglème C., Godfraind T., Miller R. C. Enhanced responsiveness of rat isolated aorta to clonidine after removal of the endothelial cells. Br J Pharmacol. 1984 Jan;81(1):16–18. doi: 10.1111/j.1476-5381.1984.tb10736.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Hirata M., Kohse K. P., Chang C. H., Ikebe T., Murad F. Mechanism of cyclic GMP inhibition of inositol phosphate formation in rat aorta segments and cultured bovine aortic smooth muscle cells. J Biol Chem. 1990 Jan 25;265(3):1268–1273. [PubMed] [Google Scholar]
  6. Hsu C. Y., Knapp D. R., Halushka P. V. The effects of alpha adrenergic agents on human platelet aggregation. J Pharmacol Exp Ther. 1979 Mar;208(3):366–370. [PubMed] [Google Scholar]
  7. Jaffe E. A. Physiologic functions of normal endothelial cells. Ann N Y Acad Sci. 1985;454:279–291. doi: 10.1111/j.1749-6632.1985.tb11868.x. [DOI] [PubMed] [Google Scholar]
  8. Ko F. N., Lin C. N., Liou S. S., Huang T. F., Teng C. M. Vasorelaxation of rat thoracic aorta caused by norathyriol isolated from Gentianaceae. Eur J Pharmacol. 1991 Jan 3;192(1):133–139. doi: 10.1016/0014-2999(91)90079-6. [DOI] [PubMed] [Google Scholar]
  9. LOWRY O. H., ROSEBROUGH N. J., FARR A. L., RANDALL R. J. Protein measurement with the Folin phenol reagent. J Biol Chem. 1951 Nov;193(1):265–275. [PubMed] [Google Scholar]
  10. MacKay D. How should values of pA2 and affinity constants for pharmacological competitive antagonists be estimated? J Pharm Pharmacol. 1978 May;30(5):312–313. doi: 10.1111/j.2042-7158.1978.tb13237.x. [DOI] [PubMed] [Google Scholar]
  11. Motulsky H. J., Shattil S. J., Insel P. A. Characterization of alpha 2-adrenergic receptors on human platelets using [3H]yohimbine. Biochem Biophys Res Commun. 1980 Dec 31;97(4):1562–1570. doi: 10.1016/s0006-291x(80)80044-1. [DOI] [PubMed] [Google Scholar]
  12. Neylon C. B., Summers R. J. Stimulation of alpha 1-adrenoceptors in rat kidney mediates increased inositol phospholipid hydrolysis. Br J Pharmacol. 1987 Jun;91(2):367–376. doi: 10.1111/j.1476-5381.1987.tb10291.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Palmer R. M., Ferrige A. G., Moncada S. Nitric oxide release accounts for the biological activity of endothelium-derived relaxing factor. Nature. 1987 Jun 11;327(6122):524–526. doi: 10.1038/327524a0. [DOI] [PubMed] [Google Scholar]
  14. Teng C. M., Yu S. M., Chen C. C., Huang Y. L., Huang T. F. EDRF-release and Ca+(+)-channel blockade by magnolol, an antiplatelet agent isolated from Chinese herb Magnolia officinalis, in rat thoracic aorta. Life Sci. 1990;47(13):1153–1161. doi: 10.1016/0024-3205(90)90176-r. [DOI] [PubMed] [Google Scholar]
  15. Vanhoutte P. M., Rubanyi G. M., Miller V. M., Houston D. S. Modulation of vascular smooth muscle contraction by the endothelium. Annu Rev Physiol. 1986;48:307–320. doi: 10.1146/annurev.ph.48.030186.001515. [DOI] [PubMed] [Google Scholar]
  16. Yu S. M., Chen C. C., Huang Y. L., Tsai C. W., Lin C. H., Huang T. F., Teng C. M. Vasorelaxing effect in rat thoracic aorta caused by denudatin B, isolated from the Chinese herb, magnolia fargesii. Eur J Pharmacol. 1990 Oct 2;187(1):39–47. doi: 10.1016/0014-2999(90)90338-7. [DOI] [PubMed] [Google Scholar]

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