Skip to main content
NCBI home page
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1986 Mar;87(3):587–594. doi: 10.1111/j.1476-5381.1986.tb10201.x

Adrenoceptor blocking properties of atropine-like agents anisodamine and anisodine on brain and cardiovascular tissues of rats.

D R Varma, T L Yue
PMCID: PMC1916562  PMID: 2879586

Abstract

The cholinoceptor antagonists anisodamine and anisodine are widely used in the People's Republic of China for the management of acute circulatory shock but the mechanism of their beneficial effects is not fully known; we therefore investigated if these agents possessed adrenoceptor blocking properties. The antagonistic effect of anisodamine and anisodine against the specific binding of the alpha 1-adrenoceptor ligand [3H]-WB-4101 to cardiac and brain tissue membrane preparations and against the effects of phenylephrine on isolated aortic strips and left atria of rats were compared with classical muscarinic receptor and adrenoceptor blocking agents. Both anisodamine and anisodine possessed alpha 1-adrenoceptor blocking properties; the order of potency of various agents in displacing the binding of [3H]-WB-4101 to receptors and in antagonizing the effects of phenylephrine on aortic strips and left atria was: prazosin greater than atropine greater than anisodamine greater than scopolamine greater than anisodine. It is concluded that both anisodamine and to a lesser extent anisodine possess alpha 1-adrenoceptor blocking properties; this antagonistic activity of anisodamine may contribute to its salutary effects on the microcirculation. However, it is unlikely that anisodine produces a significant adrenoceptor blockade in the clinically used dose-range.

Full text

PDF
587

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. ARUNLAKSHANA O., SCHILD H. O. Some quantitative uses of drug antagonists. Br J Pharmacol Chemother. 1959 Mar;14(1):48–58. doi: 10.1111/j.1476-5381.1959.tb00928.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Abraham S., Cantor E. H., Spector S. Atropine lowers blood pressure in normotensive rats through blockade of alpha-adrenergic receptors. Life Sci. 1981 Jan 19;28(3):315–322. doi: 10.1016/0024-3205(81)90739-6. [DOI] [PubMed] [Google Scholar]
  3. Benfey B. G., Varma D. R., Yue T. L. Myocardial inotropic responses and adrenoceptors in protein-deficient rats. Br J Pharmacol. 1983 Nov;80(3):527–531. doi: 10.1111/j.1476-5381.1983.tb10725.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Benfey B. G., Yong M. S., Belleau B., Melchiorre C. Inhibition of the cardiac inotropic effect of phenylephrine by a tetramine disulfide with irreversible alpha-adrenoceptor blocking activity. Can J Physiol Pharmacol. 1979 May;57(5):510–516. doi: 10.1139/y79-077. [DOI] [PubMed] [Google Scholar]
  5. Besse J. C., Furchgott R. F. Dissociation constants and relative efficacies of agonists acting on alpha adrenergic receptors in rabbit aorta. J Pharmacol Exp Ther. 1976 Apr;197(1):66–78. [PubMed] [Google Scholar]
  6. Cantor E. H., Abraham S., Marcum E. A., Spector S. Structure-activity requirements for hypotension and alpha-adrenergic receptor blockade by analogues of atropine. Eur J Pharmacol. 1983 May 20;90(1):75–83. doi: 10.1016/0014-2999(83)90215-7. [DOI] [PubMed] [Google Scholar]
  7. Cheng Y., Prusoff W. H. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol. 1973 Dec 1;22(23):3099–3108. doi: 10.1016/0006-2952(73)90196-2. [DOI] [PubMed] [Google Scholar]
  8. Digges K. G., Summers R. J. Characterization of postsynaptic alpha-adrenoceptors in rat aortic strips and portal veins. Br J Pharmacol. 1983 Jul;79(3):655–665. doi: 10.1111/j.1476-5381.1983.tb10002.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. FLECKENSTEIN A. A quantitative study of antagonists of adrenaline on the vessels of the rabbit's ear. Br J Pharmacol Chemother. 1952 Dec;7(4):553–562. doi: 10.1111/j.1476-5381.1952.tb00721.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. FURCHGOTT R. F. The pharmacology of vascular smooth muscle. Pharmacol Rev. 1955 Jun;7(2):183–265. [PubMed] [Google Scholar]
  11. Kapur H., Rouot B., Snyder S. H. Binding to alpha-adrenergic receptors: differential pharmacological potencies and binding affinities of benzodioxanes. Eur J Pharmacol. 1979 Aug 15;57(4):317–328. doi: 10.1016/0014-2999(79)90494-1. [DOI] [PubMed] [Google Scholar]
  12. 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]
  13. Ruffolo R. R., Jr, Waddell J. E., Yaden E. L. Heterogeneity of postsynaptic Alpha adrenergic receptors in mammalian aortas. J Pharmacol Exp Ther. 1982 May;221(2):309–314. [PubMed] [Google Scholar]
  14. U'Prichard D. C., Bechtel W. D., Rouot B. M., Snyder S. H. Multiple apparent alpha-noradrenergic receptor binding sites in rat brain: effect of 6-hydroxydopamine. Mol Pharmacol. 1979 Jul;16(1):47–60. [PubMed] [Google Scholar]
  15. Xiu R. J., Hammerschmidt D. E., Coppo P. A., Jacob H. S. Anisodamine inhibits thromboxane synthesis, granulocyte aggregation, and platelet aggregation. A possible mechanism for its efficacy in bacteremic shock. JAMA. 1982 Mar 12;247(10):1458–1460. doi: 10.1001/jama.247.10.1458. [DOI] [PubMed] [Google Scholar]
  16. Yue T. L., Varma D. R., Powell W. S. Effects of protein deficiency on the metabolism of arachidonic acid by rat pleural polymorphonuclear leukocytes. Biochim Biophys Acta. 1983 May 16;751(3):332–339. doi: 10.1016/0005-2760(83)90291-6. [DOI] [PubMed] [Google Scholar]

Articles from British Journal of Pharmacology are provided here courtesy of The British Pharmacological Society

RESOURCES