Skip to main content
NCBI home page
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1981 Feb;72(2):319–334. doi: 10.1111/j.1476-5381.1981.tb09131.x

Actions of various muscarinic agonists on membrane potential, potassium efflux, and contraction of longitudinal muscle of guinea-pig intestine.

T B Bolton, J P Clark
PMCID: PMC2071508  PMID: 7214100

Abstract

1 Depolarizations were recorded intracellularly in smooth muscle from the taenia of the guinea-pig caecum in response to the iontophoretic application of acetylcholine, carbachol, oxotremorine-M, methylfurmethide, hexyl trimethylammonium and tetramethylammonium (TMA). 2 No differences between the iontophoretic responses to agonists stable to cholinesterase were detected. 3 The latency and time to peak of acetylcholine-induced depolarizations were less than those to stable agonists, and the response was briefer and less complex in shape. These differences were reduced, or disappeared, upon inhibition of cholinesterase. 4 The rate of loss of 42K and changes in length were measured in superfused strips weighing about 10 mg of separated longitudinal muscle of guinea-pig ileum. 5 Acetylcholine, carbachol, methylfurmethide, butyltrimethylammonium and TMA contracted the muscle and increased the rate of loss of 42K. 6 Contrary to previous reports, no evidence of a selective action of any of these agonists on 42K loss was detected. TMA appeared to be a partial agonist in evoking 42K loss, although it produced a maximum contraction. 7 The maximum 42K efflux produced by acetylcholine was about 40% of the maximum evoked by application of carbachol or methylfurmethide. If cholinesterase was inhibited, the 42K efflux evoked by maximally effective concentrations of acetylcholine was comparable to that evoked by a stable agonist. 8 These results are consistent with the idea that the muscarinic agonists used interact in an essentially similar way with muscarinic receptors to produce their effects on membrane potential, permeability, and tension.

Full text

PDF
319

Selected References

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

  1. Beld A. J., Ariëns E. J. Stereospecific binding as a tool in attempts to localize and isolate muscarinic receptors. Part II. Binding of (plus)-benzetimide, (minus)-benzetimide and atropine to a fraction from bovine tracheal smooth muscle and to bovine caudate nucleus. Eur J Pharmacol. 1974 Feb;25(2):203–209. doi: 10.1016/0014-2999(74)90051-x. [DOI] [PubMed] [Google Scholar]
  2. Birdsall N. J., Burgen A. S., Hiley C. R., Hulme E. C. Binding of agonists and antagonists to muscarinic receptors. J Supramol Struct. 1976;4(3):367–371. doi: 10.1002/jss.400040307. [DOI] [PubMed] [Google Scholar]
  3. Birdsall N. J., Burgen A. S., Hulme E. C. The binding of agonists to brain muscarinic receptors. Mol Pharmacol. 1978 Sep;14(5):723–736. [PubMed] [Google Scholar]
  4. Birdsall N. J., Hulme E. C. Biochemical studies on muscarinic acetylcholine receptors. J Neurochem. 1976 Jul;27(1):7–16. doi: 10.1111/j.1471-4159.1976.tb01536.x. [DOI] [PubMed] [Google Scholar]
  5. Bolton T. B. Effects of stimulating the acetylcholine receptor on the current-voltage relationships of the smooth muscle membrane studied by voltage clamp of potential recorded by micro-electrode. J Physiol. 1975 Aug;250(1):175–202. doi: 10.1113/jphysiol.1975.sp011048. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Bolton T. B. Mechanisms of action of transmitters and other substances on smooth muscle. Physiol Rev. 1979 Jul;59(3):606–718. doi: 10.1152/physrev.1979.59.3.606. [DOI] [PubMed] [Google Scholar]
  7. Bolton T. B. On the latency and form of the membrane responses of smooth muscle to the iontophoretic application of acetylcholine or carbachol. Proc R Soc Lond B Biol Sci. 1976 Aug 27;194(1114):99–119. doi: 10.1098/rspb.1976.0068. [DOI] [PubMed] [Google Scholar]
  8. Bolton T. B. The depolarizing action of acetylcholine or carbachol in intestinal smooth muscle. J Physiol. 1972 Feb;220(3):647–671. doi: 10.1113/jphysiol.1972.sp009728. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Burgen A. S., Hiley C. R., Young J. M. The binding of (3H)-propylbenzilycholine mustard by longitudinal muscle strips from guinea-pig small intestine. Br J Pharmacol. 1974 Jan;50(1):145–151. doi: 10.1111/j.1476-5381.1974.tb09602.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Burgen A. S., Hiley C. R., Young J. M. The properties of muscarinic receptors in mammalian cerebral cortex. Br J Pharmacol. 1974 Jun;51(2):279–285. doi: 10.1111/j.1476-5381.1974.tb09658.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Burgen A. S., Spero L. The effects of calcium and magnesium on the response of intestine smooth muscle to drugs. Br J Pharmacol. 1970 Nov;40(3):492–500. doi: 10.1111/j.1476-5381.1970.tb10630.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Casteels R. Calculation of the membrane potential in smooth muscle cells of the guinea-pig's taenia coli by the Goldman equation. J Physiol. 1969 Nov;205(1):193–208. doi: 10.1113/jphysiol.1969.sp008960. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Cox B., Lomas D. M. The effects of eserine and neostigmine on the guinea-pig ileum and on ileal longitudinal muscle strips. J Pharm Pharmacol. 1972 Jul;24(7):541–546. doi: 10.1111/j.2042-7158.1972.tb09054.x. [DOI] [PubMed] [Google Scholar]
  14. DEL CASTILLO L., KATZ B. A study of curare action with an electrical micromethod. Proc R Soc Lond B Biol Sci. 1957 May 7;146(924):339–356. doi: 10.1098/rspb.1957.0015. [DOI] [PubMed] [Google Scholar]
  15. DURBIN R. P., JENKINSON D. H. The effect of carbachol on the permeability of depolarized smooth muscle to inorganic ions. J Physiol. 1961 Jun;157:74–89. doi: 10.1113/jphysiol.1961.sp006706. [DOI] [PMC free article] [PubMed] [Google Scholar]
  16. GEORGE E. P. Resistance values in a syncytium. Aust J Exp Biol Med Sci. 1961 Jun;39:267–274. doi: 10.1038/icb.1961.27. [DOI] [PubMed] [Google Scholar]
  17. Gabella G. Hypertrophy of intestinal smooth muscle. Cell Tissue Res. 1975 Nov 7;163(2):199–214. [PubMed] [Google Scholar]
  18. Hulme E. C., Birdsall N. J., Burgen A. S., Mehta P. The binding of antagonists to brain muscarinic receptors. Mol Pharmacol. 1978 Sep;14(5):737–750. [PubMed] [Google Scholar]
  19. Kloog Y., Sachs D. I., Korczyn A. D., Heron D. S., Sokolovsky M. Muscarinic acetylcholine receptors in cat iris. Biochem Pharmacol. 1979 May 1;28(9):1505–1511. doi: 10.1016/0006-2952(79)90465-9. [DOI] [PubMed] [Google Scholar]
  20. Kloog Y., Sokolovsky M. Muscarinic acetylcholine receptors interactions: competition binding studies with agonists and antagonists. Brain Res. 1977 Sep 23;134(1):167–172. doi: 10.1016/0006-8993(77)90936-2. [DOI] [PubMed] [Google Scholar]
  21. Kuriyama H., Tomita T. The action potential in the smooth muscle of the guinea pig taenia coli and ureter studied by the double sucrose-gap method. J Gen Physiol. 1970 Feb;55(2):147–162. doi: 10.1085/jgp.55.2.147. [DOI] [PMC free article] [PubMed] [Google Scholar]
  22. Purves R. D. Muscarinic excitation: a microelectrophoretic study on cultured smooth muscle cells. Br J Pharmacol. 1974 Sep;52(1):77–86. doi: 10.1111/j.1476-5381.1974.tb09689.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  23. Rang H. P. The kinetics of action of acetylcholine antagonists in smooth muscle. Proc R Soc Lond B Biol Sci. 1966 Apr 19;164(996):488–510. doi: 10.1098/rspb.1966.0045. [DOI] [PubMed] [Google Scholar]
  24. Snyder S. H., Chang K. J., Kuhar M. J., Yamamura H. I. Biochemical indentification of the mammalian muscarinic cholinergic receptor. Fed Proc. 1975 Sep;34(10):1915–1921. [PubMed] [Google Scholar]
  25. Taylor I. K., Cuthbert A. W., Young M. Muscarinic receptors in rat intestinal muscle: comparison with the guinea pig. Eur J Pharmacol. 1975 Apr;31(2):319–326. doi: 10.1016/0014-2999(75)90055-2. [DOI] [PubMed] [Google Scholar]
  26. Ward D., Young J. M. Ligand binding to muscarinic receptors in intact longitudinal muscle strips from guinea-pig intestine. Br J Pharmacol. 1977 Oct;61(2):189–197. doi: 10.1111/j.1476-5381.1977.tb08404.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  27. Young J. M. Desensitisation and agonist binding to cholinergic receptors in intestinal smooth muscle. FEBS Lett. 1974 Sep 15;46(1):354–356. doi: 10.1016/0014-5793(74)80405-9. [DOI] [PubMed] [Google Scholar]

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

RESOURCES