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. 1986 Jun;88(2):451–455. doi: 10.1111/j.1476-5381.1986.tb10223.x

The effect of ionic strength on cardiac muscarinic receptors.

A S Burgen
PMCID: PMC1916837  PMID: 3730701

Abstract

The binding of N-methylscopolamine (NMS) and carbachol to muscarinic receptors in the rat heart has been measured as a function of ionic strength (mu). The binding of NMS was reduced by 3.69 fold for a 10 fold increase in ionic strength. The binding of carbachol was affected in two ways. Firstly, the proportions of the subsites were changed. Above mu = 0.5 M, the superhigh (SH) subsite was converted into the low (L) subsite and above mu = 0.8 M, the high (H) subsite was also converted into the L subsite. Therefore, at high ionic strength, no agonist-determined subsites can be detected. In addition, increase in ionic strength reduced the binding of carbachol to all subsites and to a much greater extent than for NMS.

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Selected References

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

  1. Berrie C. P., Birdsall N. J., Burgen A. S., Hulme E. C. Guanine nucleotides modulate muscarinic receptor binding in the heart. Biochem Biophys Res Commun. 1979 Apr 27;87(4):1000–1005. doi: 10.1016/s0006-291x(79)80006-6. [DOI] [PubMed] [Google Scholar]
  2. Birdsall N. J., Burgen A. S., Hulme E. C. A study of the muscarinic receptor by gel electrophoresis. Br J Pharmacol. 1979 Jun;66(2):337–342. doi: 10.1111/j.1476-5381.1979.tb13685.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Birdsall N. J., Burgen A. S., Hulme E. C., Wells J. W. The effects of ions on the binding of agonists and antagonists to muscarinic receptors. Br J Pharmacol. 1979 Nov;67(3):371–377. doi: 10.1111/j.1476-5381.1979.tb08690.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Birdsall N. J., Hulme E. C., Burgen A. The character of the muscarinic receptors in different regions of the rat brain. Proc R Soc Lond B Biol Sci. 1980 Feb 13;207(1166):1–12. doi: 10.1098/rspb.1980.0011. [DOI] [PubMed] [Google Scholar]
  5. Haga K., Haga T. Purification of the muscarinic acetylcholine receptor from porcine brain. J Biol Chem. 1985 Jul 5;260(13):7927–7935. [PubMed] [Google Scholar]
  6. Hulme E. C., Berrie C. P., Birdsall N. J., Burgen A. S. Two populations of binding sites for muscarinic antagonists in the rat heart. Eur J Pharmacol. 1981 Jul 17;73(2-3):137–142. doi: 10.1016/0014-2999(81)90085-6. [DOI] [PubMed] [Google Scholar]
  7. Peterson G. L., Herron G. S., Yamaki M., Fullerton D. S., Schimerlik M. I. Purification of the muscarinic acetylcholine receptor from porcine atria. Proc Natl Acad Sci U S A. 1984 Aug;81(15):4993–4997. doi: 10.1073/pnas.81.15.4993. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Pfaffinger P. J., Martin J. M., Hunter D. D., Nathanson N. M., Hille B. GTP-binding proteins couple cardiac muscarinic receptors to a K channel. Nature. 1985 Oct 10;317(6037):536–538. doi: 10.1038/317536a0. [DOI] [PubMed] [Google Scholar]
  9. Rosenberger L. B., Yamamura H. I., Roeske W. R. Cardiac muscarinic cholinergic receptor binding is regulated by Na+ and guanyl nucleotides. J Biol Chem. 1980 Feb 10;255(3):820–823. [PubMed] [Google Scholar]
  10. Shirakawa O., Tanaka C. Molecular characterization of muscarinic receptor subtypes in bovine cerebral cortex by radiation inactivation and molecular exclusion h.p.l.c. Br J Pharmacol. 1985 Oct;86(2):375–383. doi: 10.1111/j.1476-5381.1985.tb08906.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Wei J. W., Sulakhe P. V. Agonist-antagonist interactions with rat atrial muscarinic cholinergic receptor sites: differential regulation by guanine nucleotides. Eur J Pharmacol. 1979 Sep 1;58(1):91–92. doi: 10.1016/0014-2999(79)90346-7. [DOI] [PubMed] [Google Scholar]

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