Skip to main content
NCBI home page
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1990 Nov;101(3):553–558. doi: 10.1111/j.1476-5381.1990.tb14119.x

An examination of the 5-HT3 receptor mediating contraction and evoked [3H]-acetylcholine release in the guinea-pig ileum.

A Fox 1, I K Morton 1
PMCID: PMC1917721  PMID: 2150179

Abstract

1. The relative contributions of two classes of 5-hydroxytryptamine (5-HT) receptor (5-HT2 and 5-HT3) to the contractile action of 5-HT, 2-methyl-5-hydroxytryptamine (2-methyl-5-HT) and alpha-methyl-5-hydroxytryptamine (alpha-methyl-5-HT) were studied in the guinea-pig ileum longitudinal muscle-myenteric plexus strip (LMMP) preparation. Contractility studies were combined with an analysis of the effects of the three agonists on [3H]-acetylcholine ([3H]-ACh) release from preparations preincubated with [3H]-choline. 2. In contracting the LMMP, 5-HT was approximately one order of magnitude more active than 2-methyl-5-HT and alpha-methyl-5-HT, with relative activities for 5-HT: 2-methyl-5-HT: alpha-methyl-5-HT of 1.00: 0.13: 0.10. 3. Ketanserin (1 microM) was without effect on the concentration-response curves for concentration to 5-HT. 2-methyl-5-HT or alpha-methyl-5-HT, whilst ondansetron (GR38032F: 1 microM) produced a parallel rightward displacement of the upper part of the concentration-response curves to 5-HT and alpha-methyl-5-HT and of the entire curve to 2-methyl-5-HT. 4. In increasing the spontaneous release of [3H]-ACh from the LMMP, 5-HT was again approximately one order of magnitude more active than 2-methyl-5-HT and alpha-methyl-5-HT with relative activities for 5-HT: 2-methyl-5-HT: alpha-methyl-5-HT of 1.00: 0.19: 0.11. 5.(ABSTRACT TRUNCATED AT 250 WORDS)

Full text

PDF
553

Selected References

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

  1. BROWNLEE G., JOHNSON E. S. THE SITE OF THE 5-HYDROXYTRYPTAMINE RECEPTOR ON THE INTRAMURAL NERVOUS PLEXUS OF THE GUINEA-PIG ISOLATED ILEUM. Br J Pharmacol Chemother. 1963 Oct;21:306–322. doi: 10.1111/j.1476-5381.1963.tb01529.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Black J. W., Shankley N. P. Pharmacological analysis of muscarinic receptors coupled to oxyntic cell secretion in the mouse stomach. Br J Pharmacol. 1985 Nov;86(3):601–607. doi: 10.1111/j.1476-5381.1985.tb08936.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Bradley P. B., Engel G., Feniuk W., Fozard J. R., Humphrey P. P., Middlemiss D. N., Mylecharane E. J., Richardson B. P., Saxena P. R. Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine. Neuropharmacology. 1986 Jun;25(6):563–576. doi: 10.1016/0028-3908(86)90207-8. [DOI] [PubMed] [Google Scholar]
  4. Buchheit K. H., Engel G., Mutschler E., Richardson B. Study of the contractile effect of 5-hydroxytryptamine (5-HT) in the isolated longitudinal muscle strip from guinea-pig ileum. Evidence for two distinct release mechanisms. Naunyn Schmiedebergs Arch Pharmacol. 1985 Mar;329(1):36–41. doi: 10.1007/BF00695189. [DOI] [PubMed] [Google Scholar]
  5. Butler A., Hill J. M., Ireland S. J., Jordan C. C., Tyers M. B. Pharmacological properties of GR38032F, a novel antagonist at 5-HT3 receptors. Br J Pharmacol. 1988 Jun;94(2):397–412. doi: 10.1111/j.1476-5381.1988.tb11542.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Chahl L. A. Substance P mediates atropine-sensitive response of guinea-pig ileum to serotonin. Eur J Pharmacol. 1983 Mar 4;87(4):485–489. doi: 10.1016/0014-2999(83)90090-0. [DOI] [PubMed] [Google Scholar]
  7. Clarke D. E., Craig D. A., Fozard J. R. The 5-HT4 receptor: naughty, but nice. Trends Pharmacol Sci. 1989 Oct;10(10):385–386. doi: 10.1016/0165-6147(89)90177-6. [DOI] [PubMed] [Google Scholar]
  8. Costa M., Furness J. B. The sites of action of 5-hydroxytryptamine in nerve-muscle preparations from the guinea-pig small intestine and colon. Br J Pharmacol. 1979 Feb;65(2):237–248. doi: 10.1111/j.1476-5381.1979.tb07824.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Feniuk W., Humphrey P. P., Watts A. D. 5-Hydroxytryptamine-induced relaxation of isolated mammalian smooth muscle. Eur J Pharmacol. 1983 Dec 9;96(1-2):71–78. doi: 10.1016/0014-2999(83)90530-7. [DOI] [PubMed] [Google Scholar]
  10. Fozard J. R. MDL 72222: a potent and highly selective antagonist at neuronal 5-hydroxytryptamine receptors. Naunyn Schmiedebergs Arch Pharmacol. 1984 May;326(1):36–44. doi: 10.1007/BF00518776. [DOI] [PubMed] [Google Scholar]
  11. GADDUM J. H., PICARELLI Z. P. Two kinds of tryptamine receptor. Br J Pharmacol Chemother. 1957 Sep;12(3):323–328. doi: 10.1111/j.1476-5381.1957.tb00142.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Ireland S. J., Tyers M. B. Pharmacological characterization of 5-hydroxytryptamine-induced depolarization of the rat isolated vagus nerve. Br J Pharmacol. 1987 Jan;90(1):229–238. doi: 10.1111/j.1476-5381.1987.tb16844.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Kilbinger H., Pfeuffer-Friederich I. Two types of receptors for 5-hydroxytryptamine on the cholinergic nerves of the guinea-pig myenteric plexus. Br J Pharmacol. 1985 Jun;85(2):529–539. doi: 10.1111/j.1476-5381.1985.tb08890.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. RANG H. P. STIMULANT ACTIONS OF VOLATILE ANAESTHETICS ON SMOOTH MUSCLE. Br J Pharmacol Chemother. 1964 Apr;22:356–365. doi: 10.1111/j.1476-5381.1964.tb02040.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Richardson B. P., Engel G., Donatsch P., Stadler P. A. Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs. Nature. 1985 Jul 11;316(6024):126–131. doi: 10.1038/316126a0. [DOI] [PubMed] [Google Scholar]
  16. Sanger G. J. Increased gut cholinergic activity and antagonism of 5-hydroxytryptamine M-receptors by BRL 24924: potential clinical importance of BRL 24924. Br J Pharmacol. 1987 May;91(1):77–87. doi: 10.1111/j.1476-5381.1987.tb08985.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  17. Sanger G. J., Nelson D. R. Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron). Eur J Pharmacol. 1989 Jan 10;159(2):113–124. doi: 10.1016/0014-2999(89)90695-x. [DOI] [PubMed] [Google Scholar]
  18. Szerb J. C. Storage and release of labelled acetylcholine in the myenteric plexus of the guinea-pig ileum. Can J Physiol Pharmacol. 1976 Feb;54(1):12–22. doi: 10.1139/y76-003. [DOI] [PubMed] [Google Scholar]
  19. Wikberg J. Release of 3H-acetylcholine from isolated guinea pig ileum. A radiochemical method for studying the release on the cholinergic neurotransmitter in the intestine. Acta Physiol Scand. 1977 Nov;101(3):302–317. doi: 10.1111/j.1748-1716.1977.tb06012.x. [DOI] [PubMed] [Google Scholar]
  20. Wormser U., Laufer R., Hart Y., Chorev M., Gilon C., Selinger Z. Highly selective agonists for substance P receptor subtypes. EMBO J. 1986 Nov;5(11):2805–2808. doi: 10.1002/j.1460-2075.1986.tb04571.x. [DOI] [PMC free article] [PubMed] [Google Scholar]

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

RESOURCES