Skip to main content
NCBI home page
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1981 Feb;72(2):201–210. doi: 10.1111/j.1476-5381.1981.tb09114.x

Distribution and types of adrenoceptors in the guinea-pig ileum: the action of α-and β-adrenoceptor agonists

V Bauer
PMCID: PMC2071517  PMID: 6111369

Abstract

1 Segments of guinea-pig ileum and the myenteric plexus-longitudinal smooth muscle preparation were used for a study of the actions of adrenaline, noradrenaline, isoprenaline, ephedrine and phenylephrine on the responses of coaxially stimulated ileum at different distances from the ileocaecal valve.

2 The responses of the ileum to electrical stimulation were suppressed by adrenaline, nonadrenaline and ephedrine, while phenylephrine and isoprenaline inhibited them only partially.

3 The twitch inhibition elicited by these adrenoceptor agonists was the same at all distances from the ileocaecal valve. There was no significant difference between their cumulative and non-cumulative concentration-response curves.

4 Smooth muscle relaxation was induced only by isoprenaline and contraction only by phenylephrine at all distances from the ileocaecal junction. Adrenaline and noradrenaline evoked smooth muscle contraction in the terminal (0 to 20 cm), a concentration-dependent, biphasic response in the intermediate part (21 to 50 cm) and a relaxation in the proximal ileum (> 50 cm from the ilecocaecal valve). Ephedrine did not change significantly the smooth muscle tension in the terminal and the intermediate segments and induced smooth muscle relaxation in the proximal ones.

5 Ouabain and a potassium-free solution did not appear to influence the prejunctional action of noradrenaline nor the amplitude of smooth muscle relaxation in the proximal ileum, whereas the concentration-contractor response curves were significantly depressed and shifted to the right by ouabain and in a potassium-free solution.

6 The brief initial (phasic) contraction induced by acetylcholine was not influenced during the sustained increase or decrease in tension induced by catecholamines. On the contrary, the stimulatory catecholamine actions disappeared or were changed to smooth muscle relaxation by acetylcholine pretreatment. Potassium chloride pretreatment did not change the character of the adrenoceptor agonist action of the agonists studied.

7 Since there is a similar prejunctional action at all distances from the ileocaecal valve and a different postjunctional effect of the adrenoceptor agonists at different distances from the ileocaecal junction, it could be suggested that in the guinea-pig ileum there are at least two α-adrenoceptors (inhibitory prejunctional-α2, stimulatory postjunctional-α1), an inhibitory postjunctional β-adrenoceptor and an as yet uncharacterized inhibitory postjunctional receptor.

8 Based on the specific postjunctional action of phenylephrine and the prejunctional action of ephedrine in the guinea-pig ileum, these drugs could be used with success as `specific' α1- and α2-adrenoceptor stimulants.

Full text

PDF
201

Selected References

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

  1. AHLQUIST R. P., LEVY B. Andrenergic receptive mechanism of canine ileum. J Pharmacol Exp Ther. 1959 Oct;127:146–149. [PubMed] [Google Scholar]
  2. Anderson A. A., Lees G. M. Investigation of occurrence of tolerance to bronchodilator drugs in chronically pretreated guinea-pigs. Br J Pharmacol. 1976 Mar;56(3):331–338. doi: 10.1111/j.1476-5381.1976.tb07647.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Andersson R., Mohme-Lundholm E. Metabolic actions in intestinal smooth muscle associated with relaxation mediated by adrenergic alpha- and beta-receptors. Acta Physiol Scand. 1970 Jun;79(2):244–261. doi: 10.1111/j.1748-1716.1970.tb04724.x. [DOI] [PubMed] [Google Scholar]
  4. Andersson R., Mohme-Lundholm E. Studies on the relaxing actions mediated by stimulation of adrenergic alpha- and beta-receptors in taenia coli of the rabbit and guinea pig. Acta Physiol Scand. 1969 Nov;77(3):372–384. doi: 10.1111/j.1748-1716.1969.tb04582.x. [DOI] [PubMed] [Google Scholar]
  5. Andersson R. Role of cyclic AMP and Ca ++ in the metabolic and relaxing effects of catecholamines in intestinal smooth muscle. Acta Physiol Scand. 1972 Jul;85(3):312–322. doi: 10.1111/j.1748-1716.1972.tb05267.x. [DOI] [PubMed] [Google Scholar]
  6. BURNSTOCK G. The action of adrenaline on excitability and membrane potential in the taenia coli of the guinea-pig and the effect of DNP on this action and on the action of acetylcholine. J Physiol. 1958 Aug 29;143(1):183–194. doi: 10.1113/jphysiol.1958.sp006052. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Bauer V., Zakhari S. Pharmacological studies with beta-adrenoreceptor blocking agents I. Effect on the smooth muscle of the taenia coli of the guinea pig. Life Sci. 1977 Sep 1;21(5):683–694. doi: 10.1016/0024-3205(77)90076-5. [DOI] [PubMed] [Google Scholar]
  8. Bowman W. C., Hall M. T. Inhibition of rabbit intestine mediated by alpha- and beta-adrenoceptors. Br J Pharmacol. 1970 Feb;38(2):399–415. doi: 10.1111/j.1476-5381.1970.tb08528.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Brody T. M., Diamond J. Blockade of the biochemical correlates of contraction and relaxation in uterine and intestinal smooth muscle. Ann N Y Acad Sci. 1967 Feb 10;139(3):772–780. doi: 10.1111/j.1749-6632.1967.tb41245.x. [DOI] [PubMed] [Google Scholar]
  10. Bär H. P. Cyclic nucleotides and smooth muscle. Adv Cyclic Nucleotide Res. 1974;4(0):195–237. [PubMed] [Google Scholar]
  11. Bülbring E., Tomita T. Increase of membrane conductance by adrenaline in the smooth muscle of guinea-pig taenia coli. Proc R Soc Lond B Biol Sci. 1969 Mar 11;172(1027):89–102. doi: 10.1098/rspb.1969.0013. [DOI] [PubMed] [Google Scholar]
  12. Bülbring E., Tomita T. Suppression of spontaneous spike generation by catecholamines in the smooth muscle of the guinea-pig taenia coli. Proc R Soc Lond B Biol Sci. 1969 Mar 11;172(1027):103–119. doi: 10.1098/rspb.1969.0014. [DOI] [PubMed] [Google Scholar]
  13. Casteels R., Droogmans G., Hendrickx H. Membrane potential of smooth muscle cells in K-free solution. J Physiol. 1971 Sep;217(2):281–295. doi: 10.1113/jphysiol.1971.sp009571. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Costa M., Gabella G. Adrenergic innervation of the alimentary canal. Z Zellforsch Mikrosk Anat. 1971;122(3):357–377. doi: 10.1007/BF00935995. [DOI] [PubMed] [Google Scholar]
  15. Drew G. M. Pharmacological characterization of presynaptic alpha-adrenoceptors which regulate-cholinergic activity in the guinea-pig ileum [proceedings]. Br J Pharmacol. 1977 Mar;59(3):513P–513P. [PMC free article] [PubMed] [Google Scholar]
  16. Drew G. M. Pharmacological characterization of the presynaptic alpha-adrenoceptors regulating cholinergic activity in the guinea-pig ileum. Br J Pharmacol. 1978 Oct;64(2):293–300. doi: 10.1111/j.1476-5381.1978.tb17303.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  17. Gabella G. Fine structure of the myenteric plexus in the guinea-pig ileum. J Anat. 1972 Jan;111(Pt 1):69–97. [PMC free article] [PubMed] [Google Scholar]
  18. HARTFELDER G., KUSCHINSKY G., MOSLER K. H. Der Antagonismus verschiedener Sympatholytica gegenüber dem inhibitorischen Adrenalin-oder Noradrenalineffekt am elektrisch gereizten Meerschweinchenileum. Naunyn Schmiedebergs Arch Exp Pathol Pharmakol. 1958;234(2):91–101. [PubMed] [Google Scholar]
  19. Hamberger B., Norberg K. A., Ungerstedt U. Adrenergic synaptic terminals in autonomic ganglia. Acta Physiol Scand. 1965 Jul;64(3):285–286. [PubMed] [Google Scholar]
  20. Innes I. R., Kohli J. D. Excitatory action of sympathomimetic amines on 5-hydroxytryptamine receptors of gut. Br J Pharmacol. 1969 Mar;35(3):383–393. doi: 10.1111/j.1476-5381.1969.tb08280.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  21. Kosterlitz H. W., Lydon R. J., Watt A. J. The effects of adrenaline, noradrenaline and isoprenaline on inhibitory alpha- and beta-adrenoceptors in the longitudinal muscle of the guinea-pig ileum. Br J Pharmacol. 1970 Jun;39(2):398–413. doi: 10.1111/j.1476-5381.1970.tb12903.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  22. Langer S. Z. Sixth gaddum memorial lecture, National Institute for Medical Research, Mill Hill, January 1977. Presynaptic receptors and their role in the regulation of transmitter release. Br J Pharmacol. 1977 Aug;60(4):481–497. doi: 10.1111/j.1476-5381.1977.tb07526.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  23. MCDOUGAL M. D., WEST G. B. [The action of isoprenaline on intestinal muscle]. Arch Int Pharmacodyn Ther. 1952;90(1):86–92. [PubMed] [Google Scholar]
  24. MUNRO A. F. Effect of autonomic drugs on the responses of isolated preparations from the guinea-pig intestine to electrical stimulation. J Physiol. 1953 Apr 28;120(1-2):41–52. doi: 10.1113/jphysiol.1953.sp004871. [DOI] [PMC free article] [PubMed] [Google Scholar]
  25. McDOUGAL M. D., WEST G. B. The inhibition of the peristaltic reflex by sympathomimetic amines. Br J Pharmacol Chemother. 1954 Jun;9(2):131–137. doi: 10.1111/j.1476-5381.1954.tb00831.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  26. NORBERG K. A. ADRENERGIC INNERVATION OF THE INTESTINAL WALL STUDIED BY FLUORESCENCE MICROSCOPY. Int J Neuropharmacol. 1964 Sep;3:379–382. doi: 10.1016/0028-3908(64)90067-x. [DOI] [PubMed] [Google Scholar]
  27. Paton W. D., Vizi E. S. The inhibitory action of noradrenaline and adrenaline on acetylcholine output by guinea-pig ileum longitudinal muscle strip. Br J Pharmacol. 1969 Jan;35(1):10–28. doi: 10.1111/j.1476-5381.1969.tb07964.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  28. Paton W. D., Vizi E. S., Zar M. A. The mechanism of acetylcholine release from parasympathetic nerves. J Physiol. 1971 Jul;215(3):819–848. doi: 10.1113/jphysiol.1971.sp009500. [DOI] [PMC free article] [PubMed] [Google Scholar]
  29. Paton W. D., Zar M. A. The origin of acetylcholine released from guinea-pig intestine and longitudinal muscle strips. J Physiol. 1968 Jan;194(1):13–33. doi: 10.1113/jphysiol.1968.sp008392. [DOI] [PMC free article] [PubMed] [Google Scholar]
  30. Tansy M. F., Martin J. S., Landin W. E., Kendall F. M. Localization of isoproterenol-induced contractions of canine small intestine. J Pharm Sci. 1979 Jan;68(1):127–128. doi: 10.1002/jps.2600680147. [DOI] [PubMed] [Google Scholar]
  31. Wikberg J. Differentiation between pre- and postjunctional alpha-receptors in guinea pig ileum and rabbit aorta. Acta Physiol Scand. 1978 Jul;103(3):225–239. doi: 10.1111/j.1748-1716.1978.tb06210.x. [DOI] [PubMed] [Google Scholar]
  32. Wikberg J. Localization of adrenergic receptors in guinea pig ileum and rabbit jejunum to cholinergic neurons and to smooth muscle cells. Acta Physiol Scand. 1977 Feb;99(2):190–207. doi: 10.1111/j.1748-1716.1977.tb10370.x. [DOI] [PubMed] [Google Scholar]
  33. Willems J. L., Bernard P. J., Delaunois A. L., De Schaepdryver A. F. Adrenergic receptors in the progesterone dominated rabbit uterus. Arch Int Pharmacodyn Ther. 1965 Sep;157(1):243–250. [PubMed] [Google Scholar]

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

RESOURCES