Pharmacological profile of the 5-hydroxytryptamine receptor that mediates relaxation of rat oesophageal smooth muscle

S. E. Ohia, Y. D. Cheung, D. Bieger, Christopher Triggle

Research output: Contribution to journalArticle

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Abstract

1. 1. The pharmacological profile of the inhibitory 5-hydroxytrytamine (5-HT) receptor in rat oesophageal smooth muscle has been characterized by means of a series of agonists active at 5-HT1-, 5-HT2-, 5-HT3- and 5-HT4-receptor sites, and a broad range of antagonists. The possible involvement of cyclic nucleotides in the 5-HT response was also examined. 2. 2. Under conditions of tone induced by muscarinic receptor activation, the upper two-thirds (proximal segment) of the oesophageal smooth muscle tunic was more sensitive to the inhibitory effects of 5-HT receptor agonists when compared with the distal region. 3. 3. The inhibitory response to 5-HT was blocked by MDL 72222 (5-HT3 antagonist) and ICS 205-930 (5-HT3/5-HT4 antagonist) but not by antagonists active at 5-HT1- or 5-HT2-receptors. 4. 4. The phosphodiesterase inhibitor, 3-isobutyl-methyl-xanthine (IBMX) enhanced oesophageal smooth muscle inhibitory response to 5-HT, isoprenaline and forskolin, but not that elicited by the potassium channel opener, BRL 34915. 5. 5. 5-HT increased tissue cyclic AMP content over basal levels in proximal and distal segments of oesophageal smooth muscle. However, 5-HT had no significant effect on basal cyclic GMP levels in both segments. 6. 6. We conclude that the inhibitory 5-HT receptor in rat oesophageal smooth muscle may represent a high affinity subtype which is sensitive to 5-HT3/5-HT4 antagonists and is coupled to the cyclic AMP pathway.

Original languageEnglish
Pages (from-to)649-658
Number of pages10
JournalGeneral Pharmacology
Volume23
Issue number4
DOIs
Publication statusPublished - 1992
Externally publishedYes

Fingerprint

Serotonin Receptors
Smooth Muscle
Pharmacology
Serotonin 5-HT4 Receptor Antagonists
tropisetron
Cyclic AMP
Phosphodiesterase 3 Inhibitors
Receptors, Serotonin, 5-HT4
Cromakalim
Serotonin 5-HT3 Receptor Antagonists
Serotonin Receptor Agonists
Xanthine
Cyclic Nucleotides
Potassium Channels
Cyclic GMP
Muscarinic Receptors
Colforsin
Isoproterenol

ASJC Scopus subject areas

  • Pharmacology

Cite this

Pharmacological profile of the 5-hydroxytryptamine receptor that mediates relaxation of rat oesophageal smooth muscle. / Ohia, S. E.; Cheung, Y. D.; Bieger, D.; Triggle, Christopher.

In: General Pharmacology, Vol. 23, No. 4, 1992, p. 649-658.

Research output: Contribution to journalArticle

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