Characterisation of 5-HT2 receptor subtypes in the Suncus murinus intestine

Farideh A. Javid, Robert J. Naylor

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

The involvement of 5-HT2 receptor subtypes in mediating a contraction response in the isolated intestine of Suncus murinus was investigated using DOI ((±)-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane, a 5-HT2 receptor agonist) which produced a bell-shaped concentration response curve that was significantly (p<0.05) reduced by methysergide (a 5-HT(1/2) receptor antagonist, 1 μM) but not ketanserin (a 5-HT(2A) receptor antagonist, 1 μM), yohimbine (a 5-HT(2B) receptor antagonist, 1 μM) or a combination of ondansetron (a 5-HT3 receptor antagonist, 1 μM) plus SB204070 (8-amino-7- chloro(N-butyl-4-piperidyl) methylbenzo-1,4-dioxan-5-carboxylate hydrochloride, a 5-HT4 receptor antagonist, 1 nM). The contraction response to the lower concentrations of DOI (10 nM-0.3 μM) was reduced in the presence of SB206553 (5-methyl-1-(3-pyridylcarbamoyl)-1,2,3,5- tetrahydropyrrolo[2,3-f]indole, a 5-HT(2B/2C) receptor antagonist, 1 μM), whilst conversely, the reducing response to the higher concentrations of DOI (1-30 μM) was prevented. A repeated challenge with 3 μM DOI produced a smaller response (desensitisation) and also reduced the response to 5-HT (5- hydroxytryptamine, 0.3 μM) that was inhibited by SB206553 (1 μM). Data indicate that 5-HT(2C) receptors are likely candidates to mediate the contractile response to DOI and demonstrate desensitisation to repeated challenges.

Original languageEnglish
Pages (from-to)161-169
Number of pages9
JournalEuropean Journal of Pharmacology
Volume381
Issue number2-3
DOIs
Publication statusPublished - 24 Sep 1999
Externally publishedYes

Fingerprint

Intestines
Serotonin
Serotonin 5-HT4 Receptor Antagonists
Serotonin 5-HT2 Receptor Agonists
Receptors, Serotonin, 5-HT4
Serotonin 5-HT3 Receptor Antagonists
Receptors, Serotonin, 5-HT3
Methysergide
Ondansetron
Ketanserin
Propane
Yohimbine
SB 206553

Cite this

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title = "Characterisation of 5-HT2 receptor subtypes in the Suncus murinus intestine",
abstract = "The involvement of 5-HT2 receptor subtypes in mediating a contraction response in the isolated intestine of Suncus murinus was investigated using DOI ((±)-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane, a 5-HT2 receptor agonist) which produced a bell-shaped concentration response curve that was significantly (p<0.05) reduced by methysergide (a 5-HT(1/2) receptor antagonist, 1 μM) but not ketanserin (a 5-HT(2A) receptor antagonist, 1 μM), yohimbine (a 5-HT(2B) receptor antagonist, 1 μM) or a combination of ondansetron (a 5-HT3 receptor antagonist, 1 μM) plus SB204070 (8-amino-7- chloro(N-butyl-4-piperidyl) methylbenzo-1,4-dioxan-5-carboxylate hydrochloride, a 5-HT4 receptor antagonist, 1 nM). The contraction response to the lower concentrations of DOI (10 nM-0.3 μM) was reduced in the presence of SB206553 (5-methyl-1-(3-pyridylcarbamoyl)-1,2,3,5- tetrahydropyrrolo[2,3-f]indole, a 5-HT(2B/2C) receptor antagonist, 1 μM), whilst conversely, the reducing response to the higher concentrations of DOI (1-30 μM) was prevented. A repeated challenge with 3 μM DOI produced a smaller response (desensitisation) and also reduced the response to 5-HT (5- hydroxytryptamine, 0.3 μM) that was inhibited by SB206553 (1 μM). Data indicate that 5-HT(2C) receptors are likely candidates to mediate the contractile response to DOI and demonstrate desensitisation to repeated challenges.",
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Characterisation of 5-HT2 receptor subtypes in the Suncus murinus intestine. / Javid, Farideh A.; Naylor, Robert J.

In: European Journal of Pharmacology, Vol. 381, No. 2-3, 24.09.1999, p. 161-169.

Research output: Contribution to journalArticle

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