Abstract:
:We examined the effects of YM-31636 (2-(1H-imidazol-4-ylmethyl)-8H-indeno[1,2-d]thiazole monofumarate), a novel 5-HT3 receptor agonist, on gastrointestinal functions including visceral pain reflex in rats. Injection of YM-31636 increased the number of fecal pellets. This effect was completely inhibited by ramosetron, a 5-HT3 receptor antagonist. YM-31636 also increased the intracolonic pressure measured in both conscious and anesthetized rats. In isolated distal colon, YM-31636 increased the short-circuit current response. This effect was abolished by ramosetron. Both the maximal response and the potency of YM-31636 were weaker than those of other 5-HT3 receptor agonists. In two visceral pain reflex models, YM-31636 neither changed the magnitude of pressor response to colonic distension in anesthetized rats nor affected the visceromotor threshold to colorectal distension in conscious rats. In conclusion, YM-31636 facilitated defecation without increasing visceral pain. Consequently, 5-HT3 receptor agonists like YM-31636 would be promising in the treatment of chronic constipation.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Kiso T,Ito H,Miyata K,Kamato T,Naitoh Y,Iwaoka K,Yamaguchi Tdoi
10.1016/s0014-2999(01)01425-xkeywords:
subject
Has Abstractpub_date
2001-11-09 00:00:00pages
35-41issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(01)01425-Xjournal_volume
431pub_type
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