PMID: 8950316Jan 1, 1996Paper

Identification and characterization of the 5-HT4 receptor in the intestinal tract and striatum of the guinea pig

Life Sciences
Y Uchiyama-TsuyukiM Muramatsu

Abstract

Receptors for 5-hydroxytryptamine (5-HT) of the 5-HT4 type were investigated in the intestinal tract and the striatum in guinea-pig, in binding studies using the 5-HT4 radioligand, [3H]GR113808. In the intestinal tract, specific binding was observed in preparations of the longitudinal muscle with the myenteric plexus (LMMPs) but not in the whole tissue. Saturable binding of [3H]GR113808 was demonstrated (striatum: Kd = 0.054 +/- 0.002 nM, Bmax = 90.25 +/- 10.44 fmol/mg protein, LMMPs of ileum: Kd = 0.077 +/- 0.016 nM, Bmax = 11.95 +/- 3.24 fmol/mg protein). Selective 5-HT4 receptor agonists and antagonists inhibited binding of [3H]GR113808 with high affinities in LMMPs of the ilcum and which correlated well with their actions on the striatum (r = 0.98), as indicated by the rank order of displacement potencies: SDZ205-557 > LY297524 > cisapride = BIMU8 > 5-HT > mosapride > renzapride > 5-hydroxy-N-methyltryptamine(5-HMT) > (+/-) zacopride > alpha-methyl-5-hydroxytryptamine (alpha-M-5-HT) > 5-methyltryptamine(5-MT) > 5-carboxamidotryptamine (5-CT). The number of binding sites of [3H]GR113808 in the intestine was significantly smaller than that in the brain. In the intestine, a larger number of binding sites was noted in the upper...Continue Reading

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Citations

Dec 17, 2003·Proceedings of the National Academy of Sciences of the United States of America·Miro Smriga, Kunio Torii
Sep 1, 2011·Progress in Neurobiology·Philippe HuotJonathan M Brotchie
Feb 13, 2007·British Journal of Pharmacology·R G VickeryJ A M Smith
Jun 25, 1998·Japanese Journal of Pharmacology·T YoshikawaK Hosoki
Sep 23, 2003·European Journal of Gastroenterology & Hepatology·Magnus RuthLars Lundell

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