Comparison of 5-HT4 Receptors in Guinea-Pig Colon and Rat Oesophagus: Effects of Novel Agonists and Antagonists.
Naunyn-Schmiedeberg's archives of pharmacology(1996)
Abstract
5-HT4 receptors in isolated distal colon myenteric plexus of guinea-pig, mediating contraction of longitudinal smooth muscle, have been further characterized by selective agonists and antagonists. The indole agonists, 5-HT and 5-methoxytryptamine (5-MeOT), were full agonists (relative to 5-HT) with potency values (pEC50) of 8.0 ± 0.1 (n = 50) and 7.8 ± 0.1 (n = 12), respectively. 5-HT4 receptor agonists of other structural classes, including benzimidazolones (BIMU 1 and BIMU 8), and benzamides ((S)-zacopride, (R)-zacopride, renzapride, SC 49518) were partial agonists with intrinsic activities less than that of 5-HT. In general, the potencies for these compounds at 5-HT4 receptors in guinea-pig colon were similar to the potencies seen in the rat isolated oesophagus, where 5-HT4 receptors mediate relaxation.
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Key words
5-HT4 receptors,Guinea-pig distal colon,Rat oesophagus,GR 113808,SB 204070,(S)RS 56532,RS 23597
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