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Piglet sinoatrial 5-HT receptors resemble human atrial 5-HT4-like receptors

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Summary

5-Hydroxytryptamine (5-HT), 5-carboxamidotryptamine (5-CT) and the gastrointestinal kinetic benzamides renzapride and cisapride caused tachycardia in spontaneously beating right atria of piglet in the presence of 400 nmol/l(±)-propranolol and 6 μmol/l cocaine. The maximum tachycardia caused by agonists, compared to that evoked by 200 μmol/l(−)-isoprenaline, was 63% for 5-HT, 50% for 5-CT, 50% for renzapride and 28% for cisapride. The rank order of potency was 5-HT > renzapride > cisapride > 5-CT. The effects of the agonists, but not those of (−)-isoprenaline, were antagonised by 3α-tropanyl-1H-indole-3-carboxylic acid (ICS 205930); the pKB of ICS 205930 (vs 5-HT) was 6.9. These characteristics suggest that piglet sinoatrial 5-HT receptors are similar to “so-called” 5-HT4 receptors previously described in mouse colliculi neurons. Piglet sinoatrial 5-HT4-like receptors resemble the human atrial 5-HT receptors that mediate positive isotropic effects of 5-HT.

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  1. Smith Kline Beecham Pharmaceuticals, The Frythe, Welwyn, AL6 9AR, Hertfordshire, UK

    Alberto J. Kaumann

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  1. Alberto J. Kaumann
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Kaumann, A.J. Piglet sinoatrial 5-HT receptors resemble human atrial 5-HT4-like receptors. Naunyn-Schmiedeberg's Arch Pharmacol 342, 619–622 (1990). https://doi.org/10.1007/BF00169055

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  • DOI: https://doi.org/10.1007/BF00169055

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