Partial agonistic activity of GR43175 at the inhibitory prejunctional 5-HT1-like receptor in rat kidney

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Abstract
1 The pharmacological effect of the selective 5-HT receptor agonist GR43175 has been studied in the isolated perfused rat kidney with particular reference to the inhibitory prejunctional 5-HT1-like receptor. 2 GR43175 (1 .times. 10-8 to 1 .times. 10-5 M) inhibited the electrically evoked release of tritium from renal noradrenergic nerves but did not affect the basal (nonstimulated) release of tritium or perfusion pressure. 3 The inhibitory prejunctional action of GR43175, as well as that of 5-HT, was blocked by methiothepin, suggesting that both agonists act at the inhibitory 5-HT1-like site. 4 GR43175, relative to 5-HT, acted as a weak partial agonist at the inhibitory prejunctional 5-HT1-like receptor and antagonized 5-HT-induced inhibition of tritium release, suggesting again that a common site of action is involved. 5 The results support the conclusion that the 5-HT1-like receptor activated by GR43175 in the rat kidney is very similar to that identified in dog saphenous vein and certain other tissues.

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