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The 5-hydroxytryptamine (5-HT2) receptor stimulates inositol phosphate formation in intact and broken WRK1 cells: determination of occupancy- response relationships for 5-HT agonists

RN Cory, B Rouot, G Guillon, F Sladeczek, MN Balestre and J Bockaert

5-Hydroxytryptamine (5-HT) stimulates the accumulation of inositol- trisphosphate in WRK1 cells, a cell line originating from a rat mammary tumor. 5-HT acts via a single receptor type for which it has an affinity constant estimated to be 1.27 microM. A series of agonists known to act at 5-HT2 receptors are partial agonists in this system and have a rank order of relative intrinsic efficacies corresponding to that seen in other systems possessing 5-HT2 receptors. There is an essentially linear occupancy-response relationship for 5-HT and other agonists indicating the absence of a strong amplification mechanism between receptor activation and inositol phosphate formation. The selective blockade of the 5-HT response by nanomolar concentrations of 5-HT2 selective antagonists but not by drugs acting at other 5-HT receptor subtypes suggest that the receptor in WRK1 cells is of the 5- HT2 type. Additionally, we demonstrate that in WRK1 membranes 5-HT acts via the 5-HT2 receptor to elicit a GTP dependent increase in the production of inositol-bisphosphate and inositol-trisphosphate. These properties of the WRK1 cell line indicate that it is a useful model with which to study the nature of 5-HT receptor coupling to the putative second messenger(s), the inositol phosphates.

Volume 241, Issue 1, pp. 258-267, 04/01/1987
Copyright © 1987 by American Society for Pharmacology and Experimental Therapeutics






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Copyright © 1987 by the American Society for Pharmacology and Experimental Therapeutics.