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Abstract Five serotonin‐S 2 antagonists, ketanserin, pipamperone, methysergide, ritanserin, and LSD, were tested for their ability to inhibit signal transduction coupled to the serotonin‐S 2 receptor by measuring the serotonin‐induced 32 P phosphatidic acid formation. The five drugs inhibited the response in a non‐competitive manner. Since drugs such as ketanserin and pipamperone were found to dissociate rapidly from serotonin‐S 2 receptor sites in binding studies, slowly reversible binding can hardly explain the apparent non‐competitive inhibition of the biochemical effect. The authors, therefore, propose a new model of interaction between the serotonin‐S 2 receptor macromolecule and the signal transducing system that is compatible with the present and previous experimental observations.
Courcelles et al. (Thu,) studied this question.
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