Abstract
In this study, it has been clearly demonstrated that a selective 5-hydroxytryptamine (5-HT) 1A agonist, 8-OH-2-(di- n-propylamino)-tetraline (8-OH-DPAT, 1 μM) significantly inhibited forskolin (10 μM)-stimulated cyclic AMP (cAMP) accumulation in the C6BU-1 cells transfected with 5-HT 1A receptor gene. Further, this 8-OH-DPAT-induced inhibition of forskolin-stimulated activity was significantly attenuated after pre-exposure to 5-HT (10μM) for 12 h. Spiperone (l0μM), a 5-HT 1A and 5-HT 2A antagonist, prevented 5-HT-induced desensitization of 5-HT 1A receptor, but a selective 5-HT 2A receptor antagonist, ketanserin, did not. In addition, pre-exposure to a selective 5-HT 2A agonist, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI, 10μM), for 24 h did not alter the inhibitory effect of 8-OH-DPAT on forskolin-stimulated cAMP accumulation in these transfected cells, suggesting that prolonged exposure to 5-HT induced 5-HT 1A receptor desensitization, mediated by 5-HT 1A receptor but not 5-HT 2A receptors.
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