Effects of moderate and intensive training on functional activity of central 5-HT1B receptors in the rat substantia nigra.

The efficacy of the selective 5-HT1B receptor agonist CP 93,129 in inhibiting the forskolin-stimulated adenylyl cyclase activity in the rat substantia nigra was reduced by both moderate and intensive prolonged training compared with sedentary resting rats. The concentration-response curves of the agonist were shifted to the right with a sixfold increase of the half-maximal inhibitory concentration. A difference was observed between the two training exercises in regard to further changes in 5-HT1B receptor sensitivity induced by an acute restraint stress. This manipulation did not affect the functional response of the 5-HT1B receptors further in moderately trained rats, whereas an additional desensitization of the 5-HT1B receptors was observed in intensively trained rats. These results strongly suggest the existence of regulation mechanisms altering the functional efficacy of 5-HT1B receptors and, accordingly, affecting the serotonergic activity, since 5-HT1B receptors modulate the neuronal release of the amine.