Activation of central 5HT1B receptors increases locomotor activity in mice

The effects of 5-HT1B/D receptor agonists anpirtoline, S-CM-GTNH2 and CP93129 were examined in locomotor activity tests in mice. Anpirtoline and S-CM-GTNH2 both significantly increased locomotor activity (ambulation) (minimum affective doses; 3 and 30 mg/kg respectively). CP93129 injected subcutaneously was without effect, but increased locomotor activity when given i.c.v. Thus activation of central 5-HT1B receptors results in increased locomotor activity. The effects of anpirtoline and S-CM-GTNH2 were blocked by the antagonist GR 127935 suggesting that GR 127935 is an effective antagonist of 5-HT1B receptors in vivo. (C) 1997 John Wiley & Sons, Ltd.