ARYLPIPERAZIDE DERIVATIVES OF PHENYLPIPERAZINES AS A NEW CLASS OF POTENT AND SELECTIVE 5-HT1B RECEPTOR ANTAGONISTS

A new series of arylpiperazide derivatives of phenylpiperazines of gen eral formula 4 has been prepared and evaluated as 5-HT1B receptor anta gonists. In vitro experiments at human cloned 5-HT1B receptors show th at these derivatives are potent and selective 5-HT1B receptor, antagon ists. Among them, compound 4f was found to be orally active, to gain a ccess to the CNS and more importantly to induce an increase in extrace llular brain 5-HT upon systemic administration. (C) 1997 Elsevier Scie nce Ltd.