Synthesis and evaluation of new 2-piperazinylbnenzothiazoles with high 5-HT(1A) and 5-HT3 affinities

Article abstract of DOI:10.1016/0223-5234(96)88289-4

Original 2-piperazinylbenzothiazole derivatives were synthesized and studied as mixed ligands for serotoninergic 5-HT(1A) and 5-HT₃ receptors. The studied compounds exhibited significant affinities for these two serotoninergic receptor subtypes. The pharmacological profile of these ligands was agonist for 5-HT(1A) receptors and antagonist for 5-HT₃ receptor subsites. Compounds with such a pharmacological profile are of clinical relevance in the treatment of psychotropic diseases (eg anxiety, depression and schizophrenia). The present paper reports the chemistry and the in vitro pharmacological evaluation of these ligands.