High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor

This paper reports the synthesis and affinities on the 5HT(1A) versus the alpha(1)A receptors of new arylpiperazinylalkylthiothienopyrimidine and thiadiazole derivatives 16-24. Arylpiperazines 16-23 show affinities values in the nanomolar range for the 5HT(1A) receptor. The compound 16 is highly potent (K-i 0.26 nM, selectivity 28), the derivatives 20 and 21 are less potent, but highly selective (K-i 9.40 and 5.06 nM, selectivity 207 and 73, respectively). (C) 2000 Elsevier Science Ltd. All rights reserved.