Analogues of the 5-HT(1A) serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced α1-adrenergic affinity

Article abstract of DOI:10.1021/jm00112a043

1-(2-Methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine (NAN-190; 1a) is a putative postsynaptic 5-HT(1A) serotonin antagonist. This high affinity ligand (K(i) = 0.6 nM), although selective for 5-HT(1A) versus other 5-HT receptors, binds with nearly equa