Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl) propyl] bis (4-fluorophenyl) amines as potential irreversible ligands for the dopamine …

J Cao, JR Lever, T Kopajtic, JL Katz…

Index: Cao, Jianjing; Kulkarni, Santosh S.; Husbands, Stephen M.; Bowen, Wayne D.; Williams, Wanda; Kopajtic, Theresa; Katz, Jonathan L.; George, Clifford; Newman, Amy Hauck Journal of Medicinal Chemistry, 2003 , vol. 46, # 13 p. 2589 - 2598

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Citation Number: 12

Abstract

Potential irreversible ligands were prepared, based on a series of 3-(1-piperazinyl) propyl-N, N-bis (4-fluorophenyl) amines, as molecular probes for the dopamine transporter (DAT). Both azido-and isothiocyanato-substituted phenylalkyl analogues were synthesized and evaluated for displacement of [3H] WIN 35 428 in rat caudate putamen tissue. All of the analogues showed moderate binding potencies at the DAT. The azido analogue, 16b, ...