Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:23

Article

Motel, William C.¹  Healy, Jason R.²  Viard, Eddy²  Pouw, Buddy³  Martin, Kelly E.^1,4  Matsumoto, Rae R.^2,3  Coop, Andrew¹ 

[1] Univ Maryland, Sch Pharm, Dept Pharmaceut Sci, Baltimore, MD 21201 USA

[2] W Virginia Univ, Sch Pharm, Dept Basic Pharmaceut Sci, Morgantown, WV 26506 USA

[3] Univ Oklahoma, Hlth Sci Ctr, Dept Pharmaceut Sci, Coll Pharm, Oklahoma City, OK 73190 USA

[4] Carolinas Med Ctr, Dept Pharm, Charlotte, NC 28203 USA

关键词: Sigma receptor;    Dopamine transporter;    Structure-activity relationships;    Neurotransmitter;    Cocaine;    Methamphetamine;   

DOI  :  10.1016/j.bmcl.2013.09.038

来源: Elsevier

【 摘 要 】

Selective sigma(2) ligands continue to be an active target for medications to attenuate the effects of psychostimulants. In the course of our studies to determine the optimal substituents in the sigma(2)-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorophenyl)-4-phenethylpiperazine actually had preferentially increased affinity for dopamine transporters (DAT), yielding a highly selective DAT ligand. (C) 2013 Elsevier Ltd. All rights reserved.

【 授权许可】

Free