TY - JOUR
T1 - Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909)
T2 - High affinity ligands for the dopamine transporter
AU - Prisinzano, Thomas
AU - Greiner, Elisabeth
AU - Johnson, Edward M.
AU - Dersch, Christina M.
AU - Marcus, Jamila
AU - Partilla, John S.
AU - Rothman, Richard B.
AU - Jacobson, Arthur E.
AU - Rice, Kenner C.
PY - 2002/9/12
Y1 - 2002/9/12
N2 - A series of 4-[2-[bis(4-fluorophenyl)methoxy]ethylpiperidines were examined for their ability to bind to the dopamine transporter (DAT), the norepinephrine transporter, and the serotonin transporter (SERT). In particular, the role of the N-substituent on affinity and selectivity for the DAT was probed. 4-[2-[Bis(4-fluorophenyl)methoxy]ethyl-1-(2-naphthylmethyl)piperidine was found to possess subnanomolar affinity (Ki = 0.7 nM) and good selectivity for the DAT (SERT/DAT = 323).
AB - A series of 4-[2-[bis(4-fluorophenyl)methoxy]ethylpiperidines were examined for their ability to bind to the dopamine transporter (DAT), the norepinephrine transporter, and the serotonin transporter (SERT). In particular, the role of the N-substituent on affinity and selectivity for the DAT was probed. 4-[2-[Bis(4-fluorophenyl)methoxy]ethyl-1-(2-naphthylmethyl)piperidine was found to possess subnanomolar affinity (Ki = 0.7 nM) and good selectivity for the DAT (SERT/DAT = 323).
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U2 - 10.1021/jm020264r
DO - 10.1021/jm020264r
M3 - Article
C2 - 12213078
AN - SCOPUS:0037068499
SN - 0022-2623
VL - 45
SP - 4371
EP - 4374
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 19
ER -