| 12213078 |
Prisinzano T, Greiner E, Johnson EM 2nd, Dersch CM, Marcus J, Partilla JS, Rothman RB, Jacobson AE, Rice KC: Piperidine analogues of 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR 12909): high affinity ligands for the dopamine transporter. J Med Chem. 2002 Sep 12;45(19):4371-4.
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 (K (i) = 0.7 nM) and good selectivity for the DAT (SERT/DAT = 323). |
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