11123994 |
Zhang Y, Rothman RB, Dersch CM, de Costa BR, Jacobson AE, Rice KC: Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis (4-fluorophenyl) methoxy] ethyl]-4-(3-phenylpropyl) piperazine (GBR 12909). J Med Chem. 2000 Dec 14;43(25):4840-9.
A series of analogues related to 1-[2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl) piperazine (2) and 1- inverted question mark2-[bis (4-fluorophenyl) methoxy] ethyl inverted question mark-4-(3-phenylpropyl) piperazine (3) (GBR 12935 and GBR 12909, respectively), in which the piperazine moiety was replaced by bridged piperazines for structural rigidity, has been designed, synthesized, and evaluated for their ability to bind to the dopamine transporter (DAT) and to inhibit the uptake of (3) H-labeled dopamine (DA). |
31(0,1,1,1) |
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