title: N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter.
abstract: A series of N-phenylalkyl-substituted tropane analogs of boat conformation was synthesized, and these tropanes were evaluated for their ability to inhibit high affinity uptake of dopamine (DA) and serotonin (5-HT) into striatal nerve endings (synaptosomes). Some of these compounds exhibit high affinity for the DA transporter with a 5-HT/DA transporter selectivity ratio of >50.
authors.affiliation: Drug Discovery Program, Institute for Cognitive and Computational Sciences, Georgetown University Medical Center, Washington, DC 20007-2197, USA.
authors.forename: K R
authors.initials: KR
authors.lastname: Prakash
authors.forename: A P
authors.initials: AP
authors.lastname: Tamiz
authors.forename: G L
authors.initials: GL
authors.lastname: Araldi
authors.forename: M
authors.initials: M
authors.lastname: Zhang
authors.forename: K M
authors.initials: KM
authors.lastname: Johnson
authors.forename: A P
authors.initials: AP
authors.lastname: Kozikowski
mesh_terms: D002352:Carrier Proteins / Q000378:metabolism*; D004298:Dopamine / Q000378:metabolism; D050483:Dopamine Plasma Membrane Transport Proteins; D066298:In Vitro Techniques; D008562:Membrane Glycoproteins / Q000378:metabolism*; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D012701:Serotonin / Q000378:metabolism; D050486:Serotonin Plasma Membrane Transport Proteins; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism; D014326:Tropanes / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D002352:Carrier Proteins; D050483:Dopamine Plasma Membrane Transport Proteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D050486:Serotonin Plasma Membrane Transport Proteins; D014326:Tropanes; D012701:Serotonin; D004298:Dopamine