Synthesis, Dopamine Transporter Affinity, Dopamine Uptake Inhibition, and Locomotor Stimulant Activity of 2-Substituted 3β-Phenyltropane Derivatives

A series of 2β-substituted 3β-phenyltropanes were synthesized as analogs of cocaine and tested in vitro for their ability to displace bound [3H]WIN 35,428 (2b) and inhibit dopamine uptake in rat caudate-putamen tissue. The analogs bound with high affinity (K i = 11−22 nM) to the dopamine transporter...

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Veröffentlicht in:	Journal of medicinal chemistry 1997-03, Vol.40 (6), p.858-863
Hauptverfasser:	Xu, Lifen, Kelkar, Shreekrishna V, Lomenzo, Stacey A, Izenwasser, Sari, Katz, Jonathan L, Kline, Richard H, Trudell, Mark L
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites Binding, Competitive Biological and medical sciences Brain - drug effects Carrier Proteins - antagonists & inhibitors Carrier Proteins - metabolism Catecholaminergic system Cocaine - analogs & derivatives Cocaine - metabolism Cocaine - pharmacology Dopamine - metabolism Dopamine Plasma Membrane Transport Proteins Dopamine Uptake Inhibitors - chemical synthesis Dopamine Uptake Inhibitors - chemistry Dopamine Uptake Inhibitors - metabolism Dopamine Uptake Inhibitors - pharmacology Dose-Response Relationship, Drug Magnetic Resonance Spectroscopy Medical sciences Membrane Glycoproteins Membrane Transport Proteins Molecular Structure Motor Activity - drug effects Nerve Tissue Proteins Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Rats Tropanes - chemical synthesis Tropanes - chemistry Tropanes - metabolism Tropanes - pharmacology
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