Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: potential positron emission tomography (PET) imaging agents for the dopamine transporter
| Autor: | Nora S. Kula, Rushi Zong, Xiao-Hui Gu, John L. Neumeyer, Ross J. Baldessarini |
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| Rok vydání: | 2001 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Nerve Tissue Proteins Binding Competitive Biochemistry Iodine Radioisotopes Radioligand Assay Structure-Activity Relationship chemistry.chemical_compound Cocaine Drug Discovery medicine Animals Molecular Biology Serotonin transporter Fluoroethyl Dopamine transporter Serotonin Plasma Membrane Transport Proteins Dopamine Plasma Membrane Transport Proteins Membrane Glycoproteins Norepinephrine Plasma Membrane Transport Proteins Symporters biology medicine.diagnostic_test Organic Chemistry Membrane Transport Proteins Tropane Pet imaging Rats chemistry Norepinephrine transporter Positron emission tomography biology.protein Molecular Medicine Carrier Proteins Selectivity Tomography Emission-Computed Tropanes |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 11:3049-3053 |
| ISSN: | 0960-894X |
| Popis: | A series of novel fluoroalkyl-containing tropane derivatives was synthesized, and their binding affinities for the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET) were determined via competitive binding assays. Among these derivatives, the fluoropropyl ester of beta-CIT (19), the fluoroethyl ester of beta-CIT (20), the N-fluoropropyl derivative of beta-CBT (12), and the fluoropropyl ester of beta-CMT (18) displayed higher affinity and greater selectivity for the DAT versus SERT and NET than FP-CIT, which indicates that they are attractive candidates for the development of (18)F-labeled PET imaging agents for the DAT. |
| Databáze: | OpenAIRE |
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