Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.
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Ben-Daniel R, Deuther-Conrad W, Scheunemann M, Steinbach J, Brust P, Mishani E
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.
Bioorg Med Chem. 2008 Jun 15;16(12):6364-70. doi: 10.1016/j.bmc.2008.05.006. Epub 2008 May 7.
- PubMed ID
- 18487050 [ View in PubMed]
- Abstract
The synthesis and structure-activity relationship of a new class of indole derivatives with low-nanomolar affinity for the SERT and high selectivity versus the 5-HT1A receptor were recently reported. Based on their chemical structure, four new indolylpropylamine derivatives which contain atoms to afford future labeling with PET isotopes, were synthesized and evaluated as SERT ligands. The chemistry of these novel derivatives, their biological evaluation, the general method of preparing the precursor indole for labeling, and the C-11 labeling of the most promising indole derivative, are described herein.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Citalopram Sodium-dependent serotonin transporter Ki (nM) 4.38 N/A N/A Details Citalopram Sodium-dependent serotonin transporter Ki (nM) 32.8 N/A N/A Details Midomafetamine Sodium-dependent serotonin transporter Ki (nM) 0.73 N/A N/A Details Midomafetamine Sodium-dependent serotonin transporter Ki (nM) 2.03 N/A N/A Details Paroxetine Sodium-dependent serotonin transporter Ki (nM) 0.42 N/A N/A Details Paroxetine Sodium-dependent serotonin transporter Ki (nM) 0.38 N/A N/A Details