Abstract
A series of 3α-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes was synthesized and the binding affinities of the compounds were determined at the dopamine transporter. The unsubstituted analogue 7b (Ki=98 nM) was the most potent compound of the series with binding affinity three-times greater than cocaine and only 5-fold less than GBR-12909. The structure-activity data for 7a-f suggests that these compounds may be binding at the dopamine transporter in a similar fashion to GBR 12909.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 2387-2390 |
| Number of pages | 4 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 12 |
| Issue number | 17 |
| DOIs | |
| State | Published - Sep 2 2002 |
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry
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Bradley, A. L., Izenwasser, S., Wade, D., Klein-Stevens, C., Zhu, N., & Trudell, M. L. (2002). Synthesis and dopamine transporter binding affinities of 3α-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes. Bioorganic and Medicinal Chemistry Letters, 12(17), 2387-2390. https://doi.org/10.1016/S0960-894X(02)00464-X