Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 5, Pages 1482-1486Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm701357m
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Funding
- NCRR NIH HHS [C06 RR14503, P20 RR021929] Funding Source: Medline
- NIDA NIH HHS [DA011979, DA013978, DA023205] Funding Source: Medline
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Cocaine's toxicity can be mitigated by blocking its interaction with sigma-1 receptors. The involvement of sigma-2 receptors remains unclear. To investigate their potential role, we have designed compounds through a convergent synthesis utilizing a highly selective sigma-1 ligand and elements of a selective sigma-2 ligand. Among the synthesized compounds was produced a subnanomolar sigma-2 ligand with an 11-fold preference over sigma-1 receptors. These compounds may be useful in developing effective pharmacotherapies for cocaine toxicity.
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