Pharmacological Properties of DOV 315,090, an Ocinaplon Metabolite
Author Information
Author(s): Berezhnoy Dmytro, Gravielle Maria C, Downing Scott, Kostakis Emmanuel, Basile Anthony S, Skolnick Phil, Gibbs Terrell T, Farb David H
Primary Institution: Boston University School of Medicine
Hypothesis
The pharmacological properties of ocinaplon in vivo might be influenced by an active biotransformation product with greater selectivity for the α2 subunit relative to α1.
Conclusion
DOV 315,090 could contribute to the action of ocinaplon in vivo, but the anxioselective properties of ocinaplon cannot be readily explained by a subtype selective effect of DOV 315,090.
Supporting Evidence
- DOV 315,090 appears rapidly in plasma following administration of ocinaplon.
- DOV 315,090 possesses modulatory activity at GABAA-Rs.
- The selectivity profile of DOV 315,090 is similar to that of ocinaplon.
Takeaway
This study looked at how a drug called DOV 315,090, which comes from another drug called ocinaplon, works in the body. It found that DOV 315,090 helps with anxiety but doesn't work in a way that makes it better than ocinaplon.
Methodology
The pharmacological properties of DOV 315,090 were assessed using radioligand binding studies and two-electrode voltage clamp electrophysiology.
Limitations
The study was conducted in heterologous expression systems, which may lack certain modulatory proteins or regulatory mechanisms present in neurons.
Digital Object Identifier (DOI)
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