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Synthesis, biological evaluation, and molecular modeling of ORM-10921 and its analogs as α -adrenoceptor antagonists. | LitMetric

The α -adrenoceptor (α -AR) is regarded as one of the potential targets for antipsychotics. A few of structurally diverse α -AR antagonists have been reported, among which ORM-10921, containing one rigid tetracyclic framework with two neighboring chiral centers, has exhibited remarkable antipsychotic-like effects and pro-cognitive properties in different animal models. Yet the binding mode of ORM-10921 remains elusive. In this study, all of its four stereoisomers and a set of its analogs were synthesized and in vitro evaluated for their α -AR antagonist activities. The molecular docking study and hydration site analysis gave a rational explanation for the biological results, which might provide helpful insights into the binding mode and future optimization.

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http://dx.doi.org/10.1002/ardp.202300125DOI Listing

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