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CVN417 is an orally active antagonist of nAChR containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. It inhibits Ca(2+) efflux through nAChR subunits, displaying IC50 values of 0.086 μM (α6), 2.56 μM (α3), and 0.657 μM (α4). CVN417 has shown efficacy in reducing resting tremor in rodent models, suggesting a potential to ameliorate movement disorders in conditions like Parkinson's disease [1].
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Description | CVN417 is an orally active antagonist of nAChR containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. It inhibits Ca(2+) efflux through nAChR subunits, displaying IC50 values of 0.086 μM (α6), 2.56 μM (α3), and 0.657 μM (α4). CVN417 has shown efficacy in reducing resting tremor in rodent models, suggesting a potential to ameliorate movement disorders in conditions like Parkinson's disease [1]. |
In vitro | CVN417 (10 μM; 0-2 h) exhibits lower metabolic turnover in human liver microsomes or hepatocytes [1]. In vitro ADME data for CVN417 [1] show intrinsic clearance rates (Cl int) in human liver microsomes of 2.8 μL/min/mg, in rat 31.2, mouse 33.3, and dog 27.7; and in hepatocytes (mL/min/10^6 cells) in human 3.7, rat 20.8, mouse 25.1, and dog 32.3. |
Storage | Shipping with blue ice. |
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