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Derivation of equations for deriving functional parameters from whole cell binding assay Taking note of the definitions of EC 50 values for various receptor species (AR, RB, ARB), we can rearrange the above equation (8) for fractional receptor occupancy by a properly labeled and detectable (e.g., radioactive or fluorescent) agonist as follows: where, EC 50 values are efficacy-corrected potency and defined as key geometric descriptors 5 : Similarly, solving equation (9), fractional receptor occupancy by a properly labeled modulator is Finally, solving equation (10), fractional receptor occupancy by both agonist and modulator is The above rearranged equations (16, 17, 18) suggest that a properly designed dose combination matrix-dependent receptor binding assay with functional whole cells may be able to allow reliable determination of EC 50 values for all bound receptor species (AR, RB, ARB)

Results: The estimated geometric mean t1/2F in uninduced adults was 40.0 hours versus the expected elimination half-life of 1216 hours in this population (including patients on valproic acid monotherapy)

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