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The calculated maximal brain concentration of [11C]AF150 S) of 2.9 nM remained approximately 70 times below the K d,H (200 nM), of AF150(S) for M1ACh-R, under baseline conditions.
The same holds true for SNT207858, i.e. the maximal brain concentration is about 110 nM [22], and thus, considering the IC50s of 22 nM (binding) and 11 nM (function), above the concentration required for central effects (Table 1).
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However, maximal brain concentrations of the active compound DB75 were very low (13 nmol/mg of tissue at 24 h).
The plasma concentration was significantly correlated with the brain concentration.
unbound brain concentration.
total brain concentration.
total brain concentration of the drug.
Youth athletes are at increased risk due to maximal brain plasticity during development [7].
Brain uptake of [11C]oseltamivr was evaluated by its normalized brain concentration, brain-to-plasma concentration ratio, and plasma-to-brain transfer rate.
The tarenflurbil brain concentration was 1.3μM.
87 Only after increasing the systemically administered dose of bumetanide by nearly two orders of magnitude, could brain concentrations in the range of the half maximal inhibition constant of NKCC1 be briefly reached.
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