Darifenacin is a selective M3 muscarinic receptor antagonist with pKi of 8.9. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 µM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6.
In vivo Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50-55%. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
|Related AChR/AChE Products|
|Scopolamine hydrobromide trihydrate
Scopolamine hydrobromide trihydrate is a competitive muscarinic acetylcholine receptor with an IC50 of 55.3 ± 4.3 nM.
Choline Glycerophosphate is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue.
MK-7622 is a cholinesterase inhibitor, it is also a muscarinic M1 receptor positive allosteric modulator.
Acotiamide is a potent, selective and reversible inhibitor of human and canine stomach-derived acetylcholinesterase (AChE).
Huperzine A is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor extracted from traditional Chinese herb.
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