Tadalafil (Cialis) is a PDE inhibitor. Tadalafil (Cialis), which has demonstrated a high level of selectivity for PDE5 over the other phosphodiesterases, has shown efficacy in improving erectile function and sexual satisfaction in phase III trials. PDE11A3, PDE11A2, and PDE11A1, which contain progressively shorter N-termini, were more sensitive than PDE11A4 to inhibition by Tadalafil (Cialis).
|Animal models||Sham-operated rats|
|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 48 mg/mL|
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CP671305 is a potent and selective, orally active inhibitor of phosphodiesterase-4-D with high activities.
ITI-214 phosphate is an orally active, potent and selective inhibitors of PDE1, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
IBMX is a pDE inhibitor (non-selective) with IC50 values of 6.5±1.2, 26.3±3.9 and 31.7±5.3 μM for PDE3, 4 and 5 respectively.
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