Linopirdine dihydrochloride is a blocker of KV7 (KCNQ) voltage-gated potassium channels; blocks KV7.1 + 7.3 (KCNQ2 + 3) / M-currents (IC50 = 4 - 7 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 8.9 μM). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo.
Molecular Weight | 464.39 |
Formula | C26H21N3O.2HCl |
CAS Number | 113168-57-3 |
Solubility (25°C) | Water 40 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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