A 331440 dihydrochloride is a high affinity histamine H3 receptor antagonist (Ki values are 21.7 and 22.7 nM for rat and human H3 receptors, respectively). Exhibits selectivity for human H3 over H1, H2 and H4 receptors (Ki values are 2940, 14400 and >10000 nM respectively). Shown to reduce weight in a diet-induced obesity model.
Molecular Weight | 422.39 |
Formula | C22H27N3O.2HCl |
CAS Number | 1049740-32-0 |
Solubility (25°C) | DMSO 8.45 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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