Amitriptyline (MK-230, N-750, Ro41575) is an inhibitor of the serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki values of 3.45 nM and 13.3 nM, respectively, and also inhibits the histamine receptor H1, the histamine receptor H4, 5-HT2, and the Sigma 1 receptor with Ki values of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. It can also inhibit histamine receptor H1, histamine receptor H4, 5-HT2 and Sigma 1 receptor with Ki values of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively, and can be used in studies of depression and neuropathic pain.
| Molecular Weight | 277.4 |
| Formula | C20H23N |
| CAS Number | 50-48-6 |
| 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.
[1] Elliot W McClure, et al. ACS Chem Neurosci. Classics in Chemical Neuroscience: Amitriptyline
[3] No authors listed. Nurs Times. Amitriptyline and nortriptyline
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