Pramipexole is a partial/full D2S, D2L, D3, D4, receptor agonist with a Ki of 3.9, 2.2, 0.5, 5.1 nM. It also possesses low/insignificant affinity (500-10,000 nM) for the 5-HT1A, 5-HT1B, 5-HT1D, and α2-adrenergic receptors. It has negligible affinity (>10,000 nM) for the D1, D5, 5-HT2, α1-adrenergic, β-adrenergic, H1, and mACh receptors. It is a non-ergoline dopamine agonist indicated for treating early-stage Parkinson’s disease (PD) and restless legs syndrome (RLS).
| Molecular Weight | 302.26 |
| Formula | C10H17N3S.2HCl.H2O |
| CAS Number | 191217-81-9 |
| Solubility (25°C) | DMSO 40 mg/mL Water 60 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.
[3] Marta Łaszcz, et al. Stability studies and structural characterization of pramipexole
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