(S)-Pramipexole-d5 is intended for use as an internal standard for the quantification of (S)-pramipexole by GC- or LC-MS. (S)-Pramipexole is a dopamine D2S, D2L, D3, and D4 receptor agonist (EC50s = 426.58, 338.84, 2.24, and 128.82 nM, respectively, in a [35S]GTPγS binding assay).1 It is also a partial agonist of α2A-adrenergic receptors (α2A-ARs; EC50 = 3,548.13 nM). (S)-Pramipexole is selective for dopamine D2-4 receptors (Kis = 954.99, 1,698.24, 12.59, 128.82 nM for D2S, D2L, D3, and D4 receptors, respectively, in a radioligand binding assay) over D1 and D5 receptors (Kis = >10,000 nM for both).2 It prevents MPTP-induced decreases in the number of dopaminergic neurons in the substantia nigra pars compacta in common marmosets when administered at a dose of 60 μg/kg per day before, during, and after administration of MPTP.3 Formulations containing (S)-pramipexole have been used in the treatment of Parkinson's disease and restless legs syndrome.
1.Newman-Tancredi, A., Cussac, D., Audinot, V., et al.Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D2-like receptor and α1/α2-adrenoceptorJ. Pharmacol. Exp. Ther.303(2)805-814(2002) 2.Millan, M.J., Maiofiss, L., Cussac, D., et al.Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypesJ. Pharmacol. Exp. Ther.303(2)791-804(2002) 3.Iravani, M.M., Haddon, C.O., Cooper, J.M., et al.Pramipexole protects against MPTP toxicity in non-human primatesJ. Neurochem.96(5)1315-1321(2006)