(S)-Pramipexole (hydrochloride)

(S)-Pramipexole is a dopamine D_2S, D_2L, 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 α_2A-adrenergic receptors (α_2A-ARs; EC₅₀ = 3,548.13 nM). (S)-Pramipexole is selective for dopamine D_2-4 receptors (K_is = 954.99, 1,698.24, 12.59, 128.82 nM for for D_2S, D_2L, D₃, and D₄ receptors, respectively, in a radioligand binding assay) over D₁ and D₅ receptors (K_is = >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.

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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-adrenoceptor. J. 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 subtypes. J. 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 primates. J. Neurochem. 96(5), 1315-1321 (2006).