Pridopidine

Pridopidine is a ligand of sigma non-opioid intracellular receptor 1 (σ₁ receptor) and a dopaminergic stabilizer.^1,2 It binds to the σ₁ receptor and dopamine D₂ receptor in the high-affinity state (K_is = 81.3 and 7,521 nM, respectively). Pridopidine (100 µmol/kg) increases striatal 3,4-dihydroxyphenylacetic acid (DOPAC) levels and locomotor activity, as well as inhibits amphetamine-induced locomotor activity, in rats.² It improves motor function and reduces striatal mutant huntingtin (mHtt) aggregates in the R6/2 mouse model of Huntington’s disease when administered at doses of 5 or 6 mg/kg.³ Pridopidine (30 mg/kg) prevents muscle atrophy and the loss of innervated neuromuscular junctions in the SOD1-G93A mouse model of amyotrophic lateral sclerosis (ALS).⁴

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1. Sahlholm, K., Århem, P., Fuxe, K., et al. The dopamine stabilizers ACR16 and (–)-OSU6162 display nanomolar affinities at the σ-1 receptor. Mol. Psychiatry 18(1), 12-14 (2013).

2. Pettersson, F., Pontén, H., Waters, N., et al. Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D₂ receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16). J. Med. Chem. 53(6), 2510-2520 (2013).

3. Squitieri, F., Di Pardo, A., Favellato, M., et al. Pridopidine, a dopamine stabilizer, improves motor performance and shows neuroprotective effects in Huntington disease R6/2 mouse model. J. Cell. Mol. Med. 19(11), 2540-2548 (2015).

4. Ionescu, A., Gradus, T., Altman, T., et al. Targeting the sigma-1 receptor via pridopidine ameliorates central features of ALS pathology in a SOD1G93A model. Cell Death Dis. 10(3), 210 (2019).