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S221237 is a small molecule antagonist of the G protein-coupled receptor 37 (GPR37), also known as the Parkin-associated endothelin receptor-like receptor (PAELR). Developed by Servier, the compound is being investigated for the treatment of Parkinson's disease. GPR37 is a G protein-coupled receptor that is highly expressed in the brain, particularly in dopaminergic neurons of the substantia nigra. The accumulation of misfolded GPR37 is a characteristic feature of certain forms of Parkinson's disease, and its signaling is thought to contribute to neuronal death. By blocking GPR37, S221237 aims to provide neuroprotection and potentially slow disease progression. The drug has undergone Phase 1 clinical evaluation to assess its safety, tolerability, and pharmacokinetics in both healthy volunteers and patients with Parkinson's disease.
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