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Riminkefon is a potent, non-peptide, orally active antagonist of neurotensin receptors, specifically targeting both neurotensin receptor 1 (NTR1) and neurotensin receptor 2 (NTR2). Developed by Sanofi, it was designed to block the biological effects of the neuropeptide neurotensin, which is involved in the regulation of dopaminergic transmission and various central nervous system functions. Unlike its predecessor meclinertant, which is highly selective for NTR1, riminkefon exhibits high affinity for both receptor subtypes, providing a more comprehensive blockade of neurotensin signaling. It was primarily investigated for the treatment of psychiatric and neurological conditions, including schizophrenia and Parkinson's disease, due to its ability to modulate dopamine release and neurotensin-induced behavioral effects in preclinical models. However, clinical development was ultimately discontinued.
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