SAR110068

SAR110068 is a **potent, selective, and orally bioavailable small molecule antagonist/inverse agonist of the histamine H3 receptor**. Originally developed by **Sanofi**, it was designed for the treatment of **sleep–wake disorders** such as **narcolepsy**. The compound acts by blocking the histamine H3 receptor (H3R), which modulates the release of various neurotransmitters (including acetylcholine, noradrenaline, dopamine, GABA, and serotonin) in the central nervous system. SAR110068 demonstrated **high affinity and selectivity for H3R** and produced **awakening effects in preclinical models**. However, development of SAR110068 for narcolepsy has been **discontinued**.[1][3]