LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with K i s of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders.
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