LML134

LML134 is an orally active, highly selective small molecule inverse agonist of the histamine H3 receptor (H3R). It was developed by Novartis for the treatment of excessive sleepiness associated with sleep disorders such as shift work disorder and circadian rhythm sleep disorders. The compound demonstrates high affinity for the human H3 receptor and was designed to achieve rapid brain penetration and strong wakefulness-promoting effects while minimizing insomnia as a side effect. Clinical trials showed that LML134 reduced night-time sleepiness in shift workers compared to placebo and was generally well tolerated; however, development was discontinued after phase II trials due to business reasons[1][2][3][4][5][7].

Other names

1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate