gsk239512

GSK239512 is a potent and selective small molecule antagonist/inverse agonist of the histamine H3 receptor. It was developed by GSK as an orally active investigational therapy for cognitive dysfunction in neurodegenerative and neuropsychiatric disorders, including Alzheimer's disease, multiple sclerosis, and schizophrenia. The drug acts by blocking the histamine H3 receptor, which plays a role in negative neuromodulation of neurotransmitters involved in cognition. Clinical trials reached up to phase II but were discontinued globally around 2017 due to lack of sufficient efficacy or strategic reasons[1][4][5][6].

Other names

1-(6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)oxy)pyridin-3-yl)pyrrolidin-2-one