MK-0249

MK-0249 is a potent, selective, and orally active small molecule antagonist (inverse agonist) of the histamine H3 receptor. It was developed for the treatment of cognitive deficits and disorders such as Alzheimer's disease, schizophrenia, attention-deficit/hyperactivity disorder (ADHD), sleep apnea syndromes, excessive daytime sleepiness, and hypopnea syndrome. The drug demonstrated high affinity for the human H3 receptor (IC50 = 1.7 nM) and showed promising preclinical results in models of cognitive impairment[1][4][5][8]. Despite initial promise in phase I/II clinical trials for several neuropsychiatric indications—including Alzheimer's disease, ADHD, schizophrenia, obesity, and sleep apnea—MK‑0249 failed to demonstrate sufficient efficacy in these conditions. As a result, further development was discontinued[2][3][4][6][7].

Other names

1167574-41-5862309-06-6