azd5213

AZD5213 is a potent, selective, and competitive small molecule antagonist (inverse agonist) of the human histamine H3 receptor. Developed by AstraZeneca, it was designed to achieve a pharmacokinetic profile that allows for circadian fluctuations in H3 receptor occupancy, potentially reducing sleep disruption while maintaining daytime efficacy. In preclinical studies, AZD5213 increased the release of neurotransmitters such as histamine, acetylcholine, dopamine, and norepinephrine in the brain. It demonstrated efficacy in rodent models of cognition and neuropathic pain. Clinically, it was investigated for neurological disorders including Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), diabetic neuropathies (painful diabetic neuropathy), mild cognitive impairment, and Tourette's syndrome. The drug showed dose-dependent H3 receptor occupancy with rapid absorption and a short half-life (~5–7 hours). Development has been discontinued for all indications[1][2][5][6][7].

Other names

AZD-5213AZD5213AZD 5213