AZ12807110

AZ12807110 (also known as [11C]GSK189254) is a radiolabeled small molecule that acts as a highly selective antagonist and inverse agonist of the histamine H3 receptor. Developed by AstraZeneca and originally identified by GSK, the compound is primarily utilized as a positron emission tomography (PET) radioligand. Its high affinity and selectivity for the H3 receptor make it an effective tool for imaging the distribution of these receptors in the central nervous system and for conducting receptor occupancy studies. In clinical development, it has been used to evaluate the pharmacodynamic profiles of therapeutic H3 receptor antagonists, such as AZD5213, by measuring their ability to displace the radioligand from brain regions. This quantification helps researchers determine optimal dosing regimens that balance daytime efficacy with the avoidance of nocturnal sleep disruption in conditions like cognitive disorders and sleep-wake regulation.

Other names

[11C]AZ12807110[11C]GSK18925411C-GSK189254