Mechanism of action: Growth hormone secretagogue receptor type 1a (GHS-R1a) inverse agonist; ghrelin receptor inverse agonist

Preclinical pharmacology

AZ12861903 is a high affinity inverse agonist of GHS-R1a with binding IC50 values of 6.7nM and 39nM against human and mouse receptors respectively. AZ12861903 has good oral exposure and CNS exposure has been measured in rodent (free brain:plasma = 0.42 and 1.3in mouse and rat respectively).

Treatment with AZ12861903 in vivo reduced acute (6 h) food intake in free feeding mice in line with free target coverage in brain. This effect was shown to be mediated by GHS-R1a since null (KO) mice showed no significant feed intake reduction when dosed with AZ12861903.

Additional Information

Clinical Trials for this compound

See all of the Clinical Trials currently associated with this compound:

Journal of Medicinal Chemistry

Identification, Optimization, and Pharmacology of Acylurea GHS-R1a Inverse Agonists

Gene information from the NCBi

This compound works on the following genes: