Capromorelin, a member of the growthhormonesecretagogue (GHS) class of drugs, is a ghrelin receptor agonist and a novel therapy for stimulation of appetite in dogs with Ki value of 7 nM for hGHS-R1a and EC50 value of 3 nM for rat pituicyte. Capromorelin
PF-04628935 is a potent antagonist inverse agonist of the ghrelin receptor, growthhormonesecretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. PF-04628935 is orally bioavailable and brain penetrant.
BMS-317180 is a potent, novel, orally effective growthhormonesecretagogue (GHS) that shows an excellent safety profile in preclinical studies. The compound was advanced into clinical development.
AZ-GHS-22 is an inverse agonist of the growthhormonesecretagogue receptor 1a (GHS-R1a), which is also known as the ghrelin receptor.1It binds to GHS-R1a with an IC50value of 0.77 nM. AZ-GHS-22 decreases food intake in mice by 54% in the first two hours after administration of a 100 mg/kg dose. 1.McCoull, W., Barton, P., Brown, A.J.H., et al.Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonistsJ. Med. Chem.57(14)6128-6140(2014)
Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin growthhormonesecretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growthhormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for its potential applications in research related to cachexia, gastroparesis, and gastric intestinal dysmobility disorders [4] [5].