ghsr

L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist and benzolactam derivative, known for reversing glucocorticoid-induced inhibition of GH secretion. L-692429 exhibits high affinity for the G protein-coupled receptor and is useful in studying acromegaly and obesity.

Relamorelin(BIM28131, RM131) is a selective and potent ghrelin/growth hormone secretagogue receptor (GHSR) agonist with high affinity for GHS-1a receptor (Ki value is 0.42 ± 0.063 nM). Relamorelin(BIM28131, RM131) is also a centrally permeable pentapeptide analog that can increase growth hormone levels and accelerate gastric emptying, and has the potential to study cachexia.

Anamorelin (ONO-7643) is a novel ghrelin receptor agonist (EC50: 0.74 nM in the FLIPR assay).

Ibutamoren Mesylate (MK-0677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.

Obestatin (rat) acetate is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin (rat) acetate has anti-inflammatory, anti-myocardial infarction and antioxidant properties. Obestatin (rat) acetate suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain.

PF-5190457 is an effective and selective ghrelin receptor inverse agonist (pKi: 8.36).

TM-N1324 is a GPR39 agonist. TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn2+, respectively. TM-N1324 has similar potencies to murine GPR39 with EC50s of 180 nM and 5 nM, respectively.

TC-G-1008 (GPR39-C3) is a zinc receptor agonist with EC50 values of 0.4 nM for rat GPR39 and 0.8 nM for human GPR39.

AnaMorelin hydrochloride (RC-1291 hydrochloride) is a novel ghrelin receptor agonist(EC50 : 0.74 nM, in the FLIPR assay).

Capromorelin Tartrate (CP 424391-18) is a potent, orally active growth hormone secretagogue receptor (GHSR) agonist (Ki: 7 nM for hGHS-R1a).

GHSR-1a agonist-1 (Compound 4b) is an orally active agonist of the human growth hormone secretagogue receptor 1a (GHSR-1a) with an EC50 of 0.49 nM. It effectively stimulates the release of endogenous growth hormone by activating GHSR-1a. Doses as low as 0.1 mg/kg (administered orally) can increase body weight and length in 4-week-old rats. GHSR-1a agonist-1 is applicable in research on pediatric growth and developmental delays.

EX-1314 (BMS-604992) is a growth hormone secretagogue receptor (GHSR) agonist.

BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Additionally, BMS-604992 dihydrochloride stimulates food intake in rodents.

Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin/growth hormone secretagogue 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 growth hormone 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].

BMS-604992 (EX-1314) free base is a selective, orally active, small-molecule growth hormone secretagogue receptor (GHSR) agonist with high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM), capable of stimulating food intake in rodents.

Macimorelin acetate is an orally active agonist of the GHSR (Growth Hormone Secretagogue Receptor) and functions as a growth hormone (GH) secretagogue. As a ghrelin mimetic, it potently stimulates the release of endogenous growth hormone by binding to GHSR. Macimorelin acetate is clinically utilized as a diagnostic tool for Adult Growth Hormone Deficiency (AGHD) and is being investigated for the treatment of Cancer Anorexia-Cachexia Syndrome (CACS). Additionally, it has shown potential in neurological research for suppressing seizure activity.

Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a potent and selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR), exhibiting a K_i of 0.42 nM for the GHS-1a receptor. This compound can cross the blood-brain barrier and effectively increases growth hormone levels while promoting faster gastric emptying, showing significant research potential for conditions such as cachexia, gastroparesis, and disorders related to gastric/intestinal motility [1] [2] [3] [4] [5].

GHRF, porcine, a growth hormone releasing factor (GHRF) peptide (porcine), binds to the growth hormone secretagogue receptor (GHSR), thereby inducing the release of growth hormone [1] [2].

Anamorelin Fumarate is a novel ghrelin receptor agonist (EC50: 0.74 nM in the FLIPR assay).

JMV 2959 hydrochloride (925238-89-7 free base) is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells.

JMV 2959 is an antagonist of growth hormone secretagogue receptor type 1a (GHS-R1a) (IC50: 32 nM).

Ulimorelin is a ghrelin receptor agonist (EC50: 29 nM and a Ki of 16 nM). Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors.

Substituted piperidines-1 can promote the release of growth hormone in humans and animals.

Ibutamoren (MK-677) is a drug which acts as a potent, orally active growth hormone secretagogue, mimicking the GH stimulating action of the endogenous hormone ghrelin. It also alters the metabolism of body fat and so may have an application in the treatment of obesity.