ghrelin receptor

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

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

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

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

Ghrelin receptor full agonist-3 (Compound 22) is a selective, potent, orally active full agonist of the growth hormone secretagogue receptor (ghrelin receptor) with an EC50 value of 1.8 nM. It stimulates pulsatile secretion of growth hormone (GH), significantly increasing both the frequency and duration of GH release, thereby inducing a sustained rise in insulin-like growth factor-1 (IGF-1) levels. This compound is applicable for research in oncology and chronic obstructive pulmonary disease.

Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist.

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.

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.

KARI 201 is a selective, brain-penetrant, competitive inhibitor of acid sphingomyelinase (ASM) with an IC50 of 338.3 nM. Additionally, KARI 201 acts as an agonist of the growth hormone secretagogue receptor (ghrelin receptor). It is capable of improving the neuropathological characteristics of Alzheimer's disease.

KARI 201 hydrochloride is a selective, brain-penetrant, competitive inhibitor of acid sphingomyelinase (ASM) with an IC50 of 338.3 nM. It also acts as an agonist for the growth hormone-releasing peptide receptor (ghrelin receptor). Additionally, KARI 201 hydrochloride can enhance the neuropathological features of Alzheimer's disease.

(S)-PF-5190457 ((S)-PF-05190457) is the S-enantiomer of PF-5190457. PF-5190457 (PF-05190457) acts as an effective and selective inverse agonist of the growth hormone secretagogue receptor (ghrelin receptor), with a pKi of 8.36.

Capromorelin, a member of the growth hormone secretagogue (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

ghrelin receptor (GHS-R1a) agonist

orally active ghrelin receptor (GHS-R1a) agonist

YIL 781 is a selective ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM), showing a weak affinity for kinesin receptors (K = 6 μM). YIL 781 improves glucose homeostasis in vivo and in vitro by blocking ghrelin secretion.

GSK 894281 is a ghrelin receptor agonist. It may produces myocardial degeneration/necrosis in rats.

GSK1614343 is an antagonist of ghrelin receptor.

GSK-894490A is an agonist of ghrelin receptor. GSK-894490A crosses the blood/brain barrier and elicit pro-cognitive effects.

PF-04628935 is a potent antagonist/inverse agonist of the ghrelin receptor, growth hormone secretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. PF-04628935 is orally bioavailable and brain penetrant.

SM-130,686 is a potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue. It has around half the potency of the endogenous agonist ghrelin as a stimulator of growth hormone release.

Tabimorelin is a potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue.

YIL781 is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM) with no significant affinity for the motilin receptor (Ki = 6 μM).

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. At 80 μg/kg, JMV3002 inhibits hexarelin-stimulated food intake by up to 98% in rats. It does not induce growth hormone release nor inhibit hexarelin-stimulated growth hormone secretion at a dose of 160 μg/kg in infant rats.