ghrelin receptor

Anamorelin (ONO-7643) 是新型ghrelin receptor 激动剂，根据FLIPR 检测，得到其EC50=0.74 nM。

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

PF-5190457 是具有选择性的、有效的生长素释放肽受体选择性的反向激动剂(pKi:8.36)。

AnaMorelin hydrochloride (RC-1291 hydrochloride) 是生长素受体激动剂，根据 FLIPR 检测，得到 EC50=0.74 nM。

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

Relamorelin(BIM28131, RM131) 是一种具有选择性和有效性的生长素释放肽 生长激素促分泌素受体 (GHSR) 激动剂，对 GHS-1a 受体具有很高的亲和力（Ki值为0.42 ± 0.063 nM）。Relamorelin(BIM28131, RM131) 也是一种具有中枢渗透性的五肽类似物，可增加生长激素水平，加速胃排空，具有研究恶病质的潜力。

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.

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是一种选择性ghrelin 受体拮抗剂(GHS-R1a) (Ki = 17 nM))，对运动素受体显示出较弱的亲和力(K = 6 μ M)。YIL 781通过阻断胃饥饿素分泌对体内和体外胰岛素分泌改善体内葡萄糖稳态。

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.

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)

Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. 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 as much as 98% in rats. JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 μg kg.

AZ-GHS-22 is an inverse agonist of the growth hormone secretagogue 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 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].

Macimorelin (EP-1572) acetate，一种 GH 促分泌素，是一种具有口服活性的GHSR 激动剂。Macimorelin acetate 可刺激 GH 的释放。Macimorelin acetate 可用于成人生长激素缺乏症 (AGHD) 和癌症厌食-恶病质综合征 (CACS) 的研究。

TZP-102 is a potent, oral, ghrelin receptor agonist that has been shown to improve diabetic gastroparesis symptoms.

Relamorelin (RM-131) TFA，一种生长素类似物，是一种选择性的生长素释放肽 生长激素促分泌素受体 (GHSR) 激动剂，对GHS-1a 受体的Ki 值为 0.42 nM。Relamorelin TFA 是一种五肽，具有中枢渗透性。Relamorelin TFA 增加生长激素水平，加速胃排空，具有用于恶病质、胃轻瘫和胃 肠运动障碍研究的潜力。