growth hormone secretagogue receptor

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

Ibutamoren Mesylate (MK-0677) 是非肽段类生长激素促分泌素受体 (GHSR) 激动剂，也是一种口服有活性的生长激素 (GH) 促分泌素。

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)。

TM-N1324 是一种 GPR39 激动剂。 TM-N1324 在没有和存在 Zn2+ 的情况下分别以 280 nM 和 9 nM 的高效率和效力激活人 GPR39。 TM-N1324 对鼠 GPR39 表现出相似的效力，EC50 分别为 180 nM 和 5 nM。

TC-G-1008 (GPR39-C3) 是一种口服有活性的 GPR39激动剂，可作用于大鼠受体(EC50: 0.4 nM)和人类受体(EC50:0.8 nM)的。

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。

Capromorelin Tartrate (CP 424391-18) 是口服有活性的 growth hormone secretagogue receptor 有效激动剂，能够作用于 hGHS-R1a(Ki:7 nM)。

L-692429 (MK-0751) 是一种有效的非肽基生长激素促分泌素 (GHS) 激动剂，是一种苯并内酰胺的衍生物，可逆转糖皮质激素对 GH 分泌的抑制。L-692429 对 G 蛋白偶联受体 (G protein-coupled receptor)具有很高的亲和力，可用于研究肢端肥大症和肥胖。

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。

JMV 2959 hydrochloride (925238-89-7 free base) 是一种生长激素促分泌素受体 1a 型 (GHS-R1a) 拮抗剂，在 LLC-PK1 细胞中的 IC50 为 32±3 nM。

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

GHSR-1a agonist-1 (Compound 4b) 是一种口服有效的人源生长激素促分泌素受体 1a (GHSR-1a) 激动剂，EC50为 0.49 nM。通过激活 GHSR-1a，GHSR-1a agonist-1 能有效刺激内源性生长激素的释放。GHSR-1a agonist-1 以低至 0.1 mg/kg 的剂量（口服）即可增加 4 周龄大鼠的体重和体长，适用于儿童生长发育迟缓领域的研究。

KARI 201 是一种竞争性和选择性的酸性鞘磷脂酶 (ASM) 抑制剂，IC50为 338.3 nM，并具有良好的脑渗透性。同时，KARI 201 也是生长素释放肽受体 (ghrelin receptor) 的激动剂。该化合物能够改善与阿尔茨海默病相关的神经病理特征。

Ghrelin receptor full agonist-3 (Compound 22) 是一种选择性且具口服活性的强效生长激素释放肽受体完全激动剂，其EC50为1.8 nM。该化合物能够刺激生长激素（GH）的脉冲式分泌，显著增加生长激素分泌的频率和持续时间，进而引发胰岛素样生长因子-1 (IGF-1) 水平持续升高。该化合物可用于癌症及慢性阻塞性肺疾病的研究。

AZ-GHS-38 (compound 38) 是一种能被口服吸收且能穿过血脑屏障的生长激素促分泌素受体 (GHS-R1a) 反向激动剂，IC50为6.7 nM。AZ-GHS-38 能够减少正常小鼠的急性食物摄入量，并可用于抗肥胖研究。

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

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.

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

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)

BMS-604992 (EX-1314) dihydrochloride is a selective and 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). Furthermore, BMS-604992 dihydrochloride has been shown to stimulate 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. It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Moreover, BMS-604992 free base has the ability to stimulate food intake in rodents.