ghs-r1a

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).

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。

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。

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。

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

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.

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].

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)。

orally active ghrelin receptor (GHS-R1a) agonist

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

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)

LEAP-2 (Human liver expressed antimicrobial peptide-2) 是一种抗菌肽，是生长素释放肽的内源性竞争性拮抗剂，也是组成型 GHS-R1a 活性的反向激动剂，可用于研究肥胖和其他代谢疾病。

An endogenous ligand for the ghrelin receptor (GHS-R1a), produced by alternative splicing of the rat ghrelin gene. Potently induces Ca2+ release in cells expressing ghrelin receptors (EC50 = 2.4 nM) and stimulates GH release in vivo.