antagonist g

Antagonist G is an anticancer peptide and is also a broad spectrum neuropeptide growth factor antagonist.

G-Protein antagonist peptide acetate 是一种 substance P 相关肽，可抑制 G 蛋白与其受体的结合。G-Protein antagonist peptide acetate 竞争性和可逆性地抑制毒蕈碱型乙酰胆碱受体 M2 (M2 muscarinic receptor) 对 Gi 或 Go 的激活，并通过 β-肾上腺素受体抑制 Gs 的激活。

Antagonist G TFA 作为后叶加压素（vasopressin）的有效拮抗剂，同时对GRP和缓激肽具有弱拮抗作用。此外，Antagonist G 能够诱导AG-1转录，增强癌细胞对化疗的敏感性。

Substance P-related peptide that inhibits binding of G proteins to their receptors. Competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

A 779 是一种 G 蛋白偶联受体 Mas 的有效拮抗剂，Mas 受体是Ang1-7 receptor，与传统的AngII 不同。

Proadrenomedullin N-terminal 12 peptide (PAMP-12) 是一种内源性肽段，源自人体肾上腺髓质，对应人类PAMP-20的9-20氨基酸，涉及降低血压。它是MAS相关G蛋白偶联受体家族成员X2 (MRGPRX2) 的激动剂。在表达人MRGPRX2的CHO细胞中，PAMP-12抑制forskolin诱导的cAMP积累（EC50 = 57.2 nM），特异性诱导表达MRGPRX2的CHO细胞的钙离子动员（EC50 = 41 nM），而在表达MRGPRX1、MRGPRX3或MRGPRX4的细胞中则无此效应（在1 µM浓度下）。PAMP-12还能作为烟碱型乙酰胆碱受体（nAChRs）的拮抗剂，抑制carbachol诱导的儿茶酚胺释放（IC50 = 1.3 µM）及钙和钠的流入（IC50分别为0.39 µM和0.87 µM），但不抑制组胺诱导的儿茶酚胺释放或钙和钠的流入（IC50 >1 µM），在初级牛肾上腺嗜铬细胞中有此表现。当以10至50 nmol/kg剂量给予正常血压大鼠时，PAMP-12能降低平均动脉血压。

Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004). Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3 References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004).

Dopamine D3 受体激动剂13a是一种Dopamine D3 受体激动剂。该化合物选择性地与Dopamine D3 受体结合，相较于Dopamine D1、D2和D4受体(Kis = 0.14、4,600、2.85和756 nM，分别)具有更高的亲和力，并且还能与血清素(5-HT)受体亚型5-HT1A、5-HT2A、5-HT2B和5-HT2C(Kis = 6、54、1.47和252 nM，分别)结合；然而，它是Dopamine D2受体的部分激动剂(EC50 = 2.26 nM，在G蛋白招募分析中)并且作为Dopamine D3受体的拮抗剂(IC50 = 4.62 nM)。在大鼠身上，当剂量为3 mg/kg时，Dopamine D3 受体激动剂13a能减少可卡因自我给药。

Ac-RYYRIK-NH2 TFA 作为高效的ORL1部分激动剂，充当ORL1的内源性配体，在CHO细胞中表现出较低的解离常数(Kd=1.5 nM)。该化合物以特异性方式激活G蛋白，作为竞争性拮抗剂，抑制noc/OFQ对大鼠脑膜和脑切片上 [35S]-GTPγS 结合G蛋白的作用。

Calcitonin (8-32), salmon, is a highly selective amylin receptor antagonist. Calcitonin, a hormone involved in calcium and phosphorus metabolism, is primarily produced by the parafollicular or C cells in the thyroid gland of mammals.