rat glucagon receptor

GRA Ex-25 (GRA-Ex-25) 是glucagon 受体抑制剂，其对大鼠和人的 glucagon 受体的IC50值分别为 56 和 55 nM。

Secretin (33-59), rat (Secretin (rat)) 是由 27 个氨基酸组成的多肽。Secretin (33-59), rat 可作用于分泌素受体，能够增强胰腺的碳酸盐、酶和钾离子的分泌。

ZP3022是一种兼具glucagon-like peptide 1 receptor (GLP-1R)和cholecystokinin 2 (CCK2) receptor的激动剂。它在表达GLP-1R或CCK2 receptor的HEK293细胞中，选择性增加cAMP积累或ERK磷酸化，而在表达CCK1 receptor的HEK293细胞中，该作用较弱（人类受体的EC50分别为0.02, 10.3和>1,000 nM）。ZP3022（40 nM）在体外实验中促进大鼠新生β细胞的增殖，并在大鼠胰岛中以10和100 nM浓度应用时增强葡萄糖诱导的胰岛素分泌（GSIS），同时以40 nmol/kg剂量每日两次给药可减少大鼠体重。在db/db小鼠中，每日100 nmol/kg剂量的ZP3022增加β细胞和胰腺总体积，同时改善葡萄糖耐量。此外，它在db/db小鼠中降低食物摄入量，但不影响体重。

Skyrin是一种天然的双蒽醌衍生物和受体选择性的胰高血糖素拮抗剂，抑制HeLa、Vero、K562、Raji、Wish和Calu-1肿瘤细胞系的生长。

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

GCGR antagonist2 是一种呋喃-2-碳酰肼化合物，是具有口服活性的胰高血糖素受体拮抗剂。GCGR antagonist2 与 hGluR 结合的 Kd 值为 2.3 nM，抑制大鼠受体的 IC50值为 0.43 nM。GCGR antagonist2 可抑制胰高血糖素刺激的糖原分解。

Zavolosotine (Compound 1) 是一种通过口服途径有效的生长抑素受体 5 型 (SST5) 激动剂，其EC50值小于1 nM。Zavolosotine 能够抑制胰岛素和胰高血糖素的分泌，并提高大鼠模型中血液的胰高血糖素水平。

GLP-1 receptor agonist. Endogenous preproglucagon-derived neuropeptide that modulates feeding and metabolism. Also secreted by intestinal L-cells. Increases cAMP production and inhibits gastric acid secretion in rat stomach. Also weak glucagon receptor ag

Glucagon receptor antagonist (pA2 = 7.2 for inhibition of glucagon-induced adenylyl cyclase activation in rat liver membranes); displays no agonist activity. Enhances glucose-stimulated pancreatic insulin release in vitro. Blocks added glucagon-induced hy