vpac2

Bay 55-9837 acetate 是一种有效且高度选择性的 VPAC2 激动剂 (Kd = 0.65 nM)，可用于 2 型糖尿病研究。

MK 0893是一种高效和选择性的胰高血糖素受体(Glucagon Receptor)拮抗剂(IC50=6.6 nM)，具有竞争性、可逆性、高结合亲和力和功能性cAMP活性，可减弱胰高血糖素诱导的血糖升高，降低了急性和慢性小鼠模型的环境葡萄糖水平。

Ro 25-1553 是由 31 个氨基酸组成的血管活性肠肽 (VIP) 类似物，作为 VIP2 受体 (VPAC2 receptor) 的激动剂。在豚鼠模型中，Ro 25-1553 显示出对神经诱发或 Carbachol 诱发的气管平滑肌收缩的支气管扩张作用。

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.

PA-8是一种小分子的的 PACAP I 型(PAC1)受体拮抗剂，有 选择性、有效性和口服活性。PA-8抑制PACAP 诱导的CREB 在PAC1-受体上的磷酸化，但对VPAC11或VPAC2受体无抑制作用。PA-8也抑制pacap 诱导的体外cAMP 水平升高(IC50 = 2 nM)和体内鞘内注射后pacap 诱导的厌恶反应和机械异位性痛。

Bay 55-9837 TFA 是一种有效、高选择性的 VPAC2的激动剂，Kd 值为 0.65 nM。Bay 55-9837 TFA 可能是用于 2 型糖尿病研究的有用方法。

Vasomera是一種穩定的長效血管活性腸肽（VIP）激動劑，主要作用於G蛋白偶聯的VPAC2受體，適用於與肌肉營養不良症相關的心肌病研究。

Myristoyl-(Lys12,27,28)-VIP-Gly-Gly-Thr（free acid）是VPAC2受体的高亲和性及选择性拮抗剂。

PACAP (1-27), human, ovine, rat TFA (PACAP 1-27 TFA), an N-terminal fragment of PACAP-38, is an effective PACAP receptor antagonist with IC50 values of 3 nM for rat PAC1, 2 nM for rat VPAC1, and 5 nM for human VPAC2.

Selective VPAC2 receptor agonist (EC50 values are 0.4, 100 and >1000 nM for VPAC2, VPAC1 and PAC1, respectively in a cAMP accumulation assay; IC50 values are 60, 8700 and >10000 nM for VPAC2, VPAC1 and PAC1, respectively in a competition binding assay). S