PF-06882961 是一种口服生物可利用的胰高血糖素样肽-1 受体 (GLP-1R) 激动剂。 PF-06882961 在给大鼠的最高剂量水平下显示出对心脏的轻度至中度损害、对胸腺的中度至重度影响（有助于控制感染）、轻度至中度胃溃疡。

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). Stimulates glucose-dependent insulin secretion in isolated human pancreatic islets. Reduces HIV-1 viral replication and shows cooperative effects when given in conjunction with VPAC1 agonists.

NNC-0640 是人胰高血糖素受体的负变构调节剂，IC50 为 69.2 nM。