CCKBR agonist-2 (Compound z-44) is a Gi-preferring CCKBR agonist. CCKBR agonist-2 effectively activates the CCKBR-Gi signaling pathway ( EC 50 = 0.27 nM), but has almost no activity on Gq and Gs signaling pathways. CCKBR agonist-2 shows no significant protective effect in the mouse Alzheimer's disease model, proving that the simple activation of the Gi signal pathway does not play a dominant role in the improvement of cognitive function [1].
References:
[1]. Wang JL, et al. Elucidating pathway-selective biased CCKBR agonism for Alzheimer's disease treatment. Cell. 2025 Nov 20:S0092-8674(25)01238-3.
References:
[1]. Wang JL, et al. Elucidating pathway-selective biased CCKBR agonism for Alzheimer's disease treatment. Cell. 2025 Nov 20:S0092-8674(25)01238-3.