Cholecystokinin Receptor Agonist

Caerulein is a decapeptide and a potent cholecystokinin receptor agonist. Caerulein is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts.

Pentagastrin (ICI-50123) is a potent, selective Cholecystokinin B (CCK_B) receptor agonist with an EC₅₀ value of 11 nM. Pentagastrin enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury.

CCK2R agonist-1 (Compound 2S) is a CCK2R agonist, with an IC₅₀ of 48 nM against wild-type CCK-2R and an IC₅₀ of 450 nM against mutant CCK-2R (N353L). CCK2R agonist-1 stimulates the production of inositol phosphate. The changes in pH and HDC induced by CCK2R agonist-1 in mice are comparable to those induced by the full-length peptide agonist Gastrin. CCK2R agonist-1 can be used in studies of gastric diseases and pain.

SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.

Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin. Tetragastrin can stimulate gastric secretion. Tetragastrin is a Cholecystokinin (CCK-4) receptor agonist. Gastric mucosal protection.

A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC₅₀s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively.

CCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor (CCKBR) agonist with an EC₅₀ of 35 pM. CCKBR agonist-1 significantly increases the survival rate of neurons, with an EC₅₀ of 37 pM. CCKBR agonist-1 can improve the cognitive decline in mice by upregulating α-secretase (ADAM10) and calcium signaling molecule PLCB4, reduce the number of amyloid β (Aβ) plaques, and promote long-term potentiation (LTP). CCKBR agonist-1 can be used for the study of Alzheimer's disease.

CCKBR agonist-2 (Compound z-44) is a Gi-preferring CCKBR agonist. CCKBR agonist-2 effectively activates the CCKBR-Gi signaling pathway (EC₅₀ = 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.

Pentagastrin (ICI-50123) meglumine is a potent, selective Cholecystokinin B (CCK_B) receptor agonist with an EC₅₀ value of 11 nM. Pentagastrin meglumine enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury.

FE101120 is a non-peptide agonist CCK2 receptor agonist. FE101120 can be used for the study of diabetes.

CE-326597 is a small molecule agonist of the cholecystokinin A receptor (CCKAR). CE-326597 occupies only the lower half of the TMD pocket and cannot mimic the crucial interaction between CCK-8 and ECL1-3. CE-326597 can be used to study metabolic diseases and gastrointestinal dysfunction.

A71378 is a selectivity CCK-A receptor agonist the IC₅₀ values of 0.4 nM, 300 nM, and 1,200 nM for the pancreatic CCK-A, cortical CCK-B, and gastrin receptor, respectively. A71378 elicits pancreatic amylase secretion (EC₅₀ = 0.16 nM) and ileal muscle contraction (EC₅₀ = 3.7 nM).

FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research.

GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.

GW-5823 is a selective CCK-AR agonist with an EC₅₀ of 70 nM. GW-5823 can be studied in research on obesity.

ARL 15849XX is a cholecystokinin-8 (CCK-8) analog.

Caerulein acetate is a decapeptide and a potent cholecystokinin receptor agonist. Ceruletide acetate is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts.

BC264 is a highly potent and selective CCK-B agonist that crosses the blood-brain barrier. BC264 increases dopamine in the nucleus accumbens and facilitates motivation and attention in rats.

Jmv 176 is a CCK agonist when first given and becomes a cholecystokinin antagonist after 3-4 hours.

U-67827E is a cholecystokinin (CCK) agonist that decreases food intake over a prolonged period of time in baboons. U-67827E may affect the latency to food by inhibiting the movement of food in the stomach and magnifying a gastric distention signal.