CCKAR Antagonist

Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors.

Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC₅₀ of 6 nM and a K_i of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC₅₀ value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin.

Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.

Pranazepide (FR120480) is a selective cholecystokinin-1 receptor (CCK1-R) antagonist with an IC₅₀ of 0.67 nM against CCK1-R. Pranazepide is applicable for the research of pancreatic diseases.

PD 135158 (CAM 1028) is a selective CCK_B receptor antagonist with an IC₅₀ of 2.8 nM against mouse cortex CCK_B. PD 135158 shows anxiolytic activity.

CHEMBL333994 (FK-480) is a potent and orally active Cholecystokinin A receptor (CCK-A receptor) antagonist, with an IC₅₀ of 0.67 nM. CHEMBL333994 selectively antagonizes peripheral CCK receptors. CHEMBL333994 increases CCK mRNA level. CHEMBL333994 can be used for research of chronic pancreatitis.

TP-680 is a cholecystokinin receptor antagonist. TP-680 binds 1510 times more strongly to rat pancreatic CCK_A receptors (IC₅₀=1.2 nM) than to rat brain CCK_B receptors (IC₅₀=1812.5 nM). TP-680 can be used in the study of gastrointestinal diseases.