CCK-AR Inhibitors

The chemical class of CCK-AR inhibitors comprises a range of compounds primarily characterized by their ability to reduce the activity of the Cholecystokinin receptor type A. This class includes specific antagonists like proglumide, lorglumide, tarazepide, and devazepide, which function by directly competing with the natural ligand, cholecystokinin, for binding to the receptor. By occupying the ligand-binding site on CCK-AR, these compounds impede the activation of the receptor, effectively inhibiting its signaling pathway. Several of these inhibitors, such as dexloxiglumide and loxiglumide, are selective in their action, demonstrating a high affinity for CCK-AR and minimal effects on other receptor types. This selectivity is crucial for their role in specifically targeting CCK-AR-related pathways. Experimental compounds like PD 135,158 and asperlicin also fall under this class, having shown the ability to inhibit CCK-AR activity in research settings. Furthermore, the class includes compounds like loxapine and amperozide, which are primarily known for their antipsychotic properties but have been found to possess CCK-AR inhibitory effects. Lithium chloride, typically used in mood disorders, is also included due to its indirect influence on various neurotransmitter systems and signaling pathways, which may affect CCK-AR activity.