Devazepide: A Receptor Antagonist Analysis

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IC50: 0.26 nM

Devazepide is a CCK-A receptor antagonist.

CCK is primarily synthesized as a preprohormone and undergoes a series of enzymatic reactions to produce the fully active C-terminal amidated and tyrosine-sulfated octapeptide named CCK8. CCK’s biological function is mediated by CCK1R and CCK2R that belong to the seven transmembrane receptor superfamily.

In vitro: Previous study analyzed the impact of two CCK receptor antagonists, devazepide (a CCK1-R antagonist) and L365 260 (a CCK2-R antagonist), on the growth of Ewing tumor cells. Results showed that devazepide could inhibit cell growth of four different Ewing tumor cells, whereas the effect of L365 260 on cell growth was negligible [1].

In vivo: Previous study

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