Cholecystokinin octapeptide ammonium

Cholecystokinin octapeptide ammonium (CAS No. 70706-98-8, i.e., the ammonium salt of CCK-8, whose activity is predominantly attributable to its sulfated form, CCK-8s) is the ammonium salt form of cholecystokinin octapeptide (CAS No. 25126-32-3, catalog No.: BA2823). Cholecystokinin octapeptide is a pleiotropic brain–gut peptide whose core biological activities include induction of anxiety-like behavior, attenuation of morphine withdrawal-induced anxiety, inhibition of apoptosis, modulation of immune responses, and promotion of atrial natriuretic peptide (ANP) secretion. Its primary targets are the G protein–coupled receptors CCK1R and CCK2R, and its downstream signaling involves molecules such as β-arrestin 2, p38 MAPK, Akt, NOX4, PGC-1α, and PPARα/PPARγ. In addition, it can interact with μ-opioid receptors by regulating endorphin release. The biological effects of CCK-8 are context- and concentration-dependent. Commonly used experimental concentrations include: 0.01–1 μmol/L for in vitro cell studies (e.g., SH-SY5Y, HEK293) to inhibit apoptosis and modulate immune responses; 1–10 pmol/g body weight for intracerebroventricular (ICV) injection in zebrafish to induce anxiety-like behavior; 0.01–4 μg for ICV injection in rats to exert anxiolytic effects and antagonize electroacupuncture-induced analgesia; 5–10 mg/kg for intraperitoneal (IP) injection in rats to mimic endorphin-like effects; and 100 pM in perfused isolated rat atria to promote ANP secretion. Experimentally validated effective doses include: 0.1–1 μg (ICV, rat) for alleviating morphine withdrawal-induced anxiety; 0.1–1 μmol/L for inhibiting methamphetamine-induced neuronal apoptosis; and 100 pM CCK-8s for stimulating ANP secretion. These activities are critically dependent on sulfation (the desulfated form, CCK-8d, lacks both ANP secretagogue activity and anti-analgesic activity), with CCK1R primarily mediating the anxiolytic effects and CCK2R contributing to anti-apoptotic actions and downstream signal transduction.

References:

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