Cholecystokinin tetrapeptide (CCK-4, also PTK7) is a peptide fragment derived from the larger peptide hormone cholecystokinin. CCK-4 acts primarily in the brain as an anxiogenic, although it does retain some GI effects, but not as much as CCK-8 or the full length polypeptide CCK-58.
CAT No: 10-101-74
CAS No:35144-91-3
Synonyms/Alias:CCK-4; CCK4; CCK 4; Gastrin Tetrapeptide; Cholecystokinin Octapeptide (5-8); Cholecystokinin Tetrapeptide; Gastrin (14-17) (human)
CCK-4 Acetate, also known as Cholecystokinin tetrapeptide acetate, is a synthetic peptide fragment derived from the C-terminal region of the gastrointestinal hormone cholecystokinin. As a biologically active peptide, it is widely recognized for its role in mimicking the endogenous activity of cholecystokinin, particularly in the modulation of neurotransmitter release and gastrointestinal signaling pathways. Its defined sequence and functional properties make it a valuable molecular tool for elucidating peptide-receptor interactions, signal transduction mechanisms, and peptide-mediated physiological responses in various in vitro and in vivo research settings.
Receptor Pharmacology Studies: CCK-4 Acetate is extensively utilized in receptor binding and pharmacological profiling experiments to investigate the specificity and affinity of cholecystokinin receptors, particularly CCK1 and CCK2 subtypes. Researchers employ this peptide to characterize ligand-receptor interactions, assess agonist or antagonist activity, and delineate downstream signaling cascades triggered by receptor activation. Its defined structure enables controlled studies on receptor selectivity and the molecular determinants of peptide recognition, supporting the development of novel receptor modulators and advancing understanding of peptide hormone action.
Neuroscience Research: In neurobiological studies, CCK-4 Acetate serves as a potent tool to probe the role of cholecystokinin signaling in central nervous system pathways. By applying this peptide to neuronal cultures or animal models, investigators can examine its effects on neurotransmitter release, synaptic plasticity, and behavioral responses. Its ability to activate CCK receptors in the brain provides insights into the modulation of anxiety, stress responses, and cognitive processes, facilitating the exploration of neuropeptide function and the mapping of peptide-regulated neural circuits.
Gastrointestinal Physiology: The peptide is frequently employed in experimental models to study the physiological regulation of digestive processes. Its activity as a cholecystokinin analog allows researchers to evaluate the mechanisms underlying pancreatic enzyme secretion, gallbladder contraction, and gut motility. These investigations contribute to a deeper understanding of peptide hormone-mediated control of gastrointestinal function, as well as the interplay between neural and endocrine factors in digestive health.
Peptide Structure-Activity Relationship (SAR) Analysis: CCK-4 Acetate is integral to structure-activity relationship studies aimed at dissecting the contributions of individual amino acid residues to biological function. By comparing the activity of this tetrapeptide with longer or modified cholecystokinin fragments, scientists can identify key determinants of receptor activation and peptide stability. These insights inform the rational design of peptide analogs with tailored pharmacological profiles and improved research utility.
Peptide Synthesis and Analytical Method Development: The well-characterized sequence of CCK-4 Acetate makes it a valuable reference standard in peptide synthesis validation and analytical method development. It is routinely used to calibrate chromatographic and mass spectrometric techniques, ensuring accurate detection, quantification, and purity assessment of peptide samples. Its application in quality control and assay optimization enhances the reliability of peptide-based research workflows and supports the advancement of peptide chemistry methodologies.
Experimental panic induction with cholecystokinin tetrapeptide (CCK-4) is considered as a suitable model to investigate the pathophysiology of panic attacks. While only a few studies investigated the brain activation patterns following CCK-4, no data are available on the putative involvement of the amygdala in the CCK-4 elicited anxiety response. We studied the functional correlates of CCK-4-induced anxiety in healthy volunteers by means of functional magnetic resonance imaging (fMRI) and region of interest (ROI) analysis of the amygdala. Sixteen healthy volunteers underwent challenge with CCK-4 compared with placebo in a single-blind design. Functional brain activation patterns were determined for the CCK-4-challenge, the placebo response and anticipatory anxiety (AA). CCK-4-induced anxiety was accompanied by a strong and robust activation (random effects analysis, P < 0.00001, uncorrected for multiple testing) in the ventral anterior cingulate cortex (ACC), middle and superior frontal gyrus, precuneus, middle and superior temporal gyrus, occipital lobe, sublobar areas, cerebellum, and brainstem. In contrast, random effects group analysis for placebo and AA using the same level of significance generated no significant results. Using a more liberal level of significance, activations could be observed in some brain regions such as the dorsal part of the ACC during AA (random effects analysis, P < 0.005). Overall functional responses did not differ between panickers and nonpanickers. Only 5 of 11 subjects showed strong amygdala activation. However, ROI analysis pointed towards higher scores in fear items in these subjects. In conclusion, while overall brain activation patterns are not related to the subjective anxiety response to CCK-4, amygdala activation may be involved in the subjective perception of CCK-4-induced fear.
Eser, D., Leicht, G., Lutz, J., Wenninger, S., Kirsch, V., Schüle, C., ... & Rupprecht, R. (2009). Functional neuroanatomy of CCK‐4‐induced panic attacks in healthy volunteers. Human brain mapping, 30(2), 511-522.
3alpha-reduced neuroactive steroids such as 3alpha, 5alpha-tetrahydroprogesterone (3alpha, 5alpha-THP) and 3alpha, 5alpha-tetrahydrodeoxycorticosterone (3alpha, 5alpha-THDOC) are potent positive allosteric modulators of gamma-aminobutyric acid type A (GABAA) receptors and display pronounced anxiolytic activity in animal models. Experimental panic induction with cholecystokinin-tetrapeptide (CCK-4) and sodium lactate is accompanied by a decrease in 3alpha, 5alpha-THP concentrations in patients with panic disorder, but not in healthy controls. However, no data are available on 3alpha, 5alpha-THDOC concentrations during experimental panic induction. Therefore, we quantified 3alpha, 5alpha-THDOC concentrations in 10 healthy volunteers (nine men, one woman) before and after panic induction with CCK-4 by means of a highly sensitive and specific gas chromatography/mass spectrometry analysis. CCK-4 elicited a strong panic response as assessed by the Acute Panic Inventory. This was accompanied by an increase in 3alpha, 5alpha-THDOC, ACTH and cortisol concentrations. This increase in 3alpha, 5alpha-THDOC might be a consequence of hypothalamic-pituitary-adrenal (HPA) axis activation following CCK-4-induced panic, and might contribute to the termination of the anxiety/stress response following challenge with CCK-4 through enhancement of GABAA receptor function.
Eser, D., Di Michele, F., Zwanzger, P., Pasini, A., Baghai, T. C., Schüle, C., ... & Romeo, E. (2005). Panic induction with cholecystokinin-tetrapeptide (CCK-4) Increases plasma concentrations of the neuroactive steroid 3 [alpha], 5 [alpha] tetrahydrodeoxycorticosterone (3 [alpha], 5 [alpha]-THDOC) in healthy volunteers. Neuropsychopharmacology, 30(1), 192.
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