CCK

Cholecystokinin receptors (CCKRs) are a class of G-protein coupled receptors that respond to the peptide hormone cholecystokinin (CCK). CCK is predominantly found in the gastrointestinal tract and the central nervous system. There are two primary subtypes of cholecystokinin receptors: CCK-A (CCK1) receptor, mainly located in the pancreas, gallbladder, stomach, and certain areas of the brain, and CCK-B (CCK2) receptor, found predominantly in the brain and the stomach lining.

The primary function of CCKRs is to mediate the physiological actions of CCK. In the digestive system, CCK is involved in stimulating the digestion of fats and protein. It achieves this by inducing the secretion of digestive enzymes from the pancreas and bile from the gallbladder. Moreover, CCK plays a crucial role in regulating appetite by promoting satiety, making it a point of interest in obesity research.

In the central nervous system, CCK is involved in various functions, including anxiety, pain, and neuroendocrine control. CCK and its receptors are also implicated in psychiatric disorders like anxiety and panic attacks.

CCKRs are also significant in the medical field as potential targets for therapeutic intervention. For instance, CCK-B antagonists are being explored for their potential in treating anxiety disorders and gastrointestinal issues.

Overall, cholecystokinin receptors are integral to various physiological processes, from digestion to brain function, highlighting their importance in both understanding bodily functions and developing medical treatments.

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  1. CCK-A Receptor Agonist

    A71378 is a selective CCK-A receptor agonist with an IC50 of 0.4 nM for the pancreatic CCK-A receptor, and significantly higher IC50 values for the cortical CCK-B and gastrin receptors at 300 nM and 1,200 nM, respectively. This compound effectively stimulates pancreatic amylase secretion with an EC50 of 0.16 nM and induces ileal muscle contraction with an EC50 of 3.7 nM. A71378 is valuable for research applications focusing on gastrointestinal pharmacology and the role of CCK-A receptors in digestive processes.
  2. CCK2 Agonist

    FE100726 is a potent Cholecystokinin 2 (CCK2) receptor agonist, exhibiting high binding affinity to the CCK2 receptor. This compound has been demonstrated to effectively stimulate gastric acid secretion in anesthetized rat models. FE100726 is valuable for research related to diabetes and gastrointestinal physiology, offering insights into the role of CCK2 signaling pathways.
  3. Cholecystokinin Receptor Inhibitor

    Gastrazole free acid is a cholecystokinin receptor antagonist that demonstrates potential in inhibiting pancreatic cancer growth. By targeting gastrin receptors, this compound plays a crucial role in the modulation of gastric functions and may aid in the investigation of therapeutic strategies for gastrointestinal malignancies. Its utility in research provides insights into receptor-mediated pathways and cancer biology.
  4. CCK2 Antagonist

    PD 136450 is a potent antagonist of cholecystokinin 2 (CCK2) receptors. This compound demonstrates significant biological activity, including anti-secretory, anxiolytic, and anti-ulcer effects. PD 136450 effectively inhibits gastric acid secretion with an IC50 of 1 mg/kg and significantly reduces hemorrhagic lesions in rat models, with an IC50 of 4.7 mg/kg. It is a valuable tool for investigating gastrointestinal disorders and evaluating potential therapeutic approaches in related pharmacological research.
  5. CCK-A/B Receptors Antagonist

    Proglumide hemicalcium is a non-peptide antagonist of cholecystokinin (CCK)-A/B receptors. It selectively inhibits the actions of CCK in the central nervous system, demonstrating key biological activities such as the inhibition of gastric secretion and protection of the gastroduodenal mucosa. Additionally, Proglumide hemicalcium exhibits antiepileptic and antioxidant properties, making it a valuable reagent for research in gastrointestinal protection and neurological studies.
  6. CCK1R Agonist

    PF-04756956 is a potent agonist of the type 1 cholecystokinin receptor (CCK1R) with an EC50 of 0.47 nM. This compound is valuable for studying the mechanisms underlying obesity and associated metabolic disorders. Its activity at CCK1R makes it a significant tool for investigating therapeutic strategies aimed at regulating appetite and metabolic function.
  7. CCK1-receptor Antagonist

    JNJ-17156516 is a potent and selective antagonist of the cholecystokinin (CCK)1 receptor. This compound demonstrates significant biological activity in inhibiting CCK-induced signaling, making it valuable for research in gastrointestinal physiology and related disorders. Its oral bioavailability positions it as a useful tool in the exploration of CCK1 receptor functions and therapeutic applications.
  8. CCKB Receptor Antagonist

    Spiroglumide is a selective cholecystokinin B (CCKB) receptor antagonist. It demonstrates significant biological activity through the inhibition of CCKB receptor signaling, making it valuable for studying the physiological roles of cholecystokinin in various biological systems. Research applications include the investigation of gastrointestinal disorders and the exploration of potential therapeutic strategies in conditions linked with dysregulated CCKB receptor activity.
  9. Cholecystokinin Receptor Agonist

    ARL 15849XX is a potent agonist of the cholecystokinin receptor, specifically designed as an analog of cholecystokinin-8 (CCK-8). It effectively engages CCK receptors, stimulating pathways associated with gastrointestinal functions and satiety. This compound is valuable in research applications focusing on digestive physiology and neuropeptide signaling pathways.
  10. Cholecystokinin Receptor Agonist

    Caerulein acetate is a decapeptide that functions as a potent agonist of the cholecystokinin receptor. It exhibits significant cholecystokinetic activity, promoting contraction of the gallbladder and facilitating bile duct function. This compound is widely used in research applications related to gastrointestinal motility and the study of digestive processes.
  11. CCKB Antagonist

    PD 135158 is a selective antagonist of the CCKB receptor, exhibiting an IC50 of 2.8 nM in mouse cortex assays. This compound demonstrates notable anxiolytic properties, making it a valuable tool for research into anxiety disorders and related neuropharmacological studies. Its specificity and potency make PD 135158 suitable for investigating the role of CCKB receptors in various biological contexts.
  12. CCK-B Antagonist

    LY262691 is a selective antagonist of the cholecystokinin B (CCK-B) receptor, known for its antipsychotic properties. This compound effectively reduces the activity of spontaneously firing A9 and A10 dopamine neurons, making it a valuable tool in antipsychotic research. Its mechanism offers insights into the modulation of dopaminergic signaling pathways related to psychiatric disorders.
  13. CCK Antagonist

    LY 202769 is a cholecystokinin (CCK) and gastrin receptor antagonist, providing a valuable tool for investigating the roles of these receptors in physiological processes. This compound exhibits potent antagonistic activity, making it suitable for research into gastrointestinal disorders as well as central nervous system diseases. Its application can aid in understanding the mechanisms of action associated with CCK and gastrin receptors in these pathologies.
  14. Cholecystokinin Receptor Antagonist

    Lorglumide is a potent cholecystokinin (CCK) receptor antagonist that effectively blocks the activity of CCK at its receptors. This compound is instrumental in studying the regulation of pancreatic secretion and growth. Lorglumide serves as a valuable tool for investigating gastrointestinal physiology and related disorders.
  15. CCK Receptor Antagonist

    Cholecystokinin (27-32)-amide is a potent antagonist of the cholecystokinin (CCK) receptor, primarily interfering with CCK-mediated signaling pathways. This compound exhibits significant biological activity in regulating digestive processes and satiety. It is widely utilized in research applications focused on gastrointestinal function, neuropeptide signaling, and potential therapeutic interventions for related disorders.
  16. CCKB/Gastrin Receptor Antagonist

    RP-69758 is a selective non-peptide antagonist of the cholecystokinin-B (CCKB)/gastrin receptor, demonstrating over 200-fold specificity for CCKB compared to CCKA receptors. This compound effectively inhibits CCK-8-induced neuronal firing in rat hippocampal slices and suppresses pentagastrin-induced gastric acid secretion in rats. RP-69758 serves as a valuable tool for investigating neurological disorders and gastrointestinal diseases in research applications.
  17. CCK Agonist

    JMV 176 is a cholecystokinin (CCK) receptor agonist that exhibits its primary activity upon initial administration. Following a period of 3–4 hours, it transitions to function as a CCK antagonist. This dual-action characteristic makes JMV 176 valuable for research exploring CCK-related physiological processes and potential therapeutic applications in gastrointestinal disorders.
  18. CCK-A Receptor Antagonist

    CHEMBL333994 is a selective antagonist of the Cholecystokinin A receptor (CCK-A receptor), exhibiting a potent inhibitory activity with an IC50 of 0.67 nM. This compound selectively targets peripheral CCK receptors and has been shown to increase CCK mRNA levels. CHEMBL333994 is useful in research related to chronic pancreatitis, providing insights into its therapeutic potential in gastrointestinal disorders.
  19. CCK-B Antagonist

    GV-150013 is a selective antagonist of the cholecystokinin B (CCK-B) receptor, known for its ability to modulate neurotransmitter activity. This compound is primarily utilized in studies investigating sleep regulation and related disorders. Its distinct mechanism of action positions GV-150013 as a valuable tool for research into the pharmacological management of sleep disturbances and anxiety-related conditions.
  20. CKK Antagonist

    JMV 167 is a potent antagonist of the peripheral cholecystokinin receptor (CKK), exhibiting an IC50 value of 500 nM. This compound is valuable for research applications involving the modulation of digestive processes and appetite regulation. Its role in studying the effects of cholecystokinin signaling makes it an essential tool for investigating therapeutic strategies related to gastrointestinal disorders and metabolic conditions.
  21. CCK Agonist

    U-67827E is a cholecystokinin (CCK) agonist that modulates food intake by impacting gastrointestinal motility. This compound influences the latency to food consumption, potentially through the inhibition of gastric emptying and enhancement of gastric distention signaling. U-67827E is valuable for research applications investigating appetite regulation and the mechanisms of satiety.
  22. CCK-B Receptor Antagonist

    L-740093 is a potent cholecystokinin-B (CCK-B) receptor antagonist with significant central nervous system (CNS) penetration. This compound is utilized in research to investigate the role of CCK-B receptors in various physiological and pathological processes, including anxiety and pain modulation. Its ability to effectively cross the blood-brain barrier makes it a valuable tool for exploring CNS-related mechanisms.
  23. CCK/Gastrin Receptor Antagonist

    Benzotript is a cholecystokinin (CCK) and gastrin receptor antagonist. It exhibits significant antiproliferative effects in human colon carcinoma cell lines, making it valuable for cancer research. This compound can be employed in studies investigating the role of CCK and gastrin signaling pathways in tumor growth and development.
  24. CCKB Receptor Antagonist

    L 368935 is a potent antagonist of the cholecystokinin B receptor (CCKB receptor), demonstrating effective brain penetration and central activity. This compound is significant for research applications focused on neuropharmacology and gastrointestinal physiology, as well as studying the roles of CCKB receptors in various neurological disorders.
  25. CCK2R Antagonist

    CI-988 is a potent and selective antagonist of the cholecystokinin 2 receptor (CCK2R), exhibiting an IC50 of 1.7 nM in mouse cortex assays. Demonstrating over 1600-fold selectivity for CCK2 over the CCK1 receptor, CI-988 has been shown to possess anxiolytic and anti-tumor properties. This compound is valuable for research into therapeutic applications in anxiety disorders and cancer treatment.
  26. CCKBR Antagonist

    Itriglumide is a potent and selective antagonist of the cholecystokinin B receptor (CCKBR), exhibiting an IC50 of 2.3 nM. It effectively antagonizes gastrin response in a dose-dependent manner, with an IC50 of 5.9 nM. Itriglumide demonstrates significant antisecretory and antiulcer properties, making it a valuable reagent for research in gastrointestinal pharmacology and related studies.
  27. Decapeptid

    Caerulein, desulfated is a desulfurated form of the decapeptide Caerulein, which shares five carboxyl-terminal amino acids with gastrin and cholecystokinin (CCK). This compound primarily targets and activates CCK receptors, playing a significant role in gastrointestinal physiology. It is widely utilized in research applications focused on understanding digestive processes, appetite regulation, and modulation of pancreatic activities.
  28. Anorectic Agent

    FPL 14294 is an intranasally active anorectic agent and cholecystokinin octapeptide (CCK) analog known for its enhanced metabolic stability. This compound effectively induces satiety across various species, making it a valuable tool for research in appetite regulation and metabolic studies. Its unique properties facilitate investigations into mechanisms of weight control and potential therapeutic interventions for obesity.
  29. CCK Fragment

    Cholecystokinin (1-21) is a fragment of the cholecystokinin polypeptide that primarily targets the CCK receptors. This peptide is known to stimulate lipolysis in human adipose tissue, making it an important reagent for studies focused on metabolic regulation and energy homeostasis. Its application extends to research involving appetite regulation and gastrointestinal function.
  30. CCK-B Receptor Antagonist

    LY288513 is a selective non-peptide antagonist of the cholecystokinin B (CCK-B) receptor, exhibiting an IC50 value of 16 nM. It has been demonstrated to produce anxiolytic-like effects in murine models, making it a valuable tool for research in anxiety disorders and related neurobiological studies. Its specificity for the CCK-B receptor allows for targeted investigation into the mechanisms underlying anxiety and stress responses.
  31. CKK Antagonist

    JMV 179 is a cholecystokinin receptor (CKK) antagonist with an IC50 of 30 nM. This peptide analog is designed to inhibit CCK receptor activity, making it a valuable tool for studying the physiological and pathophysiological roles of CCK signaling. JMV 179 is utilized in various research applications, particularly in gastrointestinal studies and neuropharmacology, to explore the therapeutic potential of modulating CCK pathways.
  32. CCK B Inhibitor

    PD-135666 is a potent dipeptide inhibitor of cholecystokinin B (CCK B) receptors, demonstrating an IC50 of 0.1 nM in mouse cerebral cortex. Unlike its enantiomer, PD-140548, which selectively targets CCK A receptors in rat pancreas, PD-135666 primarily interacts with CCK B receptors. This compound has been shown to exhibit anxiolytic effects in various animal models, making it a valuable tool for studying anxiety-related disorders and CCK receptor biology.
  33. CCK Fragment

    Cholecystokinin-33 (swine) is a biologically active fragment of cholecystokinin (CCK) that primarily targets CCK receptors. It is known to reduce food intake and promote gallbladder contraction, making it relevant for studies focused on appetite regulation and gastrointestinal motility. This peptide can be utilized in research to investigate its roles in digestive processes and related metabolic disorders.
  34. CCK-A Receptor Antagonist

    (rac)-CHEMBL333994 is a potent Cholecystokinin A (CCK-A) receptor antagonist with an IC50 of 0.67 nM, demonstrating effective oral bioavailability. This compound selectively targets peripheral CCK receptors, making it valuable for studying mechanistic pathways involved in gastrointestinal disorders. Its ability to increase CCK mRNA levels positions (rac)-CHEMBL333994 as a useful tool in research aimed at understanding chronic pancreatitis and related conditions.
  35. CCK-B Agonist

    JMV 170 is a selective CCK-B agonist that specifically targets the CCK-B receptor with a binding affinity ten times greater than that for the CCK-A receptor. This compound induces contractile effects in pig smooth muscle cells, exhibiting an EC50 value of 9 pmol/L. JMV 170 is primarily utilized in research applications focusing on gastrointestinal physiology and neurobiology, particularly in studies investigating the roles of cholecystokinin in smooth muscle contractility.
  36. CCK-B Receptor Antagonist

    DA-3934 is a cholecystokinin (CCK)-B receptor antagonist that effectively inhibits gastric acid secretion. Through its mechanism of action, DA-3934 blocks Pentagastrin-induced gastric acid release in rat models. This compound is valuable for research applications focused on gastrointestinal physiology and the modulation of acid secretion pathways.
  37. CCK1 Antagonist

    VL-0395 is a selective antagonist of the cholecystokinin receptor 1 (CCK1), demonstrating an IC50 of 0.197 μM in rat pancreatic acinar cells. This compound effectively inhibits CCK1-mediated signaling pathways, making it a valuable tool for studying the physiological and pathological roles of CCK1 in digestive processes and pancreatic function. Its specificity and potency position VL-0395 as an essential reagent for research in gastrointestinal pharmacology and related fields.
  38. CCK Receptor Antagonist

    KSG-504 anhydrous is a potent antagonist of the cholecystokinin (CCK) receptor. This compound has been shown to inhibit Ethionine-induced acute pancreatitis in rat models, demonstrating its relevance in studying pancreatic function and pathology. Additionally, KSG-504 facilitates the regeneration of acinar cells, making it a valuable tool for investigating therapeutic strategies in pancreatic diseases.
  39. CCK-B Receptor Agonist

    PD-149164 is a selective agonist of the cholecystokinin B (CCK-B) receptor, exhibiting high binding affinity with IC50 values of 0.083 nM for CCK-B and 75 nM for CCK-A. This compound is instrumental in studying the role of CCK-B receptors in physiological and pathological processes, including appetite regulation, anxiety, and enhanced memory function. It serves as a valuable tool for research in neuropharmacology and gastrointestinal studies.
  40. CCK-4 Analog

    A-70874 is a tyrosine-free tetrapeptide analog of cholecystokinin (CCK-4), acting as an agonist for pancreatic amylase release. It also serves as a partial agonist, promoting phosphoinositide decomposition in pancreatic cells. With an IC50 of 4.9 nM for the guinea pig pancreatic CCK receptor, A-70874 shows a notable affinity of 1.6 μM for the CCK-B/gastrin receptor. This compound is valuable for investigating the physiological roles of CCK receptors in both the digestive system and the central nervous system.
  41. Cholecystokinin Receptor Antagonist

    TP-680 is a potent cholecystokinin receptor antagonist, exhibiting a 1510-fold higher binding affinity for rat pancreatic CCKA receptors (IC50 = 1.2 nM) compared to rat brain CCKB receptors (IC50 = 1812.5 nM). This selectivity makes TP-680 a valuable tool for investigating gastrointestinal diseases. Its ability to modulate CCK receptor activity provides insights into gastrointestinal physiology and potential therapeutic applications in disorders related to CCK signaling.
  42. Cholecystokinin Antagonist

    Asperlicin is a cholecystokinin antagonist derived from Aspergillus alliaceus. This compound exhibits inhibitory effects on cholecystokinin receptors, which play a crucial role in regulating gastrointestinal functions and satiety. Asperlicin is primarily utilized in research related to digestive disorders, appetite regulation, and the study of neuropeptide signaling pathways. Its ability to modulate cholecystokinin activity makes it a valuable tool for understanding gastrointestinal and metabolic processes.
  43. CCK-B Antagonist

    L-736380 is a potent antagonist of the cholecystokinin B (CCK-B) receptor, exhibiting a high affinity with an IC50 of 0.054 nM for CCK-B and 400 nM for CCK-A. This compound effectively inhibits gastric acid secretion in anesthetized rats with an ID50 of 0.064 mg/kg. Additionally, L-736380 demonstrates significant activity in ex vivo binding assays of [125I]CCK-8S in BKTO mouse brain membranes, with an ED50 of 1.7 mg/kg. Its function as a CCK-B antagonist makes it a valuable tool for studies related to gastrointestinal physiology and neuropharmacology.
  44. CCK Antagonist

    CCK Antagonist 1 is a potent antagonist of cholecystokinin (CCK) receptors, exhibiting IC50 values of 1.1 μM for CCK1 and 4 μM for CCK2. This compound is valuable for research into the roles of CCK in cancer and mental health disorders, facilitating the exploration of therapeutic interventions targeting these pathways. Its specificity and efficacy make it a useful tool for studying the biological functions of CCK receptors.
  45. CCKB/gastrin Receptor Antagonist

    S-0509 is a selective antagonist of the CCKB/gastrin receptor, demonstrating potent inhibition of gastric secretion. This compound exhibits strong anti-secretory properties, making it a valuable tool in studies related to gastrointestinal health. S-0509 is particularly useful for research focused on the prevention of duodenal ulcers and the modulation of gastric acid secretion.
  46. CCK-8 Antagonist

    LY219057 is a potent antagonist of cholecystokinin octapeptide (CCK-8), exhibiting an ID50 of 287.5 nM. This compound interferes with CCK-8 signaling pathways, making it valuable for investigating gastrointestinal and central nervous system functions. Its application spans research into appetite regulation, digestive processes, and potential therapeutic strategies for related disorders.
  47. CCKA Receptor Antagonist

    PD-140548 is a selective cholecystokinin (CCK-A) receptor antagonist, which plays a pivotal role in modulating neuropeptide signaling. This compound has demonstrated potential in the investigation of schizophrenia and related neuropsychiatric disorders, offering insights into the CCK system's influence on behavioral outcomes. Its specificity makes it a valuable tool for elucidating the role of CCK-A receptors in various biological processes.
  48. CCK2 Receptor/Gastrin Antagonist

    AG-041R is a selective antagonist of the CCK2 receptor and functions as a gastrin inhibitor. It effectively inhibits gastrin-induced secretion of pancreastatin with an IC50 of 2.2 nM. Additionally, AG-041R demonstrates significant anti-proliferative effects on Mastomys ECL carcinoid tumor cells, making it a valuable tool for research applications related to gastrointestinal physiology and cancer biology.
  49. Cholecystokinin Receptor Inhibitor

    CCK-A receptor inhibitor 1 is a selective inhibitor of the cholecystokinin A (CCK-A) receptor, exhibiting a binding IC50 of 340 nM. By modulating CCK-A receptor activity, this compound plays a crucial role in studying gastrointestinal physiology and related disorders. Its inhibitory properties make it useful for research applications focused on appetite regulation and the gastrointestinal system.
  50. Cholecystokinin Receptor Antagonist

    Gastrin/CCK Antagonist 1 is a selective antagonist of the cholecystokinin receptor (CCK). This compound plays a significant role in inhibiting the action of gastrin and CCK, making it a valuable tool for studying gastrointestinal disorders. Research applications include evaluating gastrointestinal motility, secretion, and potential therapeutic approaches for conditions associated with dysregulated CCK signaling.

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