Cholecystokinin inhibition

Y2. Yasui, W., Sumiyoshi, H., Ochiai, A., and Tahara, E., Cholecystokinin inhibition of tumour growth and gastrin-stimulated cyclic 3 5 -monophosphate metabolism in human gastric carcinoma in nude mice. Cancer Res. 46, 740-743 (1986). 

Larksarp and Alper used a palladium(II) catalyzed cyclocarbonylation reaction to generate a series of more complex and biologically relevant 4(3 0-Penicillium chrysogenum), have been shown to exhibit PTK inhibition and cholecystokinin inhibition as well as antimicrobial, anti-convulsant, anti-depressant and anti-inflammatory properties. Reaction of o-iodoaniline, a substituted ketenimine, and carbon monoxide with palladium(II) acetate and l,l -bis-diphenylphosphino-ferrocene (dppf) under thermal conditions gave the desired quinazolinone in near quantitative yield. In the same report, the authors showed that similar reactions could also be conducted with isocyanates and carbodiimides (not shown). 

Several neuropeptides are under current investigation for their role in anxiety disorders. Important neuropeptides include neuropeptide Y (NPY), substance P, and cholecystokinin. NPY appears to have a role in reducing the effect of stress hormones and inhibiting activity of the LC. Both mechanisms may contribute to the anxiolytic properties seen experimentally. Substance P may have anxiolytic and antidepressant properties. This may be due in part to its effects on corticotropin-releasing hormone.21... 

Cholecystokinin Endocrine cells in mucosa of duodenum Breakdown products of lipid and, to a small extent, protein digestion in duodenum Inhibits gastric emptying and gastric secretion stimulates contraction of gallbladder stimulates secretion of digestive enzymes from pancreas... 

Kleibeuker JHH, Beekhuis JNBJ, Jansen J, Piers DA, Lamers CBHW. Cholecystokinin is a physiological hormonal mediator of fat-induced inhibition of gastric emptying in man. Eur J Clin Invest 1988 18 173-177. 

Keck ME, Holsboer F (2001) Hyperactivity of CRH neiu-onal circuits as a target for therapeutic interventions in affective disorders. Peptides 22 835-844 Kellner M, Wiedemann K, Holsboer F (1992) ANF inhibits the CRH-stimulated secretion of ACTH and cortisol in man. Life Sci 50 1835-1842 Kellner M, Herzog L, Yassouridis A, Holsboer F, Wiedemann K (1995) A possible role of atrial natriuretic hormone in pituitary-adrenocortical imresponsiveness in lactate-induced panic disorder. Am J Psychiatry 152 1365-1367 Kennedy JL, Bradwein J, Koszycki D (1999) Investigation of cholecystokinin system genes in panic disorder. Mol Psychiatry 4 284-285... 

While researchers believe that the GABAergic response is responsible for the major effects of the BZs, other mechanisms of action have been proposed. The BZs increase calcium-dependent potassium, inhibit tetrodotoxin-sensitive NA channels, and antagonize cholecystokinin-induced excitation. The clinical relevance of these actions is unknown at this time (Polk, 1988 Hobbs et ah, 1996). 

Wang HY, Friedman E Chronic lithium desensitization of autoreceptors mediating serotonin release. Psychopharmacology 94 312-314, 1988 Wang HY, Friedman E Lithium inhibition of protein kinase C activation-induced serotonin release. Psychopharmacology 99 213-218, 1989 Wank SA, Pisegna JR, de Weerth A Brain and gastrointestinal cholecystokinin receptor family structure and functional expression. Proc Natl Acad Sci USA 89 8691-8695, 1992... 

A. G. Phillips, R. E. Lane, C. D. Blaha (1986). Inhibition of dopamine release by cholecystokinin relevance to schizophrenia. Trends Pharmacol. 7 126-127. 

It inhibits the secretion of numerous hormones and transmitters, including gastrin, cholecystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, vasoactive intestinal peptide, and 5-HT. 

Vaught et al., 1982). By this cross-talk 5-agonists inhibit the spinal release of pronociceptive cholecystokinin (CCK-... 

Neu, A., Foldy, C., and Soltesz, I. (2007). Postsynaptic origin of CBl-dependent tonic inhibition of GABA release at cholecystokinin-positive basket cell to pyramidal cell synapses in the CA1 region of the rat hippocampus.. Physiol. 578, 233—247. 

Many biologically active secreted peptides are also amidated at their carboxyl terminal, and acetylated at their amino-terminal. The consequences of these modifications are (a) to reduce the susceptibility of these peptides to degradative actions of extracellular aminopeptidases and carboxypeptidases after their secretion and (b) to influence the biological activity of the peptides. Corticotropin-releasing factor, gastrin, cholecystokinin and vasopressin require the C-terminal amide for full activity [54—56]. Acetylation of the N-terminus of a-MSH is necessary for activity, whereas acetylation of /3-endorphin inhibits its opioid activity [57], The enzymes responsible for acetylation have been identified from bovine and rat intermediate lobes [57] and enzymes with a-amidation activity have been reported in preparations of pituitary secretory granules [54,55]. 

Froetschel, M.A., Azain, M.J., Edwards, G.L., Barb, C.R., and Amos, H.E. 2001. Opioid and cholecystokinin antagonists alleviate gastric inhibition of food intake by premeal loads of casein in meal-fed rats. J. Nutr. 131, 3270-3276. 

Ito et al. (1994) studied the inhibition of CCK-8-induced pancreatic amylase secretion by a cholecystokinin type-A receptor antagonist in rats. 

There are a variety of peptide hormones acting in the gut the gastrins stimulate gastric acid secretion secretin and somatostatin inhibit the production of gastrins. Cholecystokinin and somatostatin can inhibit gastric acid secretion directly, and the former one causes the gall-bladder to contract and thus force bile into the duodenum. 

Olvanil (= A-(Vanillyl)-9-oleamide] (vanilloid phenolic) Cholecystokinin receptor Synthetic (cf. Capsaicin) Anandamide transport inhibition [14] (VR agonist) 5.8D... 

Q10 Normally, pancreatic secretion is stimulated by eating. The factors involved are both nervous and hormonal. Pancreatic secretion is increased by vagal (parasympathetic) stimulation and inhibited by sympathetic stimulation. Cholecystokinin (CCK), released from the wall of the duodenum, stimulates pancreatic juice, which is rich in enzymes. Secretin (the first hormone to be discovered, by Bayliss and Starling), which is also produced in the duodenum, stimulates a pancreatic fluid with a high bicarbonate content. 

The anxiety caused by pentagastrin is prevented by inhibiting cholecystokinin receptors (570). 

Gastric acid production is regulated by both the autonomic nervous system and several hormones. The parasympathetic nervous system, via the vagus nerve and the hormone gastrin, stimulates the parietal cell to produce gastric acid, acting both directly on parietal cells and indirectly through the stimulation of the secretion of the hormone histamine from ECL cells. Vasoactive intestinal peptides, cholecystokinin and secretin all inhibit acid production. 

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