Cholecystokinin A receptor

Cholecystokinin-A receptors are in- CN153 volved in food intake suppression in rats after intake of all fats and carbohydrates tested. J Nutr 2003 133(7) 2319-2325. 

Ninomiya et al. (1998) studied the effects of a cholecystokinin A receptor antagonist on pancreatic exocrine secretion stimulated by exogenously administered CCK-8 in conscious dogs with chronic pancreatic fistula. 

Ding and Hakanson (1996) examined the effect of drags on a cholecystokinin-A receptor-mediated response by gastric emptying of a charcoal meal in mice. 

Tokarski, J. and Hopfinger, A.J. (1994). Three-Dimensional Molecular Shape Analysis - Quantitative Structure-Activity Relationship of a Series of Cholecystokinin-A Receptor Antagonists. J.Med.Chem., 37,3639-3654. 

Cholecystokinin A receptor GI Increase in GI motility, gall bladder function... 

Miyasaka K, Kanai S, Ohta M, et al. Overexpression of cholescystokinin-B/gastrin receptor gene in the stomach of naturally occurring cholecystokinin-A receptor gene knockout rats. Digestion 1998 59(1) 26-32. 

Boeckxstaens GE, Hirsch DP, Fakhry N, et al. Involvement of cholecystokinin-A receptors in transient lower esophageal sphincter relaxations triggered by gastric distension. Am J Gastroenterol 1998 93 1823-1828. 

Molecular Shape Analysis Quantitative Structure-Activity Relationship of a Series of Cholecystokinin-A Receptor Antagonists. 

The BZ stmcture also has provided a molecular scaffold for a number of peptide receptor ligands (26). Antagonists for the cholecystokinin (CCK-A) receptor, eg, devazepide (65), the thyrotropin-releasing hormone (TRH) receptor, eg, midazolam (66), and the /i -opiate receptor, eg, tifluadom (67), as well as a series of ras famyl transferase inhibitors, eg, BZA-2B (68) (30) have been identified (Table 4). 

Archer-Lahlou, E. Tikhonova, I. Escrieut, C. Dufresne, M. Seva, C. Clerc, P. Pradayrol, L. Moroder, L. Maigret, B. Fourmy, D., Modeled structure of a G-protein-coupled receptor the cholecystokinin-1 receptor, J. Med. Chem. 2005, 48, 180-191. 

HGnn, J. Maigret, B. Tarek, M. Escrieut, C. Fourmy, D. Chipot, C., Probing a model of a GPCR/ligand complex in an explicit membrane environment. The human cholecystokinin-1 receptor, Biophys. J. 2006, 90, 1232-1240. 

Finally, a thorough receptor binding study by Raffa and colleagues (1998) showed that hypericin extracts had no effect at adrenergic (alpha or beta), adenosine, angiotensin, benzodiazepine, dopamine, bradykinin, neuropeptide Y, PCP, NMDA, opioid, cholecystokinin A, histamine HI, or nicotinic ACh receptors. Although comprehensive, this study did not look at the binding of any other hypericum constituents. 

Mezey E, Reisine TD, Skirboll L, Beinfeld M, Kiss JZ (1985) Cholecystokinin in the medial parvocellular subdivision of the paraventricular nucleus coexistence with corticotropinreleasing hormone. Ann NY Acad Sci 448 152-156 Miller CC, Holmes PV, Edwards GL (2002) Area postrema lesions elevate NPY levels and decrease anxiety-related behavior in rats. Physiol Behav 77 135-140 Miyasaka K, Kobayashi S, Ohta M, Kanai S, Yoshida Y, Nagata A, Matsui T, Noda T, Takiguchi S, Takata Y, Kawanami T, Funakoshi A (2002) Anxiety-related behaviors in cholecystokinin-A, B, and AB receptor gene knockout mice in the plus-maze. Neurosci Lett 335 115-118... 

Dorow R, Horowski R, Paschelke G, Amin M (1983) Severe anxiety induced by EG 7142, a beta-carboline ligand for benzodiazepine receptors. Lancet 2 98-99 Erankland PW, Josselyn SA, Bradwejn J, Vaccarino PJ, Yeomans JS (1997) Activation of amygdala cholecystokinin B receptors potentiates the acoustic startle response in the rat. J Neurosci 17 1838-1847... 

Miyasaka K, Kobayashi S, Ohta M, Kanai S, Yoshida Y, Nagata A, Matsui T, Noda T, Takuguchi S, Takata Y, Kawanami T, Funakoshi A (2002) Anxiety-related behaviors in cholecystokinin-A,B, and AB receptor gene knockout mice in the plus-maze. Neurosci Lett 335 115-118... 

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

Cholecystokinin CCK-A receptor, 33-residue peptide Modulate digestion Solution-phase and... 

Path A leads to tryptophan derivatives (116), some of which are potent cholecystoki-nin antagonists (73). Some quinazolinone derivatives (117) of disconnection pathway B showed extremely high potency and excellent selectivity as cholecystokinin-B receptor sub-type ligands (44). A combination of X-ray crystallography and computational chemistry was used in the decision-making process in the bond disconnection (44) and in the design cf the specific target molecules. 

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