devazepide

..CART peptide likely acts upon either peripheral or central regulators of pancreatic secretory function that are distant from the acinar unit...

..The selective CCK(A) receptor antagonists, devazepide and lorglumide, effectively attenuated the EB-induced inhibition of gastric emptying and gastrointestinal ..

..However, administration of atosiban alone had no effect on gastric emptying. Devazepide (3 mg x kg(-1)), a selective CCKA receptor antagonist, effectively attenuated the OT-induced inhibition of ..

..Serotonin inhibits food intake, and postprandial serotonin release is increased after total gastrectomy. Serotonin might contribute to early satiety and loss of body weight after total gastrectomy...

..These results indicated that elevated CCK may contribute to anorexic and anxious phenotype of PP overexpressing mice...

..Our results also suggest that the stimulatory effect of GLP-2 on SMA blood flow is NO-dependent and mediated via intrinsic, non-cholinergic enteric neurons...

..The suppression of food intake by beta-conglycinin peptone was abolished by an intravenous injection of devazepide, a selective peripheral CCK receptor antagonist...

..The present study assessed the dose-dependency of this response and the effect of two selective CCK(1) receptor antagonists, with different abilities to cross the blood-brain barrier (BBB), on PEG-CCK(9)-induced anorexia...

..CONCLUSIONS: CCK8 may regulate PKC activities in rat cerebral cortex through CCKB receptor...

..Thus, in our experimental conditions, i.e., within 30-50 days post-N. brasiliensis infection, we observed an enhancement of the anorectic effect of exogenous CCK involving mast cell degranulation and histamine...

..To investigate the central regulation of food intake by quantifying neuron activation of the nucleus of the solitary tract (NTS) after injection of cholecystokinin (CCK) or food intake in gastrectomized rats...

..A second study evaluated the effect of a CCK-1 receptor antagonist, devazepide (0...

..The proposed binding modes of GI5269 and GI0122 are supported by the structure-activity relationship of analogues and mutagenesis data for the CCK(1)-R selective antagonist L-364,718...

..The CCK-A receptor antagonist, devazepide (which reverses protein-induced food intake suppression), when given at 0.25 mg/kg, i.p...

..CONCLUSIONS: Duct-like pancreatic epithelial cells in vitro and ductal complexes in vivo express gastrin/CCK-B receptors and proliferate in response to gastrin...

Type A CCK receptor (CCKAR) antagonists differing in blood-brain barrier permeability [devazepide penetrates; the dicyclohexylammonium salt of Nalpha-3-quinolinoyl-d-Glu-N,N-dipentylamide (A-70104) does not] were used to test the ..

..The effect of oleate was abolished by the CCK-A receptor antagonist Devazepide (0...

The effects of different cholecystokinin (CCK) receptor antagonists (devazepide and L365,260) on cocaine or stress-induced reactivation of cocaine conditioned place preference (CPP) were investigated in rats...

..1 mg/kg devazepide (a peripheral CCK-A-receptor antagonist) administered intraluminally and intravenously, respectively...

..Taken together with the results of the food intake studies, this suggests that activation of CCK-A receptors is involved in the postprandial activation of NTS neurons and in the regulation of food intake...

..These results suggest that endogenous CCK, acting on CCK-A receptors, may play a key role in eliciting postprandial sleep...

..These results suggest that nicotine can exert its anorexic effect via an increase in gastric vagal afferent activity which is caused by enhanced release of both cholecystokinin and prostaglandins...

..However, at the point of maximal injury, the inflammatory response became pronounced, largely due to the role played by activated T lymphocytes...

..b>Devazepide penetrates the blood-brain barrier; A-70104, the dicyclohexylammonium salt of N alpha-3-quinolinoyl-D-Glu-N,N-..

..These results indicate that the beta-conglycinin beta 51-63 fragment is the bioactive appetite suppressant in beta-conglycinin, and multiple arginine residues in the fragment may be involved in this effect...

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..was significantly reduced by 77 and 55%, respectively, in rats treated with the CCK(1) receptor blocker devazepide or after functional vagal deafferentation by perineural capsaicin treatment...

..Findings are consistent with the notion that endogenous CCK plays a key role in the short-term control of ethanol intake in hamsters...

..the pressor response and bradycardia elicited by sCCK-8 were reduced by the selective CCKA receptor antagonists, devazepide (0.5-50 nmol kg-1) and lorglumide (1-7 mumol kg-1)...

..agonists (CCK-8, CCK-4, gastrin-17), whereas CCK-CHR showed higher affinity for the CCK-A receptor antagonist, devazepide, than for the CCK-B receptor antagonist, L-365,260...

..At dark onset, non-food-deprived rats received a bolus injection of devazepide (2...

..These studies delineate the presence of distinct CCK-A and CCK-B/gastrin receptors on canine fundic D-cells.(ABSTRACT TRUNCATED AT 250 WORDS)..

..Camostat also increased Fos-LI in the DVC. Experiment 2: Pretreatment with devazepide, a specific CCK(1) receptor antagonist abolished camostat-induced Fos-LI in the submucosal plexus and the DVC...

..They open the way to potential design of either a new family of MAP kinase inhibitors from CCK1 receptor ligand structures or new CCK1 receptor ligands based on p38 MAP kinase inhibitor structures...

..Moreover, devazepide prevented this suppression, indicating this increased sensitivity was mediated by CCK-1 receptors...

..The selective CCK(1) receptor antagonists, devazepide and lorglumide, effectively attenuated the OT-induced inhibition of gastric emptying and gastrointestinal ..

..plexus (GPI) have been characterized by use of peptide agonists and the non-peptide antagonists, lorglumide, devazepide and L-365,260. 2...

..1%), devazepide (10(-8) M: +19.4%; 10(-7) M: +30.0%) and SR-27897 (10(-10) M: +21.8%, 10(-8) M: +47.0%, P<0.05, n=8)...

..6 x 10(-5) M) and the CCK-A receptor antagonist devazepide (1...

..The evidence presented here expands our understanding of cellular mechanisms for CCK-mediated anti-analgesic and anxiogenic actions in the PAG...

..Domperidone, (+)SCH 23390, devazepide, PK 11-195 and flumazenil did not have effect on the action of Tyr-MIF-1...

..peptides is mediated by a CCK-dependent mechanism, we examined the ability of the CCK-A receptor antagonist, devazepide, to block the inhibition of saline gastric emptying produced by BN, GRP18-27 and NMB...

..of CCK receptor ligands (CCK-8S > CI988 > PD 135158 > pentagastrin > CCK-8NS > L-365,260 > CCK-4 > LY 288513 > devazepide > A71378 > lorglumide) was found to be in excellent agreement with CCK-B receptor pharmacology described in ..

..Differences in the anxiety levels of rats in summer and winter, and the role of CCK in these behavioural alterations, were also examined...

..In the present study we measured plasma CCK concentrations in acute experimental pancreatitis (AEP) in the rat, and evaluated the role of circulating CCK levels on the initial pancreatic damage in pancreatitis...

..Cholecystokinin CCK(1) receptor antagonists, lorglumide (10 mg/kg, i.v.) and devazepide (0.5 mg/kg, i.v...

..We suggest that endogenous OT regulates gallbladder phasic contraction through specific OT receptor. This effect is independent of the peripheral CCK and M receptors...

..Similar to CCK-8, devazepide, a specific CCK(1) receptor antagonist, and not L365,260, a specific CCK(2) receptor antagonist, attenuated the ..

..The selective CCK-A antagonist L-364,718 (Devazepide) antagonized both types of contraction with a pKB of 10.10 and 9.95, respectively...

..5. The selective CCKA antagonist, devazepide, was inactive at up to 300 mumol kg-1 i.p. against the three stimulants of acid secretion. 6...

..Alternatively, animals were pretreated with the CCK1 receptor antagonists devazepide and lorglumide or the 5-HT3 antagonist MDL-72222 before SO-SBTI administration...

..inhibited gastric emptying of a chow meal in wild-type but not A-IV(-/-) mice andCCK(1)R receptor blockade with devazepide (10 microg/100 g), abolished PYY(3-36)-induced inhibition of gastric emptying...

..Additional mechanisms or hormones, such as secretin, may play a role in modulating later exocrine pancreas responses to PHA...

..on feeding in rats, the influence of ip injections of 250 microg of the selective CCK(A) receptor antagonist devazepide was then tested...

..To investigate the effects of sulfated cholecystokinin octapeptide (CCK-8S) on the contractile activity of guinea-pig proximal colon...

..We have investigated the effects of apelin peptides on duodenal bicarbonate secretion in vivo and the release of cholecystokinin (CCK) from acutely isolated mucosal cells and the neuroendocrine cell line STC-1...

..The biological, pharmacological, and fluorescence properties of this reagent are described, and proof-of-concept is provided in a fluorescence polarization assay utilizing this fluorescent benzodiazepine ligand...

..The effects of CCK(A) and CCK(B) receptor antagonists (devazepide and CI-988, respectively) were examined using mouse anxiety tests (elevated-plus maze and light-dark box) and ..

..In this study, the effect of coadministration of the selective CCK receptor antagonists devazepide and L-365,260 (for selectively blocking CCK1 and CCK2 receptors, respectively), on the effect of amphetamine on ..

..These findings reveal a role for gut CCK that lowers glucose production through a neuronal network and suggest that intestinal CCK resistance may contribute to hyperglycemia in response to high-fat feeding...

..In contrast, the CCK(1) receptor antagonist devazepide inhibited the nociceptive responses to formalin...

..Our results suggest that the pain-related neurons in the nPf have an important role in mediating EA analgesia. L-364,718 potentiates EA analgesia through the CCK-A receptor of PENs and PINs in the nPf...

..Male Wistar rats were pretreated with a specific CCK(1) receptor antagonist (devazepide; 1 mg kg(-1); i.p.) or vehicle; 30 min later they received LPS (100 μg kg(-1); i.p.) or saline injection...

..The CCK(A) receptor antagonist devazepide (500 microg/kg intravenous) inhibited motion responses evoked by intravenous CCK-8...

..Our findings indeed support that our "validated CCK1R model" could be used to study the intrinsic mechanism of CCK1R activation and design new ligands...

..The selective CCK(1) receptor antagonist devazepide was used to assess CCK mediation of the control of intake produced by particular sensory aspects of food, at the ..

..CCK1 receptor antagonist devazepide counteracted effect of CCK-8 in all three genotypes, whereas CCK2 receptor antagonist L-365, 260 showed ..

..to colonic preparations induced concentration-dependent contractions which were prevented by devazepide (CCK1 receptor antagonist), enhanced by GV150013 (CCK2 receptor antagonist) or N(omega)-nitro-L-arginine ..

..Combined administration of 1 mg/kg ondansetron (Ond) and 1 mg/kg devazepide (Dev) reversed 132 mM Polycose-induced suppression to the level of control intake and significantly attenuated ..

..We conclude that activation of the vagal afferent pathway and inhibition of gastric function in response to dietary lipid is partly dependent upon apo A-IV...

..Furthermore, the affinity of the chimaera for gastrin is essentially the same as the gastrin/CCK-B receptor, indicating that the six different amino acids probably do not contribute to peptide agonist binding...

..intragastric artery injection of urocortin 2 after CCK at a subthreshold dose, and the response was reversed by devazepide. These data establish a peripheral synergistic interaction between CCK and urocortin 1 or urocortin 2 to ..

..The selective CCK1 receptor antagonists, devazepide and lorglumide, effectively attenuated the oxytocin-induced inhibition of gastric emptying and gastrointestinal ..

..In this study, we investigated the ability of different doses of PEG-CCK9 to induce conditioned taste aversion (CTA) and satiety and identified the receptors involved in CTA induction...

..Here, we used a specific assay of allosteric ligand interaction to probe the mode of binding of devazepide, a prototypic benzodiazepine ligand...

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..plus CCK-B antagonist); lorglumide (CCK-A antagonist); PD 135,158 (CCK-B antagonist and weak CCK-A agonist); devazepide or L 364,718 (CCK-A antagonist); L 365,260 (CCK-B antagonist), and melatonin...

..It was concluded that PACAP27 and PACAP38 stimulate gallbladder motility in conscious dogs through a preganglionic cholinergic mechanism...

..Finally, three different speculations that might explain the fact that intraperitoneal L-365,260 increases food intake are discussed...

..study was to investigate the effects of cholecystokinin (CCK) CCK(A) and CCKB receptor antagonists SR 27897 B, devazepide, L 365260 and PD 135158 (CAM 1028) on exploratory behaviour in the elevated zero-maze in the rat...

..Our results suggest that glycoconjugates of zymogen granule membrane involved in CCK-regulated exocytosis contain N-acetylglucosamine and sialic acid residues whose quantities are regulated by CCK...

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..These results demonstrate that CCK-8S represents the minimum ligand requirement for both high affinity and full agonist activity at the human CCK-A receptor subtype...

..They do not support the singular importance of a peripheral action of CCK in determining satiety...

..All of these effects of SR146131 were inhibited by the CCK1 receptor antagonists SR27897B and devazepide, suggesting that the effects of SR146131 were entirely mediated by the CCK1 receptor...

..together with the evidence that another CCK-B receptor antagonist, L-365,260 (5 micrograms/kg) increased, while devazepide (a CCK-A receptor antagonist; 20 micrograms/kg) decreased non-REM sleep and total sleep time, support the ..

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..We conclude that CCK contributes to the MMC related alterations in the GB motor activity and is essential in cholinergic stimulation induced of the GB emptying but not in vagally induced duodenal and GB motility...

..abstract truncated at 250 words)..

..These results suggest that L-364,718 and CR1409 act as CCK-receptor antagonists, but dbcGMP has another inhibitory effect on pepsinogen secretion in addition to the effect as a CCK-receptor antagonist in guinea pig gastric chief cells...

..While CCK appears to be the primary modulator of gallbladder contraction after a fatty meal, no influence of CCK was detected in the interdigestive (fasting) state...

..b>Devazepide, a selective CCKA receptor antagonist, L-365,260 (3R(+)-N-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-..

..The soybean trypsin inhibitor and phenylalanine did not alter food intake. Devazepide, a cholecystokinin-A receptor antagonist, significantly decreased amylase release from the dispersed chicken ..

..The effect of CGRP on food intake was not antagonized by the cholecystokinin A receptor antagonist, L364,718. These studies suggest a role for CGRP as a satiating factor...

..CCK) to this, rats were injected with 1 mg/kg of the potent, selective CCK(A) receptor antagonist, devazepide, during diestrus, when meal size is maximal, and during estrus, when it is minimal...

..3-yl)-N'-( 3-methylphenyl) urea); a selective CCK-A receptor antagonist, devazepide (L-364,718); and cimetidine on gastric acid secretion induced by pentagastrin, histamine and bethanechol in ..

..v. administration of saline or devazepide, a CCK-A antagonist. Plasma PYY increased with fat (P < 0...

..of apo A-IV and determine that both of these responses are CCK-AR- dependent using the CCK-AR antagonist devazepide. A direct effect of Cck on vagal afferents innervating the gastro-duodenum will be determined by measuring ..

..Recent studies demonstrating that devazepide, a CCK-A receptor antagonist that penetrates the blood/brain barrier, stimulates feeding in a variety of species ..

..org) requests for information. Products and services will be offered to requesting investigators for a reasonable fee, enabling us to cost recover for distribution and to develop a self supporting repository operation within 4 years. ..

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..The name of the principal investigator/program director must be provided at the top of each printed page and each continuation page. RESEARCH GRANT ..

..These relationships allow leveraging of MMRRCsupport, resulting in expanded opportunities for, and benefit to, the MMRRC National Program and the biomedical and behavioral scientific research community. ..

..By enabling availability and access of such valuable mouse models to the entire research community, the UCD-MMRRC fosters and promotes the discovery of new diagnostics, treatments, and prevention strategies against human diseases. ..

..These relationships allow leveraging of MMRRCsupport, resulting in expanded opportunities for, and benefit to, the MMRRC National Program and the biomedical and behavioral scientific research community. ..

..By enabling availability and access of such valuable mouse models to the entire research community, the UCD-MMRRC fosters and promotes the discovery of new diagnostics, treatments, and prevention strategies against human diseases. ..

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..The work will be closely coordinated, and we expect this cooperative effort to be very productive. ..

..These relationships allow leveraging of MMRRC support, resulting in expanded opportunities for, and benefit to, the MMRRC National Program and the biomedical and behavioral scientific research community. ..

..8) Determine the tonic and phasic effects of estradiol on glutamate synaptogenesis in the brainstem by using immunocytochemical detection of synaptic proteins. ..

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