Effect of dexloxiglumide and spiroglumide, two new CCK‐receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo.

Scarpignato, Carmelo; Kisfalvi, I; D’Amato, Massimo; Varga, Gábor

doi:10.1111/j.0953-0673.1996.00411.x

Cited by 34 publications

(22 citation statements)

References 3 publications

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“…This effect involves activation of CCK1R, as evidenced by studies with antagonists in rats and humans (131,154,437,459,591). Reduction of gastric emptying by a specific CCK1R agonist is also consistent with a CCK1R-mediated mechanism (80).…”

Section: Stomachmentioning

confidence: 90%

Cholecystokinin and Gastrin Receptors

Dufresne

Seva²,

Fourmy³

2006

Physiological Reviews

422

418

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Cholecystokinin and gastrin receptors (CCK1R and CCK2R) are G protein-coupled receptors that have been the subject of intensive research in the last 10 years with corresponding advances in the understanding of their functioning and physiology. In this review, we first describe general properties of the receptors, such as the different signaling pathways used to exert short- and long-term effects and the structural data that explain their binding properties, activation, and regulation. We then focus on peripheral cholecystokinin receptors by describing their tissue distribution and physiological actions. Finally, pathophysiological peripheral actions of cholecystokinin receptors and their relevance in clinical disorders are reviewed.

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Section: Stomachmentioning

confidence: 90%

Cholecystokinin and Gastrin Receptors

Dufresne

Seva²,

Fourmy³

2006

Physiological Reviews

422

418

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“…In animals infusion of CCK delays gastric emptying by relaxing the proximal part of the stomach and stimulating the pyloric sphincter [24][25][26] ; the effect is mediated by interaction with CCK 1 receptors on endings of sensory fi bres of the vagus nerve [27] . Thus, CCK 1 receptors can be modulated to increase fasting gastric volume, which is important as the gastric volume plays a role in satiety control besides many other mechanisms.…”

Section: Stomachmentioning

confidence: 99%

CCK<sub>1</sub> Antagonists: Are They Ready for Clinical Use?

Peter

D’Amato²,

Beglinger

2006

Dig Dis

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Cholecystokinin (CCK) is a peptide hormone which is found both in the gastrointestinal tract throughout the human small intestine and nerves in the myenteric plexus of the enteric nervous system and in the central nervous system. This dual location constitutes the anatomical basis for this in functions as a hormone and a neurotransmitter implicated in the regulation of both systems. CCK regulates not only motor functions in the gastrointestinal tract like lower oesophageal sphincter relaxation, gastric secretion and emptying, gall bladder contractility and bile secretion into the duodenum, intestinal and colonic motility, but also sensory functions and plays a role in the regulation of food intake. These effects are mediated through selective receptors CCK₁ and CCK₂. Over the last few years, research has focused on understanding the role of CCK, its receptors with antagonists at the biological, pharmacological, clinical and therapeutic level. As far as the CCK₁ antagonists is concerned, important inroads have been made in the potential role of these antagonists in the treatment of GERD, IBS and pancreatitis. They have also shown encouraging results in sphincter of Oddi dysfunction and some gastrointestinal cancers. This review focuses on the recent ad vances of the biological role of CCK and their CCK₁ antagonists: their current basic and clinical status in gastroenterology, with particular emphasis on the potential therapeutic role of the CCK₁ antagonists and future research directions.

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“…(c) Cholecystokinin receptor antagonists such as loxiglumide and dexloxiglumide accelerate gastric emptying in some studies. The utility of such agents in gastroparesis remains to be determined [88] . (d) Sildenafil is a phosphodiesterase 5 inhibitor which has been shown to restore gastric emptying of liquids in an animal model of diabetes [89] .…”

Section: Pharmacological Therapymentioning

confidence: 99%

Gastroparesis: Current diagnostic challenges and management considerations

Waseem¹,

Moshiree²,

Draganov³

2009

WJG

143

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Gastroparesis refers to abnormal gastric motility characterized by delayed gastric emptying in the absence of mechanical obstruction. The most common etiologies include diabetes, post-surgical and idiopathic. The most common symptoms are nausea, vomiting and epigastric pain. Gastroparesis is estimated to affect 4% of the population and symptomatology may range from little effect on daily activity to severe disability and frequent hospitalizations. The gold standard of diagnosis is solid meal gastric scintigraphy. Treatment is multimodal and includes dietary modification, prokinetic and anti-emetic medications, and surgical interventions. New advances in drug therapy, and gastric electrical stimulation techniques have been introduced and might provide new hope to patients with refractory gastroparesis. In this comprehensive review, we discuss gastroparesis with emphasis on the latest developments; from the perspective of the practicing clinician.

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Effect of dexloxiglumide and spiroglumide, two new CCK‐receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo.

Cited by 34 publications

References 3 publications

Cholecystokinin and Gastrin Receptors

Cholecystokinin and Gastrin Receptors

CCK<sub>1</sub> Antagonists: Are They Ready for Clinical Use?

Gastroparesis: Current diagnostic challenges and management considerations

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