Last update 01 Nov 2024

H+/K+ ATPase x CCK receptor

Last update 01 Nov 2024

Basic Info

Related Targets

H+/K+ ATPaseCCK receptor

Drugs associated with H+/K+ ATPase x CCK receptor

SK&F-96067

Target

CCK receptor x H+/K+ ATPase

Mechanism

CCK receptor antagonists [+1]

Active Org.

Smithkline Beecham Pharmaceuticals Ltd.

Originator Org.

GSK Plc

Active Indication

Gastrointestinal Diseases

Inactive Indication

Peptic Ulcer [+1]

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with H+/K+ ATPase x CCK receptor

100 Translational Medicine associated with H+/K+ ATPase x CCK receptor

0 Patents (Medical) associated with H+/K+ ATPase x CCK receptor

Literatures (Medical) associated with H+/K+ ATPase x CCK receptor

01 May 2024·Journal of Ethnopharmacology

Protective effects of an alcoholic extract of Kaempferia galanga L. rhizome on ethanol-induced gastric ulcer in mice

Article

Author: Liu, Haifeng ; Zhou, Xun ; Zhang, Wenrui ; Zhang, Hui ; Zhang, Yingying ; Su, Tianli ; Zou, Yuanfeng ; Zhao, Xinhong ; Yin, Zhongqiong ; Li, Lixia ; Chen, Yaqin ; Song, Xu ; Fu, Yuping ; Wang, Juan ; Hu, Yilong

ETHNOPHARMACOLOGICAL RELEVANCEThe rhizome of Kaempferia galanga L., a medicinal and edible Plant, was widely distributed in many Asian and African counties. It has been traditionally used to treat gastroenteritis, hypertension, rheumatism and asthma. However, there is a lack of modern pharmacology studies regarding its anti-gastric ulcer activity.AIM OF THE STUDYThe objective of this study is to investigate the protective effects of an extract from K. galanga L. rhizome (Kge) and its active components kaempferol and luteolin on ethanol-induced gastric ulcer.MATERIALS AND METHODSThe kge was prepared by ultrasonic-assisted extraction, and the contents of kaempferol and luteolin were determined by HPLC. The mice were randomly divided into seven groups: blank control (0.5 % CMC-Na; 0.1 mL/10 g), untreatment (0.5 % CMC-Na; 0.1 mL/10 g), Kge (100, 200 and 400 mg/kg), kaempferol (100 mg/kg) and luteolin (100 mg/kg) groups. The mice were treated intragastrically once daily for 7 days. At 1 h post the last administration, the mice in all groups except the blank control group were intragastrically administrated with anhydrous alcohol (0.1 mL/10 g) once to induce gastric ulcer. Then, fasting was continued for 1 h, followed by sample collection for evaluation by enzyme-linked immunosorbent assay and real-time reverse transcription polymerase chain reaction assay.RESULTSThe contents of kaempferol and luteolin in Kge were determined as 3713 μg/g and 2510 μg/g, respectively. Alcohol induced severely damages with edema, inflammatory cell infiltration and bleeding, and the ulcer index was 17.63 %. After pre-treatment with Kge (100, 200 and 400 mg/kg), kaempferol and luteolin, the pathological lesions were obviously alleviated and ulcer indices were reduced to 13.42 %, 11.65 %, 6.54 %, 3.58 % and 3.85 %, respectively. In untreated group, the contents of Ca²⁺, myeloperoxidase, malondialdehyde, NO, cyclic adenosine monophosphate and histamine were significantly increased, while the contents of hexosamine, superoxide dismutase, glutathione peroxidase, and prostaglandin E2 were significantly decreased; the transcriptional levels of IL-1α, IL-1β, IL-6, calcitonin gene related peptide, substance P, M3 muscarinic acetylcholine receptor, histamine H2 receptor, cholecystokinin 2 receptor and H⁺/K⁺ ATPase were significantly increased when compared with the blank control group. After pre-treatment, all of these changes were alleviated, even returned to normal levels. Kge exhibited anti-gastric ulcer activity and the high dose of Kge (400 mg/kg) exhibited comparable activity to that of kaempferol and luteolin.CONCLUSIONThe study showed that K. galanga L., kaempferol, and luteolin have protective effects against ethanol-induced gastric ulcers. This is achieved by regulating the mucosal barrier, oxidative stress, and gastric regulatory mediators, as well as inhibiting the TRPV1 signaling pathway and gastric acid secretion, ultimately reducing the gastric ulcer index.

20 Jul 2023·Veterinary sciences

Exploring the Differential Expression of a Set of Key Genes Involved in the Regulation and Functioning of the Stomach in the Post-Weaned Pig.

Article

Author: Connolly, Kathryn Ruth ; O'Doherty, John V ; Ryan, Marion ; Kiernan, Dillon P ; Sweeney, Torres

Despite playing a key role in digestion, there is only a broad characterization of the spatiotemporal development of the three glandular regions of the stomach (cardiac, fundic and pyloric) in the weaned pig. Hence, the objective of this experiment was to explore the differential expression (DE) of a panel of key genes within the three glandular regions of the stomach. Eight pigs were sacrificed at d 8 post-weaning, and three mucosal samples were collected from each stomach's glandular regions. The expression of a panel of genes were measured using QPCR. The true cardiac gland region was characterized by increased expression of PIGR, OLFM4, CXCL8 and MUC2 relative to the two other regions (p < 0.05). The fundic gland region was characterized by increased expression of ATP4A, CLIC6, KCNQ1, HRH2, AQP4, HDC, CCKBR, CHIA, PGA5, GHRL and MBOAT4 compared to the two other regions (p < 0.05). The pyloric gland region was characterized by exclusive expression of GAST (p < 0.05). A transition region between the cardiac and fundic region (cardiac-to-oxyntic transition) was observed with a gene expression signature that resembles a cross of the signatures found in the two regions. In conclusion, unique gene expression signatures were identifiable in each of the glandular regions, with a cardiac-to-oxyntic transition region clearly identifiable in the post-weaned pigs' stomachs.

05 Oct 2022·Journal of Agricultural and Food Chemistry

Plant-Based Meat Analogues Weaken Gastrointestinal Digestive Function and Show Less Digestibility Than Real Meat in Mice

Article

Author: Xie, Yunting ; Shan, Kai ; Xu, Xinglian ; Cai, Linlin ; Zhou, Guanghong ; Li, Chunbao ; Huang, Zhiji

Real meat and plant-based meat analogues have different in vitro protein digestibility properties. This study aims to further explore their in vivo digestion and absorption and their effects on the gastrointestinal digestive function of mice. Compared with the real pork and beef, plant-based meat analogues significantly reduced the number of gastric parietal cells, the levels of gastrin/CCKBR, acetylcholine/AchR, Ca²⁺, CAMK II, PKC, and PKA, the activity of H⁺, K⁺-ATPase, and pepsin, the duodenal villus height, and the ratio of villus height to crypt depth and downregulated the expression of most nitrogen nutrient sensors. Peptidomics revealed that plant-based meat analogues released fewer peptides during in vivo digestion and increased the host- and microbial-derived peptides. Moreover, the real beef showed better absorption properties. These results suggested that plant-based meat analogues weaken gastrointestinal digestive function of mice, and their digestion and absorption performance in vivo is not as good as the real meat.

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