gastric ulcer

Cetraxate hydrochloride (DV10062) is an oral gastrointestinal medication. It has a cytoprotective effect.

CJ-42794 (CJ-042794) is a selective antagonist of the prostaglandin E receptor subtype 4 (EP4), inhibiting [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5. It exhibits a binding affinity that is at least 200-fold more selective for the human EP4 receptor than for other human EP receptor subtypes (EP1, EP2, and EP3) (IC50: 8.5 (pKi)).

BTM-1086 is a potent gastric secretory inhibitor and an anti-ulcer agent.

Bermoprofen (AD-1590) is an orally active non-steroidal anti-inflammatory compound with analgesic properties, utilized in gastric ulcer studies.

Saviprazole (Hoe-731), a proton pump inhibitor, is used potentially for treatment of gastric ulcer.

Aspirin is an orally active, selective, and irreversible inhibitor of COX-1 and COX-2 with IC₅₀ values of 5 and 210 μg/mL, respectively. It induces apoptosis, inhibits NF-κB activation and platelet prostaglandin synthesis, thereby preventing thrombosis. Additionally, it acts as a histone deacetylase inhibitor that upregulates p21, exhibiting anti-inflammatory, antipyretic, analgesic, and anti-platelet aggregation activities. Aspirin is commonly used to induce gastric ulcer models.

Indomethacin is an orally active nonsteroidal anti-inflammatory drug (NSAID) that non-selectively inhibits cyclooxygenase enzymes COX-1 and COX-2, with IC₅₀ values of 18 nM and 26 nM, respectively. It exhibits good blood-brain barrier permeability and shows significant anti-inflammatory, anti-tumor, and anti-infective activities. Indomethacin is widely used in research related to cancer, inflammation, and viral infections, and is also commonly used to induce gastric ulcer models in animals.

Reserpine (Serpalan) is an alkaloid isolated from the root of Rauwolfia serpentina. As an inhibitor of vesicular monoamine transporter 2 (VMAT2), it suppresses the uptake of norepinephrine into storage vesicles, leading to depletion of catecholamines and serotonin in central and peripheral nerve terminals. It has antihypertensive and antipsychotic effects and can be used to induce gastric ulcer and depression models.

Rebamipide (OPC12759) is a quinolinone derivative with anti-ulcer and anti-inflammatory activities. Rebamipide induces cyclooxygenase 2 (COX2) synthesis which results in an increase in endogenous prostaglandin synthesis in the gastric mucosa. This agent also inhibits H. pylori-induced production of tumor necrosis factor (TNF) alpha and subsequent inflammation of the gastric mucosa. In addition, rebamipide scavenges oxygen-derived free radicals that potentially cause mucosal injury, and stimulates prostaglandin EP4 receptor gene expression followed by mucous secretion, thereby enhancing the gastric mucosal defense.

Vonoprazan Fumarate (TAK438) , a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumarate (TAK438) inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.

Histamine dihydrochloride (Ceplene) is the dihydrochloride salt form of histamine, an endogenous metabolic product. Histamine is an organic nitrogen-containing compound with diverse biological activities. It acts as a potent stimulator of gastric acid secretion, a bronchial smooth muscle constrictor, and a vasodilator, as well as a neurotransmitter with central nervous system activity. It is commonly used to induce gastric ulcer models in research.

Irsogladine (Dicloguamine) is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.

Troxipide (Aplace), a new-type systemic non-antisecretory gastric cytoprotective agent, which is mucus-secreting, anti-ulcer, and anti-inflammatory properties irrespective of pH of stomach or duodenum.

HPi1 is a selective and orally active antimicrobial against Helicobacter pylori (IC50: 0.24 μM and a MIC of 0.08-0.16 μg/mL). HPi1 is inactive against other Xaliproden, including the gut commensals, Lactobacillus reuteri, Lactobacillus casei, and Bifidoba

Roxatidine Acetate hydrochloride (HOE 760) is a specific and competitive histamin H2-receptor antagonist. It inhibits gastric acid secretion and ulcer formation.

Roxatidine acetate is an anti-ulcer agent and histamine antagonist that inhibits gastric acid secretion. Compared to other similar drugs, Roxatidine acetate has an improved safety profile, in part because lower doses of roxatidine acetate are therapeutica

Levocarnitine propionate (L-Propionylcarnitine) is a propionyl-coenzyme A (Pro-CoA) derivative with anti-ischemic effects and high affinity for muscle L-carnitine transferase. Levocarnitine propionate enhances substrate oxidation and mitochondrial respiration in the heart of diabetic rats, reduces gastric ulcer area, induces mucosal recovery, and can be used to study acute respiratory distress syndrome and chronic gastric ulcers in Alzheimer's disease.

5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole, a gastric proton-pump inhibitor used to treat various peptic diseases. Lansoprazole is metabolized through CYP2C19, resulting in the formation of 5-Hydroxylansoprazole[1][2].

SCH28080 is a reversible and K+-competitive inhibitor of gastric H+/K+-ATPase with an IC50 value of 20 nM (rabbit microsomal membrane).SCH28080 is a potent inhibitor of acid secretion in vivo with anti-ulcer activity, anti-secretory and cytoprotective activity.

JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.

Mezolidon (KM-1146) is a compound with anti-ulcer activity that operates by strengthening the defensive mechanisms of the gastric mucosa. It achieves this, in part, by enhancing and sustaining blood flow to the gastric mucosa and by safeguarding the gastric mucosal potential difference. Mezolidon is applicable in research focused on gastric mucosal protection.

Eprazole trisulfide dimer is a trisulfide dimer of Ilaprazole. Ilaprazole is an orally active proton pump inhibitor that irreversibly inhibits the H⁺/K⁺-ATPase in a dose-dependent manner, with an IC50 of 6 μM in rabbit parietal cell preparations. Eprazole trisulfide dimer is applicable in gastric ulcer research.

Cinitapride (Blaston) is a gastroprokinetic agent. It slows the actions of the muscles to reduce the symptoms of conditions such as acid reflux, delayed gastric emptying, and ulcer dyspepsia. Cinitapride acts as an antagonist of the 5-HT2 receptors and as an agonist of the 5-HT1 and 5-HT4 receptors.

Sucrose octasulfate, a sulfated oligosaccharide derivative, functions as an inhibitor of matrix metalloproteinases (MMPs). This compound stimulates somatostatin-like immunoreactivity (SLI) release from the stomach by directly targeting D cells in the gastric mucosa. By releasing endogenous gastric somatostatin, sucrose octasulfate promotes ulcer healing. It serves as a pharmaceutical excipient, significantly enhancing wound closure in neuroischemic diabetic foot ulcers and venous leg ulcers. Additionally, sucrose octasulfate is applicable in research related to chronic wound healing.