gastrointestinal

PEG300 (Polyethylene glycol 300) is a polymer formed from repeating units of ethylene glycol that is water soluble, low immunogenicity, and biocompatible. PEG300 is a neutral polymer with a molecular weight of 300.

Cephradine (Anspor) is a beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity.

Mepenzolate Bromide (Colibantil) is a muscarinic antagonist used to treat gastrointestinal conditions.

Rifaximin is an orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity. Rifaximin binds to the beta-subunit of bacterial DNA-dependent RNA polymerase, inhibiting bacterial RNA synthesis and bacterial cell growth.

Cisapride (R 51619) is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal peristalsis, increase gastric emptying and decrease esophageal reflux.

Tegaserod maleate (SDZ-HTF-919) is a 5-HT4 agonist manufactured by Novartis for managing irritable bowel syndrome and constipation. It was the only drug approved by the United States Food and Drug Administration for relieving abdominal discomfort, bloating, and constipation associated with irritable bowel syndrome. On March 30, 2007, the FDA requested that Novartis withdraw Zelnorm from the market due to alleged increased risks of heart attack or stroke associated with its use.

Mizagliflozin is an orally active, selective SGLT1 inhibitor with a Ki value of 27 nM for human SGLT1. Mizagliflozin is 303 times more selective for SGLT1 than for SGLT2. Mizagliflozin is an anti-diabetic drug that can improve postprandial blood sugar fluctuations and may have the potential to improve chronic constipation.

Methylnaltrexone bromide (MOA-728) is one of the newer agents of peripherally-acting μ-opioid antagonists. Methylnaltrexone bromide acts to reverse some of the side effects of opioid drugs such as constipation without affecting analgesia or precipitating withdrawals.

Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.

Isopropamide iodide is a long-acting anticholinergic drug used for peptic ulcers and other gastrointestinal disorders, and as a muscarinic receptor antagonist for diseases affecting cognition [including Alzheimer's disease].

1. Tiliroside (Tribuloside) shows anticarcinogenic activity. 2. Tiliroside shows hepatoprotective activity. 3. Tiliroside shows antioxidant and anti-inflammatory activity, can inhibit neuroinflammation in neurodegenerative disorders. 4. Tiliroside has anti-diabetic effect, are at least partially mediated through inhibitory effects on carbohydrate digestion and glucose uptake in the gastrointestinal tract. 5. Tiliroside and gnaphaliin are antioxidants against in vitro Cu(2+)-induced LDL oxidation in the same order of magnitude compared to that of the reference drug, probucol. 6. Tiliroside enhances fatty acid oxidation via the enhancement adiponectin signaling associated with the activation of both AMP-activated protein kinase and peroxisome proliferator-activated receptor α and ameliorates obesity-induced metabolic disorders.

Nirogacestat (PF 03084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).

Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist, exhibiting a pEC50 of 7.9 in mouse vas deferens and a Ki of 0.75 nM for rat forebrain membrane binding.

Lipopolysaccharides (LPS), derived from Escherichia coli O55:B5, are essential components of the outer membrane of Gram-negative bacteria. Composed of lipid A, a core oligosaccharide, and an O-specific polysaccharide, LPS exhibits strong immunogenicity. It activates immune cells via the TLR4 receptor, induces chemotactic cell migration and cytokine secretion, and helps maintain the integrity of the bacterial outer membrane, protecting against bile salts and lipid-based antibiotics. LPS is commonly used to establish inflammatory models, including arthritis, chronic obstructive pulmonary disease (COPD), acute respiratory distress syndrome (ARDS), and gastrointestinal disease models.

Deoxynivalenol (Vomitoxin) is a mycotoxin produced by Fusarium spp. of the single trichothecene family and is commonly found in contaminated food and feed.Deoxynivalenol crosses the intestinal mucosa via a cellular bypass at the tight junctions.Deoxynivalenol transporters are unaffected by inhibitors of P-glycoprotein (PgP) or multidrug resistance-associated protein (MRP). Deoxynivalenol commonly causes diarrhea, vomiting, and gastrointestinal inflammation in humans and animals.

5-HT2A antagonist 1 is a 5-HT2A receptor blocker that may be useful in treating gastrointestinal and circulatory disorders.

CP 96021 is a group of 5-HT1 receptors and 5-HT2 receptors antagonists that have anti-inflammatory properties and are non-non-self anti-ulcer compounds for the treatment of gastrointestinal tract and respiratory asthma.

Benzamide Derivative 1 Benzamide derivative with gastrokinetic activity.Benzamide Derivative 1 can be used in the study of gastrointestinal diseases.

AU-224 is an orally available benzamide derivative that is a potent gastrointestinal prokinetic.

DBIBB is a non-lipid agonist of specific lysophosphatidic acid (LPA2) type 2 G-protein-coupled receptor. It is a potentially active molecule for the treatment of acute radiation syndrome caused by high intensity gamma rays on hematopoietic and gastrointestinal systems. It is an intermediate in organic synthesis and drug research. DBIBB can be used to prepare various compounds that reduce gastrointestinal radiation syndrome, increase intestinal crypt survival and intestinal cell proliferation, and reduce cell apoptosis.

Sulopenem (CP-70429) is an orally active gastrointestinal-external cephalosporin antibiotic with broad-spectrum antibacterial activity. It inhibits Gram-positive and Gram-negative bacteria and can be used in bacterial infection research.

A-65186 is an A-type glutamatergic cholecystokinin (CCK) antagonist used to study inflammation and gastrointestinal tract injury.

Minesapride, a novel 5-hydroxytryptamine 4 (5-HT4) receptor partial agonist, is a potential gastrointestinal prokinetic agent for the treatment of irritable bowel syndrome with constipation.

Ursodeoxycholic acid sodium (Sodium Ursodeoxycholate) is a naturally occurring secondary bile acid with anti-inflammatory and cytoprotective activities. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors,