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.

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

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

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.

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,

Ecabapide (DQ-2511) is a novel gastrointestinal motility promoter that significantly enhances gastric emptying in SHRSP.Ecabapide activates cyclic GMP-dependent housekeeping Cl- channels in rabbit gastric wall cells.

BMS-903452 is a potent and selective GPR119 agonist with an EC50 of 14 nM, indicated for the treatment of acute and chronic rodent diabetes. GPR119 is mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. BMS-903452 shows no significant inhibitory effect on 9 cytochrome P450 enzymes (IC50 > 40 μM), does not activate PXR (EC50 > 50 μM), and is not toxic to liver (HEPG2) cell lines.

Norcisapride is a 5-hydroxytryptamine receptor 3 (5-HT3) and (5-hydroxytryptamine receptor 4 (5-HT4) dual agonist used for the treatment of gastrointestinal disorders, orofacial disorders, and otorhinolaryngologic disorders.

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80 2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.

Bismuth Subsalicylate (Bismuth subsalicylat) is the active ingredient in the popular medication Pepto-Bismol that is used to treat nausea, heartburn, indigestion, upset stomach, diarrhea, and other temporary discomforts of the stomach and gastrointestinal tract.

Alverine citrate (NSC 35459) is utilized in functional gastrointestinal disorders.

Ursodeoxycholic acid (UDCA) can be used to dissolve gallstones and reduce cholesterol absorption.

Clidinium bromide (Ro 2-3773) , a synthetic anticholinergic agent, has been shown in experimental and clinical researchers to have a pronounced antisecretory and antispasmodic effect on the gastrointestinal tract. It can inhibit muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites. It is used for the treatment of peptic ulcer disease and also to help relieve cramps or stomach spasms or abdominal due to colicky abdominal diverticulitis, pain, and irritable bowel syndrome.

Trimebutine (Mebutin) is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid agonist effects. It is marketed for the treatment of irritable bowel syndrome (IBS) and lower gastrointestinal tract motility disorders, with IBS being one of the most common multifactorial GI disorders. It is used to restore normal bowel function and is commonly present in pharmaceutical mixtures as trimebutine maleate salt form. Trimebutine is not an FDA-Approved Clinical drug, but it is available in Canada and several other international countries.

Proglumide (Binoside) is a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.

Doxylamine Succinate is a pyridine derivate histamine H1 antagonist with pronounced sedative properties. Doxylamine succinate (Decapryn) competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of the gastrointestinal smooth muscle, caused by actions of histamine on bronchial and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes.

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.