diarrhea

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.

BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV) with an EC50 of 1.8 μM, directly binding to a hydrophobic pocket of the BVDV RdRp, and demonstrating antiviral activity against BVDV resistant to NNI thiosemicarbazone (TSC).

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.

Oxazolone is a haptenating agent that can induce models of acute or chronic colitis and atopic dermatitis. It activates Th1 Th2 responses, leading to weight loss and diarrhea, and the resulting inflammation can be alleviated by anti-IL-4 antibodies, anti-TNF-α antibodies, or IL-13R2α-Fc fusion proteins. It is also suitable for studying gene expression related to inflammatory bowel disease in zebrafish.

Aligeron, a non-selective prostaglandin (PG) antagonist, inhibits PGF2α- and PGE2-induced blood pressure decreases in cats and can prevent PGF2α-induced diarrhea in mice and PGE2-induced paw edema in rats. Additionally, Aligeron is recognized for its antioxidant-protective effect against vascular complications.

GS-6620 PM is a derivative of GS-6620, an orally administered anti-hepatitis C virus polymerase inhibitor and a novel potent C-nucleoside adenine analogue monophosphate prodrug.GS-6620 has limited activity against other viruses and maintains only partial activity against the closely related bovine viral diarrhea virus (EC50, 1.5 μM).

SLC26A3-IN-1 is an inhibitor of the anion-exchange protein SLC26A3 with an IC50 value of 340 nM. SLC26A3, a solute carrier (SLC) protein and member of the SLC26 family, exhibits a wide range of anionic specificities for chloride, bicarbonate, sulfate, and oxalate. Downregulated in adenomas (DRA), SLC26A3 is involved in intestinal absorption of chloride and oxalate and is associated with chloride-losing diarrhea.

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.

Racecadotril (Acetorphan) has been investigated for the basic science and treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis.

Diacerein (Fisiodar) is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including sevre diarrhea [L780]. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.

Isosteviol ((-)-Isosteviol), a common natural sweetener, belongs to tetracyclic diterpene glycosides. The pharmacology researches have suggested that stevioside and its hydrolysis products, steviol, isosteviol and steviolbioside, have many biological activities, such as reducing blood glucose, lowering blood pressure, anti-inflammation, anti-tumor, anti-diarrhea, antibacterium, immunoregulation, etc.

2-Methylsuccinic acid (Pyrotartaric Acid) is a normal metabolite found in human fluids. Increased urinary levels of 2-Methylsuccinic acid (Pyrotartaric Acid) (together with ethylmalonic acid) are the main biochemical measurable features in ethylmalonic encephalopathy, a rare metabolic disorder with an autosomal recessive mode of inheritance that is clinically characterized by neuromotor delay, hyperlactic acidemia, recurrent petechiae, orthostatic acrocyanosis, and chronic diarrhea.

Fidaxomicin (Tiacumicin B) is a semisynthetic macrolide antibiotic used to treat Clostridium difficile-associated diarrhea in adults. Fidaxomicin has minimal systemic absorption and has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent, acute liver injury.

Pinaverium bromide is an calcium channel blocker with Antispasmodic and effectively relieves pain, diarrhea and intestinal discomfort.

AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. It inhibits twitch contraction of the ileum and colon with IC50 values of 45.71 nM and 0.076 nM, respectively. AM9405 significantly slowed mouse intestinal motility under physiological conditions and reversed hypermotility, reducing pain in mouse models that mimic symptoms of functional GI disorders, such as stress-induced diarrhea and writhing test.

Loperamide D6 hydrochloride, a deuterium-labeled variant of Loperamide hydrochloride, acts as an opioid receptor agonist utilized for diarrhea treatment.

KDU731 is a promising drug candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety. KDU731is an orally active C. parvum inhibitor of PI4K (IC50: 25 nM). KDU731 blocks Cryptosporidium infection in vitro and in vi

Suclofenide is a benzenesulfonamide derivative that acts as an anticonvulsant and antiepileptic agent. In preclinical models, it showed potent anticonvulsant activity against electroshock and pentylenetetrazole-induced convulsions in mice. Sublethal toxicity was demonstrated by lethargy, myoclonic jerks and diarrhea.

Aminopentamide (also known as Dimevamide) is an anticholinergic compound primarily used to treat vomiting and diarrhea in dogs and cats, by acting as an antispasmodic on smooth muscles.

Acetyl tannic acid is an astringent (intestinal) used primarily in foals, calves, and dogs to treat diarrhea.

Crofelemer (Provir) is an orally active antidiarrheal agent. It targets the cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CACC), which are responsible for chloride and fluid secretion in the gastrointestinal tract. Crofelemer is applicable for research in diarrhea-related conditions.

FGFR2 3-IN-2 (compound 10) is an orally active inhibitor targeting FGFR2 and FGFR3. It exhibits IC50 values of 3.7 nM for FGFR2 and 31.2 nM for FGFR3, with a pre-incubation time of 1 hour. FGFR2 3-IN-2 demonstrates selectivity over FGFR1 4 and other kinases, and does not cause diarrhea or increased serum phosphate in vivo. In the SNU-16 gastric cancer model, FGFR2 3-IN-2 can induce tumor stasis or regression.

Anti-PEDV agent 1 (Compound D39) is a potent inhibitor of porcine epidemic diarrhea virus (PEDV) with an EC50 value of 0.09 μM. By modulating intracellular Ca2+ homeostasis, it obstructs the early internalization of PEDV during the viral entry stage. Anti-PEDV agent 1 shows promise for use in PEDV infection research.

SCUT1-2 is a bifunctional antibacterial agent with good oral bioavailability in mice (F=56.8%). It effectively kills the vegetative cells of C. difficile with a MIC of 0.06-0.50 μg/mL and inhibits spore germination in vitro. SCUT1-2 alleviates weight loss and diarrhea symptoms caused by C. difficile infection (CDI) in mice and prevents recurrence.