ibs

Propantheline bromide (Pro-Banthine) competitively antagonizes acetylcholine activity mediated by muscarinic receptors at neuroeffector sites on smooth muscle and exocrine gland cells. Propantheline Bromide is the bromide salt form of propantheline, a quaternary ammonium compound structurally related to belladonna alkaloids. An aspartic acid residue present in the N-terminal portion of the third transmembrane helix of the muscarinic receptor is believed to form an ionic bond with the tertiary or quaternary nitrogen of the antagonist. Antagonism leads to a reduction of exocrine glands secretions and to relax the bronchial muscle and reduce tone and motility of intestinal smooth muscle.

Dicyclomine hydrochloride is a muscarinic antagonist used as an antispasmodic and in urinary incontinence.

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.

GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM

IBS008738 is an effective TAZ activator that stabilises TAZ and increases unphosphorylated TAZ levels in C2C12 cells, upregulates MyoD-dependent gene transcription, promotes muscle repair in injury models, and prevents muscle atrophy.

BIBS-222, a nonpeptide angiotensin II (Ang II) receptor antagonist, appears to be an effective antihypertensive in the model of the renal hypertensive rat.

BIBS 39 is a novel nonpeptide angiotensin II (AII) receptor antagonist.

Vibsanin A, an activator of protein kinase C (PKC) and an inhibitor of HSP90, demonstrates anti-proliferative effects on human cancer cell lines.

Vibsanin C is a natural product of Viburnum, Caprifoliaceae. The catalog number is TN5231 and the CAS number is 74690-89-4. Vibsanin C can be used as a reference standard.

Renzapride (BRL 24924) is a mixed 5-hydroxytryptamine type 4 (5-HT4) agonist and 5-HT3 receptor antagonist.Renzapride can be used in the study of constipation-predominant irritable bowel syndrome (C-IBS).

Relenopride (YKP 10811) is a selective 5-HT4 receptor agonist that promotes intestinal motility and is used in the study of intestinal disorders.

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.

Linaclotide, developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation, is a potent and selective guanylate cyclase C agonist.

SSR-241586 is a neurokinin receptors antagonist,and is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).

TD-2749 is a selective 5-HT4 agonist discovered by Theravance through multivalent compound design as part of a compound discovery project aimed at finding new treatments for gastrointestinal motility disorders. It is primarily used to treat chronic constipation, constipation-predominant irritable bowel syndrome (C-IBS), opioid-induced constipation, functional dyspepsia, and diabetic gastroparesis.

(S)-Ramosetron ((S)-YM060 free base) is an orally active 5-HT3 receptor antagonist. It holds potential for studies related to conditions associated with nausea, vomiting, and irritable bowel syndrome (IBS).

ATB-429 is a mesalazine derivative capable of releasing H2S, demonstrating significant analgesic and anti-inflammatory effects in an irritable bowel syndrome (IBS) model. By releasing hydrogen sulfide (H2S), ATB-429 modulates hypersensitivity induced by colorectal distension in healthy and post-colitis rats. It alleviates abdominal withdrawal responses and inhibits spinal c-Fos mRNA expression, indicating its potential to relieve pain associated with gastrointestinal inflammation. Furthermore, ATB-429 downregulates mRNA expression of colonic cyclooxygenase-2 (COX-2) and IL-1β, an effect not observed with mesalazine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, evidenced by the reversal of ATB-429's effects with glibenclamide. These findings suggest that ATB-429 may offer therapeutic benefits for treating inflammatory pain-related bowel conditions.

Alosetron, a 5-HT3 antagonist, is used for the management of severe diarrhea-predominant irritable bowel syndrome (IBS) in women only.

Tiropramide is an antispasmodic drug. It also useful to inhibit the contractile response of the urinary bladder and in managing abdominal pain in IBS.

Cilansetron Hydrochloride can be used for irritable Bowel Syndrome (IBS) with Diarrhea Predominance.

Fenchone (AI3-00736) is a plant-derived monoterpene with anti-inflammatory, antioxidant, wound healing, antidiarrheal, antifungal, anti-injurious, and bronchodilator activities and is used in the study of Irritable Bowel Syndrome (IBS-C).

MM 419447 is a guanylate cyclase-C agonist, and it is a metabolite of linaclotide. This compound, MM 419447, shows promise in the field of irritable bowel syndrome with constipation (IBS-C) research.

Asimadoline (EMD-61753) is a proprietary small molecule therapeutic, originally discovered by Merck KGaA of Darmstadt, Germany. Asimadoline was originally developed to treat peripheral pain such as arthritis. Asimadoline is an orally administered agent that acts as a kappa opioid receptor agonist. It has shown encouraging clinical efficacy for the treatment of IBS in a barostat study in IBS patients and has the potential for treating other gastrointestinal diseases.

Tegaserod is an orally available 5-HT4R agonist and 5-HT2B receptor antagonist with inhibitory effects on various 5-hydroxytryptamine receptors. Tegaserod has antitumor activity and is used in the treatment of irritable bowel syndrome (IBS).