26095-59-0 Usage
Pharmacological effects
Otilonium bromide is an anticholinergic and antispasmodic drug. Its trade name is Siba Min. It can regulate the flow of calcium between intestinal smooth muscle extracellular and intracellular calcium pools. It is selective to gastrointestinal smooth muscle, and it has strong antispasmodic effect. It is applied to all motor function hyperthyroidism, and spasm reaction for different reasons and different parts as well as smooth muscle fibers pathological atrophy caused spasm reaction. It is also applied to the treatment of gastrointestinal distal intestine irritable bowel syndrome (IBS) or spastic pain, spastic colon, gastroenteritis, stomach, duodenum and esophagus disease, and endoscopic examination preparation (esophagoscopy, gastroscopy, ten finger colonoscopy and proctoscope). The experimental data show that the drug is absorbed very little by oral medication, and the most absorbed drug passed the biliary tract and were excreted via the stool.
The above information is edited by the lookchem of Kui Ming.
Toxicology
Acute toxicity: Non-lethal dose of oral administration to rats 1500mg/kg, to dogs is 1000mg/kg.
Chronic toxicity: experimental animals according to the program: 180 days of continuous oral administration, 11.44mg/kg/otilonium bromide. We found no abnormal changes in the results of blood biochemical and histological examination.
Teratogenicity: according to 11.44mg/kg, no embryonic and teratogenic toxicity to rats and rabbits in experiments.
Gene mutations: a large number of experiments have shown no mutagenic effect.
Side effects
Therapeutic doses of otilonium bromide doesn’t cause side effects, and it doesn’t cause atropine-like effect.
Precautions
Patients with glaucoma, prostatic hypertrophy, pyloric stenosis, pregnant or lactating women, and patients known allergic reaction to otilonium bromide should be used with caution.
Uses
Different sources of media describe the Uses of 26095-59-0 differently. You can refer to the following data:
1. Treatment of gastrointestinal spasm.
2. Inhibits platlet activating factor induced hypotension. Antispasmodic
3. Otilonium bromide is an antimuscarinic
4. Octylonium bromide is an antimuscarinic. Octylonium bromide is a platelet-activating factor antagonist as analgesic, anti-inflammatory, uterine contraction inhibiting, and anti-tumor agent.
m bromide is used as an antispasmodic.
5. antimuscarinic used as a spasmolytic agent
Description
Otilonium is an inhibitor of L-type (IC50 = 2.3 μM) and T-type calcium channels (IC50s = 0.8, 1.1, and 0.4 μM for Cav3.1, Cav3.2, and Cav3.3, respectively). It is also an antagonist of muscarinic acetylcholine receptors (mAChRs; IC50s = 0.054, 0.4, 0.222, and 0.156 μM for M1, M2, M4, and M5 muscarinic receptors, respectively) and the platelet activating factor (PAF) receptor (IC50 = 0.0552 μM). Otilonium inhibits the inward calcium current in isolated rat colonic smooth muscle cells (EC50 = 885 nM), an effect that can be blocked by the L-type calcium channel inhibitor nifedipine . It inhibits contractions induced by the muscarinic acetylcholine receptor (mAChR) agonist methacholine in isolated circular muscle of the guinea pig proximal colon (IC50 = 3.7 μM). Otilonium (4 mg/kg) decreases fecal excretion and wet dog shakes and increases the tail withdrawal latency in the tail-flick test in a rat model of opioid withdrawal syndrome induced by morphine and naloxone.
Chemical Properties
White Powder
Therapeutic Function
Anticholinergic, Spasmolytic
General Description
Otilonium bromide is an antispasmodic. It contains a red color ACh (acetylcholine) like moiety bound to an aromatic system that ends with an octyl ether.
Biochem/physiol Actions
Otilonium Bromide is a muscarinic receptor antagonist (antimuscarinic). Otilonium Bromide is a quaternary ammonium salt that exerts spasmolytic action selective on the distal gastrointestinal tract. It is used world-wide for the treatment of irritable bowel syndrome (IBS).
Safety Profile
Poison by intraperitoneal route. Moderately toxic by ingestion and subcutaneous routes. When heated to decomposition it emits toxic fumes of Brí and NOx.
Check Digit Verification of cas no
The CAS Registry Mumber 26095-59-0 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 2,6,0,9 and 5 respectively; the second part has 2 digits, 5 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 26095-59:
(7*2)+(6*6)+(5*0)+(4*9)+(3*5)+(2*5)+(1*9)=120
120 % 10 = 0
So 26095-59-0 is a valid CAS Registry Number.
InChI:InChI=1/C28H40N2O4.BrH/c1-5-8-9-10-13-21-33-26-15-12-11-14-25(26)27(31)29-24-18-16-23(17-19-24)28(32)34-22-20-30(4,6-2)7-3;/h11-12,14-19H,5-10,13,20-22H2,1-4H3;1H
26095-59-0Relevant articles and documents
ANTIBIOTIC AMMONIUM COMPOUNDS AND METHODS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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, (2020/08/22)
The present disclosure provides ammonium compounds, e.g., compounds according to Formula I as set forth herein, which are useful as antimicrobial agents. Methods for the treatment of bacterial infections and associated conditions, e.g., gastrointestinal conditions, are also described, as well as methods for altering the microbiome of subjects such as humans.
