247-457-4
Otilonium bromide
CAS: 26095-59-0
Molecular Formula: C29H43BrN2O4
247-457-4 - Names and Identifiers
| Name | Otilonium bromide |
| Synonyms | SP-63 Spasen Menoctyl Pasminox Spasmome Otilonium 247-457-4 Spasmoctyl Otilonium bromide N,N-Diethyl-N-methy-2-[[4-[[2-(octyloxy)benzoyl]amino]benzoyl]oxy]ethanaminium Bromide N,N-Diethyl-N-methyl-2-[(4-{[2-(octyloxy)benzoyl]amino}benzoyl)oxy]ethanaminium bromide N,N-diethyl-2-[(4-{[2-(heptyloxy)benzoyl]amino}benzoyl)oxy]-N-methylethanaminium bromide |
| CAS | 26095-59-0 |
| EINECS | 247-457-4 |
| 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 |
247-457-4 - Physico-chemical Properties
| Molecular Formula | C29H43BrN2O4 |
| Molar Mass | 563.57 |
| Melting Point | 130-133°C |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | -20°C |
| In vitro study | Otilonium bromide is a quaternary ammonium compound that has selective antispasmodic activity on the distal gastrointestinal tract, mainly due to its direct myocardial lytic properties. The drug can change the intestinal smooth muscle cells inside and outside the ion flow of calcium ion pool, it is relatively poor absorption can only locally exert efficacy, does not have the system effect. |
247-457-4 - Risk and Safety
| Toxicity | LD50 in mice (mg/kg) 87.0 i.p. |
247-457-4 - Reference Information
| pharmacological action | otilonium bromide is a spasmodic and anticholinergic drug, it can regulate the calcium flow between the intestinal smooth muscle cells and the intracellular calcium pool, and has selective and strong spasmolysis effect on the smooth muscle of the digestive tract, which is suitable for all hyperkinesia, spasmodic reactions of different causes and in different parts, as well as due to pathological atrophy of smooth muscle fibers. For the treatment of distal gastrointestinal irritable bowel syndrome (IBS) or spastic pain, Colon spasm, gastroenteritis, stomach, duodenum and esophageal diseases, Endoscopy Preparation (esophagoscopy, gastroscopy, duodenoscopy and rectoscopy), experimental data show that after oral administration of the drug, the absorbed part is very small, and most of the absorbed part passes through the biliary tract and is excreted through the stool. |
| toxicological studies | Acute toxicity: the non-lethal dose of oral administration in rats is 1500mg/kg, 1000mg/kg for dogs. Chronic toxicity: experimental animals were dosed according to a regimen of 180 mg/kg/day of otilonium bromide orally for 11.44 consecutive days. No abnormal changes were found in the results of blood biochemical and histological examination. Teratogenic toxicity: no embryotoxicity and teratogenic toxicity in rats and rabbits at 11.44mg/kg. Gene mutation: a large number of experiments showed no mutagenic effect. |
| adverse reactions | at the therapeutic dose of otilonium bromide does not cause side effects and does not cause atropine-like effects. |
| precautions | glaucoma, prostatic hypertrophy, pyloric stenosis, pregnant and lactating women, and patients with known hypersensitivity to otilonium bromide. |
| biological activity | Otilonium bromite is an antimuscarinic drug. |
| Target | TargetValue mAChR |
| Target | Value |
| in vitro study | Otilonium bromite is a quaternary ammonium compound with selective spasmolytic activity on the distal gastrointestinal tract, this is mainly due to its direct myocardial lytic properties. The drug can change the intestinal smooth muscle cells inside and outside the ion flow of calcium ion pool, it is relatively poor absorption can only locally exert efficacy, does not have the system effect. |
| Use | treatment of gastrointestinal spasm |
Last Update：2024-04-09 21:04:16
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