Cimetropium Bromide (DA-3177)
(Synonyms: 西托溴铵; DA-3177) 目录号 : GC30955
Cimetropium Bromide (DA-3177) (DA-3177) 是一种 mAChR 拮抗剂，用于长期治疗肠易激综合征。
Cas No.:51598-60-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
Cimetropium Bromide behaves as a competitive antagonist of muscarinic-mediated contractions in isolated colonic preparations from both species, with affinity values (pA2) ranging between 7.41 and 7.82[1]. Cimetropium has potent antimuscarinic effect in inhibition of contraction of longitudinal muscle preparations. In the superfusion experiments of the preparation which has been preloaded with labelled choline, Cimetropium decreases the labelled ACh release induced by electrical field stimulation under the muscarinic autoinhibition blocked-condition[2].
When administered intravenously to conscious dogs provided with a colonic Thiry fistula, Cimetropium is a potent inhibitor of large bowel motility evoked by both exogenous and endogenous stimuli. Cimetropium Bromide (10-100 μg/kg) counteracts colonic motor response to neostigmine administration with an ID50 of 27.9 μg/kg; both tonic and phasic components of contractile response are affected. In a comparable range of doses (3-100μg/kg), the drug inhibits motor activity elicited by intraluminal distension[1].
[1]. Identification of orally administered cimetropium bromide in the colon of the rat and its possible local spasmolytic effect. [2]. Saitoh N, et al. Characterization of antimuscarinic effect of cimetropium bromide in guinea pig ileum. J Smooth Muscle Res. 1997 Feb;33(1):1-9.
| Cas No. | 51598-60-8 | SDF | |
| 别名 | 西托溴铵; DA-3177 | ||
| Canonical SMILES | C[N+]1([C@H]2[C@@H](O3)[C@@H]3[C@@H]1C[C@H](OC([C@@H](C4=CC=CC=C4)CO)=O)C2)CC5CC5.[Br-] | ||
| 分子式 | C21H28BrNO4 | 分子量 | 438.36 |
| 溶解度 | Water : 50 mg/mL (114.06 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2812 mL | 11.4062 mL | 22.8123 mL |
| 5 mM | 0.4562 mL | 2.2812 mL | 4.5625 mL |
| 10 mM | 0.2281 mL | 1.1406 mL | 2.2812 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Assessment of Cimetropium Bromide Use for the Detection of Gastric Neoplasms During Esophagogastroduodenoscopy
Importance: Esophagogastroduodenoscopy (EGD) is a common procedure used to examine upper gastrointestinal diseases. Although cimetropium bromide and other antispasmodic agents are commonly administered as premedication to inhibit peristalsis during EGD examination, there are few data regarding the benefits of cimetropium bromide for the detection of gastric neoplasms. Objective: To investigate the association between the use of cimetropium bromide as premedication and gastric neoplasm detection rates during EGD examination. Design, setting, and participants: This propensity score-matched retrospective cohort study included 67 683 participants who received EGD screening at the Health Promotion Center of Seoul St. Mary's Hospital, The Catholic University of Korea, from January 2, 2010, to June 30, 2017. Data were analyzed from April 1 to December 30, 2021. Exposures: Participants were divided into 2 groups: those who received cimetropium bromide before EGD examination (intervention group) and those who did not (control group). Main outcomes and measures: Gastric neoplasm detection rates. Results: Among 67 683 participants, the mean (SD) age was 48.6 (10.8) years, and 36 517 participants (54.0%) were male; all participants were Asian (a racially homogenous population). Of those, 28 280 participants (41.8%; mean [SD] age, 50.3 [10.6] years; 57.8% male) received cimetropium bromide, and 39 403 participants (58.2%; mean [SD] age, 47.4 [10.8] years; 51.2% male) did not. Propensity score matching based on confounding variables yielded 41 670 matched participants (20 835 pairs). Detected lesions included 52 dysplasias (0.12%), 40 early cancers (0.10%), 7 advanced cancers (0.02%), and 3 lymphomas (0.01%). Gastric neoplasm detection rates were significantly higher in the intervention group (63 participants [0.30%]) vs the control group (39 participants [0.19%]; P = .02). A significant difference in the combined detection rate of dysplasia and early gastric cancer was found between those in the intervention group (57 participants [0.27%]) vs the control group (35 participants [0.17%]; P = .02). For small gastric lesions (<1 cm), those who received cimetropium bromide had higher detection rates (24 participants [0.12%]) than those who did not (11 participants [0.05%]; P = .03). Lesions in the gastric body were detected significantly more often in the intervention group (34 participants [0.16%]) vs the control group (15 participants [0.07%]; P = .007). In multivariate analyses involving all 67 683 participants, the use of cimetropium bromide was more likely to detect gastric neoplasms compared with nonuse (odds ratio, 1.42; 95% CI, 1.04-1.95; P = .03). Conclusions and relevance: In this study, the use of cimetropium bromide as premedication was significantly associated with increased gastric neoplasm detection rates during EGD screening, and lesions in the gastric body were detected more frequently among those who received cimetropium bromide compared with those who did not. These findings suggest that cimetropium bromide may be considered as premedication before EGD examination among individuals with no contraindications.
Cimetropium bromide does not improve polyp and adenoma detection during colonoscope withdrawal: A randomized, double-blind, placebo-controlled study
Background: Endoscopic inspection of colonic mucosa is disturbed by colonic folds and peristalsis, which may result in missed polyps. Cimetropium bromide, an antispasmodic agent, inhibits peristalsis and colonic spasms, which may improve polyp detection. The purpose of this randomized, double-blind, placebo-controlled study was to investigate whether cimetropium bromide could improve polyp and adenoma detection in the colorectum and right colon.
Methods: Patients undergoing screening or diagnostic colonoscopy were randomized to receive intravenous cimetropium bromide (5 mg) or placebo after cecal intubation. The primary outcomes were the number of polyps per patient (PPP) and adenomas per patient (APP); secondary outcomes were the polyp detection rate (PDR), adenoma detection rate (ADR), and advanced neoplasm detection rate (ANDR).
Results: A total of 181 patients were analyzed; 91 patients received cimetropium bromide and 90 patients received placebo. Cimetropium bromide and placebo groups did not significantly differ in the PPP and APP for the colorectum (1.38 ± 1.58 vs 1.69 ± 2.28, P = .298; 0.96 ± 1.27 vs 1.11 ± 1.89, P = .517, respectively) and right colon (0.70 ± 0.95 vs 0.78 ± 1.21, P = .645; 0.47 ± 0.81 vs 0.51 ± 0.81, P = .757, respectively). Two groups also did not significantly differ in the PDR, ADR, and ANDR for the colorectum and right colon. Furthermore, there were no difference between groups in the PPP, APP, PDR, ADR, and ADNR in a sub-analysis of expert and non-expert endoscopists.
Conclusions: Cimetropium bromide did not improve polyp and adenoma detection in the colorectum and right colon during colonoscope withdrawal, regardless of the expertness of the endoscopist. However, its use may be helpful in patients with active peristalsis or for beginning endoscopists during standard colonoscopy without a transparent cap.
Cimetropium bromide in the treatment of crisis in infantile colic
Background: Treatment of infantile colic remains an open issue. In Italy, cimetropium bromide is used extensively to treat infantile colic. The aim of this randomized, double-blind, placebo-controlled clinical trial was to investigate the effectiveness and side effects of cimetropium bromide in the treatment of infants with colic crisis.
Methods: Ninety-seven infants with colic were enrolled. The diagnosis of infantile colic in healthy infants with regular growth, aged 15 to 60 days was made according to the criteria of Wessel. The infants were divided into two groups, one treated with cimetropium bromide (1.2 mg/kg) and the other treated with placebo at onset of each crisis for 3 days. Duration of crying and side effects were recorded daily in a structured diary for the 3 days of therapy. Statistical analysis was performed using the chi-square and t tests.
Results: Eighty-six infants completed the trial. The average duration of crying for each crisis was 17.3 +/- 12.6 minutes in the cimetropium bromide group and 47.5 +/- 28.5 minutes in the placebo group (P < 0.005). Response to cimetropium bromide was 74%. Response to placebo was 33% (P < 0.05). Side effects did not differ significantly between the two groups, except sleepiness, which increased in the infants treated with cimetropium bromide.
Conclusion: Cimetropium bromide was more effective than placebo in reducing the duration of crying in children with infantile colic. The use of the anticholinergic drugs, aside from the dicyclomine because of its dangerous side effects, should be revaluated for treating infantile colic.
Oral cimetropium bromide, a new antimuscarinic drug, for long-term treatment of irritable bowel syndrome
Most drugs are ineffective for the long-term treatment of irritable bowel syndrome (IBS). The beneficial effects of medical treatment of IBS are poor and last for only a relative short time. Over a period of 6 months, we investigated the effectiveness of cimetropium bromide, a new antimuscarinic compound, in patients with IBS. Forty-eight patients were treated at random and in double-blind fashion with cimetropium bromide (50 mg, tid) or placebo for 6 months. Personal diary cards and monthly check-ups guaranteed the monitoring of symptoms (mainly pain). In addition, personality patterns (MHQ-CBA tests) were obtained for the patients before and after therapy, both to detect possible psychoneurotic traits and to observe the changes in these traits in relation to the changes in pain symptoms. Three patients on placebo and one on cimetropium dropped out. At the end of therapy, pain scores had decreased an average of 16% in the placebo group and 87% in the cimetropium group (p less than 0.01). Twenty patients (87%) on cimetropium versus five patients (24%) on placebo considered themselves to be globally improved (p less than 0.01). The MHQ test showed significant improvement in the anxiety score in the cimetropium group only. The CBA test confirmed a significant decrease in anxiety state (STAI-X-1) after cimetropium treatment. Eleven patients (48%) on cimetropium reported side effects (mainly dry mouth and sleepiness), but none withdrew from the study. The results of this trial indicate that long-term treatment of IBS with cimetropium bromide significantly improves symptoms and associated psychological disorders.
Comparison between the Effectiveness of Oral Phloroglucin and Cimetropium Bromide as Premedication for Diagnostic Esophagogastroduodenoscopy: An Open-Label, Randomized, Comparative Study
Background/aims: Suppression of gastrointestinal (GI) peristalsis during GI endoscopy commonly requires antispasmodic agents such as hyoscine butylbromide, atropine, glucagon, and cimetropium bromide. This study examined the efficacy of oral phloroglucin for the suppression of peristalsis, its impact on patient compliance, and any associated complications, and compared it with intravenous or intramuscular cimetropium bromide administration.
Methods: This was a randomized, investigator-blind, prospective comparative study. A total of 172 patients were randomized into two groups according to the following medications administered prior to upper endoscopy: oral phloroglucin (group A, n=86), and cimetropium bromide (group B, n=86). The numbers and the degrees of peristalsis events at the antrum and second duodenal portion were assessed for 30 seconds.
Results: A significantly higher number of gastric peristalsis events was observed in group A (0.49 vs. 0.08, p<0.001), but the difference was not clinically significant. No significant difference between both groups was found in the occurrence of duodenal peristalsis events (1.79 vs. 1.63, p=0.569). The incidence of dry mouth was significantly higher with cimetropium bromide than with phloroglucin (50% vs. 15.1%, p<0.001).
Conclusions: Oral phloroglucin can be used as an antispasmodic agent during upper endoscopy, and shows antispasmodic efficacy and adverse effects similar to those of cimetropium bromide.