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Pinaverium bromide Sale

(Synonyms: 匹维溴铵) 目录号 : GC30055

Pinaverium bromide (Icosapentaenoic acid) acts as a calcium channel blocker and is useful for functional gastrointestinal disorders.

Pinaverium bromide Chemical Structure

Cas No.:53251-94-8

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10mM (in 1mL DMSO)
¥884.00
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50mg
¥803.00
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产品描述

Pinaverium bromide (Icosapentaenoic acid) acts as a calcium channel blocker and is useful for functional gastrointestinal disorders.

[1] Christen MO. Gen Pharmacol. 1990, 21(6):821-5.

Chemical Properties

Cas No. 53251-94-8 SDF
别名 匹维溴铵
Canonical SMILES CC1(C)C2CCC(CCOCC[N+]3(CC4=CC(OC)=C(OC)C=C4Br)CCOCC3)C1C2.[Br-]
分子式 C26H41Br2NO4 分子量 591.42
溶解度 DMSO : 62.5 mg/mL (105.68 mM) 储存条件 Store at -20°C
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1 mM 1.6908 mL 8.4542 mL 16.9085 mL
5 mM 0.3382 mL 1.6908 mL 3.3817 mL
10 mM 0.1691 mL 0.8454 mL 1.6908 mL
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Research Update

Efficacy of pinaverium bromide in the treatment of irritable bowel syndrome: a systematic review and meta-analysis

Background: Spasmolytic agents are an attractive first line treatment option for irritable bowel syndrome (IBS). Pinaverium bromide (pinaverium) has antispasmodic effects on gastrointestinal smooth muscle and can relieve major IBS symptoms, but an up-to-date meta-analysis comparing the efficacy of pinaverium with placebo is lacking. The aim is to perform a systematic review and meta-analysis to assess the efficacy of pinaverium compared with placebo for IBS treatment. Methods: All placebo-controlled trials evaluating pinaverium for IBS treatment were included, up to October 2019. Treatment efficacy was evaluated by overall patient IBS symptoms. Individual symptoms were also evaluated. The effect of pinaverium versus placebo was expressed as standardized mean difference (SMD) and risk ratio (RR). Odds ratio (OR) and number needed to treat (NNT) were also calculated. Results: Eight studies were included for analysis. Pinaverium treatment had a beneficial effect on overall IBS symptom relief with a positive SMD of 0.64 [95% confidence interval (CI) 0.45-0.82, p < 0.0001] and a positive RR of 1.75 (1.26-2.43, p < 0.0008). No significant difference was found by publication year, gender, age, methodological quality score (MQS), or sample size. No publication bias was detected. OR was 3.43 (2.00-5.88, p < 0.0001), and NNT was 4. Pinaverium also demonstrated a beneficial treatment effect for abdominal pain, stool change, and bloating improvement or resolution. Conclusion: Pinaverium is superior to placebo for the treatment of IBS symptoms, irrespective of patient age or gender, study publication year, sample size, or MQS. The NNT in this meta-analysis is amongst the lowest for studies and meta-analyses of antispasmodics versus placebo in IBS.

Pinaverium Bromide Attenuates Lipopolysaccharide-Induced Excessive Systemic Inflammation via Inhibiting Neutrophil Priming

Dominant infiltration of neutrophils is a hallmark of many inflammatory diseases, especially in septic shock. IL-1β as one of the most early released proinflammatory cytokine in neutrophil, plays a pivotal role in the progress of sepsis. In this study, we built a high-throughput-compatible drug screen assay platform based on our newly constructed reporter C57BL/6 mice, pIL1-DsRed, expressing the DsRed gene under the control of the IL-1β promoter. After screening 1200 U.S. Food and Drug Administration-approved compounds, we found that pinaverium bromide (PVB) significantly suppressed the DsRed expression of primed neutrophil and improved the survival rate of mice given LPS in an endotoxin challenge analogous to sepsis, regardless of whether PVB was administered before or after LPS. PVB also protected the liver and lung from LPS-induced damage and reduced organ-specific inflammatory responses. PVB decreased the production of IL-1β, IL-6, and CXCL1 mRNA in the lungs of LPS-treated mice and decreased the serum levels of liver transaminases (alanine aminotransferase and aspartate aminotransferase) at multiple time points and doses tested. PVB can significantly suppress primed neutrophil-specific respiratory bursts and migration as well. Lastly, PVB affected neutrophils' gene expression and phenotypic changes during neutrophil priming. PVB downregulated GM-CSF-induced expression of CD54 and dectin-2 (markers of fully primed neutrophils) at both mRNA and protein levels during late-phase neutrophil priming. In summary, we demonstrated that PVB can be used as a potential therapeutic agent for sepsis by inhibiting neutrophil priming.

Action of pinaverium bromide, a calcium-antagonist, on gastrointestinal motility disorders

1. The evidence reviewed here indicates that pinaverium bromide (Dicetel) relaxes gastrointestinal (GI) structures primarily by inhibiting Ca2+ influx through potential-dependent channels of surface membranes of smooth muscle cells. 2. The in vivo selectivity of pinaverium bromide for the GI tract appears to be due mainly to its pharmacokinetic properties. Because of its low absorption (typical for quaternary ammonium compounds) and marked hepatobiliary excretion, most of the orally-administered dose of pinaverium bromide remains in the GI tract. 3. Orally-administered pinaverium bromide does not elicit adverse cardiovascular side-effects at doses that effectively relieve GI spasm, pain, transit disturbances and other symptoms related to motility disorders. 4. Pinaverium bromide is the only Ca2(+)-antagonist with known therapeutic efficacy in the treatment of irritable bowel syndrome and certain other functional intestinal disorders.

Effect of Acupuncture in Patients With Irritable Bowel Syndrome: A Randomized Controlled Trial

Objective: To evaluate the effect and safety of acupuncture for the treatment of irritable bowel syndrome (IBS) through comparisons with those of polyethylene glycol (PEG) 4000 and pinaverium bromide.
Patients and methods: This multicenter randomized controlled trial was conducted at 7 hospitals in China and enrolled participants who met the Rome III diagnostic criteria for IBS between May 3, 2015, and June 29, 2018. Participants were first stratified into constipation-predominant or diarrhea-predominant IBS group. Participants in each group were randomly assigned in a 2:1 ratio to receive acupuncture (18 sessions) or PEG 4000 (20 g/d, for IBS-C)/pinaverium bromide (150 mg/d, for IBS-D) over a 6-week period, followed by a 12-week follow-up. The primary outcome was change in total IBS-Symptom Severity Score from baseline to week 6.
Results: Of 531 patients with IBS who were randomized, 519 (344 in the acupuncture group and 175 in the PEG 4000/ pinaverium bromide group) were included in the full analysis set. From baseline to 6 weeks, the total IBS-Symptom Severity Score decreased by 123.51 (95% CI, 116.61 to 130.42) in the acupuncture group and 94.73 (95% CI, 85.03 to 104.43) in the PEG 4000/pinaverium bromide group. The between-group difference was 28.78 (95% CI, 16.84 to 40.72; P<.001). No participant experienced severe adverse effects.
Conclusion: Acupuncture may be more effective than PEG 4000 or pinaverium bromide for the treatment of IBS, with effects lasting up to 12 weeks.
Trial registration: Chinese Clinical Trials Register, ChiCTR-IOR-15006259.

Comparison of acupuncture and pinaverium bromide in the treatment of irritable bowel syndrome: A protocol for systematic review and meta-analysis

Background: Irritable bowel syndrome (IBS) is one of the most common chronic gastrointestinal diseases, and the current diagnosis of IBS is still based on symptoms and examination. Pinaverium bromide is commonly used as an antispasmodic in the treatment of IBS. But adverse effects of pinaverium bromide are common. Meta-analyses show that acupuncture has a positive therapeutic effect on IBS.
Methods: Randomized controlled trials of comparing the efficacy of acupuncture and pinaverium bromide in the treatment of IBS will be searched in the relevant database: PubMed, Embase, Cochrane Library, China National Knowledge Infrastructure (CNKI), Wanfang Database, Chinese Biomedical Literature Database (CBM), and Chinese Scientific Journal Database (VIP database). The studies selected will be exported to EndNote V.9.1 software. Data will be carried out independently from the selected articles by 2 reviewers. Any disagreement will be solved in consultation with a third reviewer.
Results: Our study aims to compare the efficacy of acupuncture and pinaverium bromide in the treatment of IBS and to fill the lack of relevant evidence.
Conclusion: Through the inclusion of relevant literature, the overall efficacy of acupuncture and pinaverium bromide in the treatment of IBS will be evaluated, and the gap between various acupuncture treatment measures will be further analyzed.
Inplasy registration number: INPLASY 202130068.