Delving into the Latest Updates on Mepenzolate Bromide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Mepenzolate bromide (JP17/INN), 340, LT-0302

+ [3]

Target

mAChRs

Action

antagonists

Mechanism

mAChRs antagonists(Muscarinic acetylcholine receptor antagonists)

Therapeutic Areas

Digestive System Disorders

Active Indication

Irritable Bowel Syndrome

Inactive Indication

Peptic Ulcer

Originator Organization

Lakeside Pharma Management AG

Active Organization

Astellas Pharma, Inc.

Inactive Organization

Sanofi-Aventis U.S. LLC

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (14 Nov 1956),

Peptic Ulcer

Regulation-

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Structure/Sequence

Molecular FormulaC21H26BrNO3

InChIKeyJRRNZNSGDSFFIR-UHFFFAOYSA-M

CAS Registry76-90-4

In mol. separation using membranes, enhanced parameters, such as an increased flux and selectivity, are required for efficiency.Addnl., in mol. separation using solvents, solvent resistance is critical in preventing solvent-induced damage.However, most membranes lack resistances to specific harsh solvents, and simultaneously enhancing solvent flux and selectivity performance, which exhibit a trade-off relation, is challenging.In this study, a high-performance solvent-resistant polybenzimidazole (PBI) membrane is fabricated via chem. crosslinking with divinyl sulfone (DVS).The membrane consists of porous finger-like support and dense skin layers, and the uniform DVS crosslinking of the PBI membrane is confirmed via chem. anal.The DVS-crosslinked PBI membrane exhibits a superior solvent stability and separation performance, with an ethanol permeance and mol. weight cut-off of 5.88 L m^-2 h^-1 bar^-1 and 483 g mol^-1, resp.These values represent an enhanced permeance and rejection performance compared to those of the pristine membrane.The DVS-crosslinked PBI membrane also displays a long-term stability in mepenzolate bromide separation over 72 h.

01 Oct 2023·Life sciences

Niacin modulates depressive-like behavior in experimental colitis through GPR109A-dependent mechanisms

Article

Author: Abd El-Haleim, Enas A ; Mohamed, Sarah S ; Khayyal, Mohamed T ; Wadie, Walaa

AIMS:

Depression is one of the common neurological comorbidities in patients with inflammatory bowel disease (IBD). The current study aimed to investigate the potential impact of niacin on colitis-induced depressive-like behavior in rats.

MATERIALS AND METHODS:

Animals were given 5 % dextran sulfate sodium (DSS) in drinking water for one week to induce colitis. Niacin (80 mg/kg), with or without mepenzolate bromide (GPR109A blocker), was administered once per day throughout the experimental period. Rats were tested for behavioral changes using open field and forced swimming tests.

KEY FINDINGS:

Niacin significantly ameliorated DSS-induced behavioral deficits and alleviated macroscopic and microscopic colonic inflammatory changes. It also augmented the hippocampal levels of ZO-1, occludin, and claudin-5 proteins, indicating the ability of niacin to restore the blood-brain barrier (BBB) integrity. Moreover, niacin decreased hippocampal IL-1ꞵ and NF-ĸB contents but increased GSH, Sirt-1, Nrf-2, HO-1 concentrations. All these beneficial effects were partially abolished by the co-administration of mepenzolate bromide.

SIGNIFICANCE:

The neuroprotective effect of niacin against DSS-induced depressive-like behavior was partially mediated through GPR109A-mediated mechanisms. Such mechanisms are also involved in modulating neuronal oxidative stress and inflammation via Sirt-1/Nrf-2/HO-1 signaling pathways.

01 Dec 2022·BMC gastroenterology

Increased prescriptions for irritable bowel syndrome after the 2018 Japan Floods: a longitudinal analysis based on the Japanese National Database of Health Insurance Claims and Specific Health Checkups

Article

Author: Kashima, Saori ; Yoshida, Shuhei ; Miyamori, Daisuke ; Matsumoto, Masatoshi ; Okazaki, Yuji

Abstract:

Background:

The frequency and intensity of natural disasters are increasing worldwide, which makes our understanding of disaster-related diseases more important than ever. Natural disasters cause mental stress and infectious diarrhea, but the causal relationship between disasters and a potential consequence of these conditions, irritable bowel syndrome (IBS), is unreported. The 2018 Japan Floods, which took place in July 2018 was one of the largest water disasters in Japan’s recorded history. We investigate the change of drug prescriptions for IBS between disaster-suffers and non-sufferers throughout the disaster period to examine the relationship.

Methods:

This is a retrospective cohort study based on the Japanese National Database of Health Insurance Claims and Specific Health Checkups in flood-stricken areas between July 2017 and June 2019. We included subjects older than 15 years of age who had visited a medical institution or been hospitalized in the hardest-hit areas of the disaster. Ramosetron, polycarbophil calcium, and mepenzolate bromide (IBS drugs) approved solely for the treatment of IBS in Japan were analyzed. The monthly rate of prescriptions for IBS drugs was compared between municipality-certified disaster victims and non-victims using a controlled interrupted time series analysis. For those who were not prescribed IBS drugs before the disaster (non-users), the occurrence of an IBS drug prescription after the disaster was evaluated using a multivariable logistic regression analysis adjusted for gender and age.

Results:

Of 5,287,888 people enrolled, 32,499 (0.61%) were certified victims. The prescription rate for IBS drugs among victims increased significantly by 128% immediately after the disaster, while it was stable among non-victims. The trend for the post-disaster prescription rate among victims moved upward significantly when compared to non-victims (0.01% per month; 95% confidence interval (CI) 0.004–0.015; P = 0.001). Among non-users, the occurrence of an IBS drug prescription for victims was 0.71% and was significantly higher than non-victims (0.35%, adjusted odds ratio 2.05; 95% CI 1.81–2.32).

Conclusions:

The 2018 Japan Floods increased the rate of prescriptions for IBS drugs, suggesting that the disaster caused or worsened IBS among victims.

100 Deals associated with Mepenzolate Bromide

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