Anticholinergic potentialities of four standard anti-secretory drugs (N-methyl-scopolammonium methylsulfate, atropine, diphemanil and prifinium) have been investigated with the help of molecular pharmacology techniques. The results gained with two different agonists (acetylcholine and carbachol) on rat and dog intestinal cholinergic receptors-jejunum and duodenum respectively-show : 1) That relative potentialities of the anticholinergic drugs (pA2) as well as those of the cholinomimetic agonists (pD2) are markedly modified according to which effector is used. 2) The N-methyl scopolammonium methylsulfate remains in any event the most potent anticholinergic drug investigated.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Discovery of the FXR/CES2 dual modulator LE-77 for the treatment of irinotecan-induced delayed diarrhea.
Bioorg Chem
December 2024
School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR China; Key Laboratory of New Drug Discovery and Evaluation of the Guangdong Provincial Education Department, Guangdong Pharmaceutical University, Guangzhou 510006, PR China; Guangzhou Key Laboratory of Construction and Application of New Drug Screening Model Systems, Guangdong Pharmaceutical University, Guangzhou 510006, PR China; Guangdong Provincial Key Laboratory of New Drug Design and Evaluation, Guangzhou, 510006, PR China. Electronic address:
Article Synopsis
- Irinotecan (CPT-11) is a drug used to treat colorectal cancer, but its effectiveness is limited by severe delayed diarrhea from toxic metabolites.
- The standard treatment for this diarrhea, loperamide, has its own side effects and often fails, indicating a need for better solutions.
- This study introduces LE-77, a compound that activates the Farnesoid X receptor (FXR) and inhibits the enzyme carboxylesterase 2 (CES2), successfully reducing intestinal toxicity and alleviating delayed diarrhea caused by CPT-11.
Quantitation of thiorphan in human plasma using LC-MS/MS and its application to a bioequivalence study.
J Chromatogr B Analyt Technol Biomed Life Sci
August 2024
Jordan Center for Pharmaceutical Research (JCPR), Amman, Jordan.
Racecadotril, an anti-secretory medication, has been used as an adjuvant in an oral rehydration therapy for children experiencing severe diarrhea. Racecadotril is quickly converted to thiorphan, an active metabolite, after oral treatment, which mediates all subsequent activities. An efficient and rapid liquid chromatography-tandem mass spectrometry method was developed and fully validated to measure thiorphan in human plasma, using thiorphan-d7 as an internal standard.
View Article and Find Full Text PDFTwenty-four-hour pH metry alone is inferior to additional impedance monitoring in the diagnosis of gastroesophageal reflux disease, particularly in presence of reduced gastric acid secretion.
Indian J Gastroenterol
August 2023
Department of Gastroenterology, Sanjay Gandhi Postgraduate Institute of Medical Sciences, Raebareli Road, Lucknow, 226 014, India.
Background: Current gold standard for the diagnosis of gastroesophageal reflux disease (GERD) is 24-hour pH metry though it fails to detect non-acidic reflux. The sensitivity of 24-hour pH metry alone (both catheter-based and Bravo capsule) is questionable, especially if gastric acid secretion is low due to reduced parietal cell mass, Helicobacter pylori-induced gastric atrophy and antisecretory therapy. Accordingly, we analyzed the diagnostic ability of 24-hour pH metry as compared to impedance monitoring in relation to the gastric pH without antisecretory therapy.
View Article and Find Full Text PDFLifestyle and dietary interventions for Ménière's disease.
Cochrane Database Syst Rev
February 2023
Cochrane UK, Oxford, UK.
Background: Ménière's disease is a condition that causes recurrent episodes of vertigo, associated with hearing loss and tinnitus. Lifestyle or dietary modifications (including reducing the amount of salt or caffeine in the diet) are sometimes suggested to be of benefit for this condition. The underlying cause of Ménière's disease is unknown, as is the way in which these interventions may work.
View Article and Find Full Text PDFHuman Challenge Studies for Cholera.
Curr Top Microbiol Immunol
October 2024
Katharine Reynolds Ireland Chair of Pediatrics, University of Alabama at Birmingham, Physician-in-Chief, Children's of Alabama, Birmingham, AL, USA.
The human challenge model permits an estimate of the vaccine protection against moderate and severe cholera. It eliminates the difficulty in setting up a vaccine study in endemic area including uncertainties about the incidence of cholera and the logistic arrangements for capturing those who do/do not become ill. Valuable information from small groups of subjects can be obtained in a short period.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!