Altogether, 138 patients were included in a study aimed at evaluating the effect of cisapride on healing and relapse of oesophagitis shown endoscopically. In the first phase of the study cisapride was given in an open fashion at 10 mg four times a day for 8 to 16 weeks, and healing was obtained in 69% of patients. Healing occurred later in patients with grades II to IV oesophagitis. The total score for reflux symptoms decreased by 67%. Eighty of the healed patients were included in the second phase. They were randomly assigned to double blind treatment with either cisapride 10 mg (n=37) or placebo (n=43) twice a day. Control endoscopy was performed when symptoms recurred or at the end of the six month trial. The cumulative percentage of patients in remission was higher (p=0.06, survival analysis) in the cisapride group than in the placebo group, the relapse rates being 20% and 39%. The duration of remission tended to be longer in patients with a lower initial degree of oesophagitis. Adverse effects were no more frequent with cisapride than with placebo. In conclusion, cisapride is efficacious in healing oesophagitis, and, unlike other gastrointestinal prokinetic drugs or low dose cimetidine (400-800 mg daily) or ranitidine (150 mg daily), it may prevent relapse of oesophagitis.
A rapid carbachol-induced disappearance of muscarinic cell surface receptors was shown using [3H]methyl scopolamine as ligand on intact 108CC15 hybrid cells or rat cerebellar cells. This phenomenon is temperature-dependent, correlated to agonist stimulation and reversible. In these short time periods (<30 min), no change was observed in the total receptor amount measured on membrane preparations. This disappearance of cell surface receptors could represent the first event in cell desensitization which could be followed by receptor recycling in physiological conditions or by receptor degradation if the stimulation by agonists persists, as in long-term regulation.
Muscarinic receptor /=?l_bUethylscopoidmine Desensitization
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.