Disease relevance of Clebopride

• Transient dyskinesia induced by clebopride [1].
• Parkinsonian syndrome after long-term treatment with clebopride [2].
• A double-blind comparison of clebopride and placebo in dyspepsia secondary to delayed gastric emptying [3].
• Progressive supranuclear palsy syndrome induced by clebopride [4].
• Effect of intramuscular clebopride on postoperative nausea and vomiting [5].

Psychiatry related information on Clebopride

• The orthopramide clebopride, a potent dopaminergic antagonist, blocks emesis in dogs and stereotyped behavior in rodents [6].

High impact information on Clebopride

• These results indicate that clebopride acts on post ganglionic cholinergic neurons at D2 and alpha-2 receptors in this preparation to enhance enteric nervous system stimulated motility [7].
• 7. Clebopride and Delagrange 2674 inhibited [3H]-FNM binding with similar potency in rat cerebellar and hippocampal membranes, suggesting they have no selectivity for BDZ1 and BDZ2 binding sites.(ABSTRACT TRUNCATED AT 250 WORDS)[8]
• 2. Clebopride, Delagrange 2674, Delagrange 2335 and BRL 20627 displayed concentration-dependent displacement of [3H]-FNM with IC50 values of 73 nM, 132 nM, 7.7 microM and 5.9 microM, respectively [8].
• 6. The pattern of binding of clebopride and Delagrange 2674 in these in vitro tests is similar to that found previously with partial agonists or antagonists at BDZ binding sites [8].
• An analysis of the hypothalamic sites at which the substituted benzamides, metoclopramide and clebopride, act to facilitate gastric emptying was undertaken in the guinea-pig [9].

Chemical compound and disease context of Clebopride

• Serum levels of prolactin (PRL), luteinizing hormone (LH), and follicle-stimulating hormone (FSH) were measured in normally cycling women and normal men before and after oral admiministration of 1 mg of clebopride, a derivative of procainamide used in the treatment of gastrointestinal diseases [10].
• It is concluded that clebopride is at least as effective as domperidone for the treatment of reflux gastritis but that more prolonged studies and different administration schedules are requested for a better evaluation [11].
• The clinical efficacy and the safety of chronic oral administration of cisapride, a new gastrointestinal prokinetic agent, (10 mg tid) and clebopride (0.5 mg tid) was assayed in 48 outpatients affected with functional dyspepsia, in a randomized double-blind study [12].

Biological context of Clebopride

• The pharmacokinetics of a new benzamide drug clebopride, in the rat and the dog [13].
• Metabolism of clebopride in vitro. Mass spectrometry and identification of products of amide hydrolysis and N-debenzylation [14].
• Clebopride at 10 microM significantly decreased the Vmax of phase 0 depolarization (p < .05) and significantly prolonged the action potential duration at 90% repolarization (APD90) (p < .01), whereas the action potential duration at 50% repolarization (APD50) was not prolonged [15].
• PLS-based quantitative structure-activity relationship for substituted benzamides of clebopride type. Application of experimental design in drug design [16].

Anatomical context of Clebopride

• The results show that the combination of clebopride and simethicone was better than placebo in reducing gastric distension and in improving the quality of echographic images of the organs located behind the stomach, that is, the gallbladder, pancreas, and left kidney [17].
• Influence of long-term treatment of the rat with clebopride on the morphology of the mammary gland [6].
• The substituted benzamide compounds alizapride, metoclopramide, clebopride and YM 09151-2 prevented the accumulation of [3H]spiperone in the substantia nigra, striatum, tuberculum olfactorium and hypothalamus [18].
• Effect of clebopride on lower esophageal sphincter pressure [19].

Associations of Clebopride with other chemical compounds

• Peripherally administered metoclopramide (0.1-10 mg/kg i.p.), clebopride (1-10 mg/kg i.p.), (-)-sulpiride (40 mg/kg i.p.), haloperidol (1 mg/kg i.p.) and domperidone (1-10 mg/kg i.p.) failed to modify gastric emptying [20].
• Facilitation of emptying by i.c.v. metoclopramide was prevented by peripheral pretreatment with atropine (0.5 mg/kg i.p.). It is concluded that the actions of apomorphine and metoclopramide/clebopride to respectively inhibit and facilitate gastric emptying may be mediated, at least in part, via central mechanisms [20].
• Domperidone (IC50 = 10(-6) M), clebopride (10(-5) M) and metoclopramide (2 X 10(-5) M) antagonized gastric relaxations induced by dopamine [21].
• Conclusion: domperidone, clebopride, metoclopramide and trimebutine exert distinct and diverse effects on the motility parameters of the gastroduodenal preparation of the guinea pig [21].
• YM 09151-2 and clebopride only weakly displaced specific binding of [3H]piflutixol to D-1 sites on rat striatal membranes, and only weakly inhibited striatal dopamine stimulated adenylate cyclase activity, when compared with cis-flupenthixol [22].

Gene context of Clebopride

• When 5 mg of bromocriptine were given before clebopride, the PRL response was completely abolished as compared with the control experiment (P < 0.001) [10].
• Climbing behaviour induced by NPA (2.5 mg/kg) could be antagonised by SCH23390 but not by clebopride, however climbing behaviour induced by a low dose of NPA (0.06 mg/kg) plus SKF38393 could be blocked by both D-1 and D-2 receptor antagonists [23].
• Potentiation of the gastric antisecretory activity of histamine H2-receptor antagonists by clebopride [24].

Analytical, diagnostic and therapeutic context of Clebopride

• Finally, basal and clebopride-stimulated ACh efflux were unaffected by the repeated microdialysis sessions [25].
• This case presented two peculiarities: (1) the condition was induced by the chronic use of clebopride, and (2) abdominal dyskinesias showed a dramatic response to the application of transcutaneous electrical nerve stimulation [26].
• After intravenous, intramuscular and oral administration of clebopride in the rat and the dog its apparent volume of distribution is high (1.6-3.2 1 kg-1) and it has a longer biological half-life than metoclopramide in both species [13].
• Radioimmunoassay for clebopride, a new benzamide drug with antidopaminergic activity [27].
• 4. The results suggest that clebopride induces analgesia against both thermal and chemical nociceptive stimuli, which is not mediated via opioid mechanisms [28].

References