(-)e-2-(3,4-dichlorocinnamyl)-1-cyclopropylmethyl-piperidine, and its antidiarrhoeal use
a technology of cyclopropylmethyl and piperidine, which is applied in the direction of heterocyclic compound active ingredients, drug compositions, biocides, etc., can solve the problems of prohibitive treatment costs, inability to use in an outpatient environment, and abandoning their generalization
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example 2
[0054] Toxicity Study
[0055] In animals, the toxicity study was carried out in mice by the oral route. No mortality was noted up to the strongest dose studied, namely 300 mg / kg. No toxic symptoms were evident at doses lower than 100 mg / kg. Starting from this dose, symptoms were observed such as respiratory depression, trembling, convulsions, a state of prostration or of lethargy which were reversible in a lapse of time of 24 hours after treatment.
example 3
[0056] In vitro Pharmacological Study: Affinity for Sigma Receptors
[0057] The study of the capacity of interaction with the sigma receptors of the eutomer which is the subject of the invention, of its antipode and of its parent racemic compound, was carried out by the determination of their binding to a rat brain membrane preparation, previously loaded with a labelled ligand specific for sigma receptors, in this; case (+)[3H]-SKF 10,047. The technique used (described by Largent, B. L. et al., J. Pharmacol. Exp. Ther., 1986, vol. 238, pp. 739-748) consists in incubating, in solutions of variable concentrations of the test product, the membrane preparation previously loaded with (+)[3H]-SKF 10,047. After filtration, the radioactivity of the solution, which is representative of the displacement of the ligand by the test: product, is measured. Results are expressed as ICSO of the test product , which is the concentration allowing the tritiated ligand to be displaced from 50% of its bind...
example 4
[0059] In vivo Pharmacological Studies
[0060] 4-1)--inhibition of experimental toxogenic diarrhoeas Methods
[0061] a) diarrhoea induced by Salmonella lipoiolysaccharide (LPS):
[0062] The test is carried out in mice according to a working procedure, instigated by M. J. CANCIO et al., Gastroenterology November 1992, 103 (5), 1437-43, which in the rat induces, by an endotoxin, alterations in the transport of water and of electrolytes at the colon level.
[0063] working procedure: dBA.sub.2 male mice (Iffa-credo, les Oncins, France) weighing between 20 and 25 g are placed in individual cages. After adaptation of the animals to their environment, the test product is administered by the oral route in solution or in aqueous suspension and then after one hour (to of the test) an injection of lipopolysaccharides (LPS) of Salmonella enteriditis (Sigma ref. L6761) is carried out in the tail vein at a rate of 15 mg / kg. A preweighed filter paper is then placed under each cage and the weight of faeces...
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