Gastrointestinal prokinetic and antiemetic effects of a new substituted pyrimidinO 6553 (2-methylamino-4-N-methylpiperazino-5-thiomethyl-6-chloropyrimidine hydrochloride).
2-Methylamino-4-N-methylpiperazino-5-methylthio-6-chloropyrimidine hydrochloride (O 6553) is a new molecule showing an original pharmacological profile in the laboratory tests. It possesses at the same time potent gastro-intestinal prokinetic and central antiemetic properties, demonstrated on the one hand by the gastro-duodenal transit of barium meal in rats, and on the other hand by apomorphine-induced vomiting in dogs. The drug also has interesting anxiolytic and antiserotonin properties and, at doses which change gastro-intestinal behaviour, it is devoid of any untoward side effect. The acute and subacute toxicities of O 6553 show that the drug has a very good safety margin.
D000818:Animals; D000932:Antiemetics; D001341:Autonomic Nervous System / Q000187:drug effects; D001522:Behavior, Animal / Q000187:drug effects; D001831:Body Temperature / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects; D004285:Dogs; D005260:Female; D005769:Gastrointestinal Motility / Q000187:drug effects*; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D010879:Piperazines / Q000494:pharmacology* / Q000633:toxicity; D011743:Pyrimidines / Q000494:pharmacology* / Q000633:toxicity; D011817:Rabbits; D051381:Rats; D012702:Serotonin Antagonists; D013997:Time Factors
D000932:Antiemetics; D010879:Piperazines; D011743:Pyrimidines; D012702:Serotonin Antagonists