New alkanamide cpds. are serotoninergic receptor, type 5-HT3, ligands - useful in treating e.g. nausea, schizophrenia, anxiety, depression, Alzheimer's disease, pain, migraine and gastrointestinal disorders

摘要

Alkanamides of formula (I) and their acid addn. salts are new. R = H, 1-6C alkyl, aryl, aryl-(1-3C)alkyl or aryloxy-(1-3C)alkyl. USE/ADVANTAGE - (I) are ligands of serotoninergic receptors, partic. 5-HT3 type. They are useful for the treatment and prevention of disorders in which serotoninergic receptors are implicated, such as nausea and vomiting (e.g. following antitumoural treatment or anaesthesia); CNS disorders such as schizophrenia, mania, anxiety and depression; cognitive disorders such as senile dementia or Alzheimer's disease; dyskinesia, pain, migraine or headaches; problems associated with alcohol or drug dependency or withdrawal and gastrointestinal disorders. The most active cpds. (I) inhibit bradycardia provoked by serotonin by at least 40% at 1 micro g/kg (i.v., rat). (I) increase gastric emptying at 0.1mg/kg (i.p. or p.o. rat). (I) have an anti-emetic effect at 5mg/kg (p.o. ferret).