ABSTRACT
Several dialkylaminoethyl benzo[b]thiophene-3-carboxylates, N-(2-dialkylaminoethyl)benzo[b]thiophene-3-carboxamides, 2-dialkylaminoethyl benzo[b]thiophene-3-carbamates, and substituted ureas with benzo[b]thiophene moiety, were prepared and tested for local anesthetic, anticholinergic, and antihistaminic activities. Several of the compounds showed significant activity.
Subject(s)
Anesthetics, Local/chemical synthesis , Histamine H1 Antagonists/chemical synthesis , Parasympatholytics/chemical synthesis , Thiophenes/chemical synthesis , Animals , Chemical Phenomena , Chemistry, Physical , Cornea/drug effects , Guinea Pigs , In Vitro Techniques , Muscle Contraction/drug effects , Muscle, Smooth/drug effects , Rabbits , Thiophenes/pharmacologyABSTRACT
1. Perphenazine, promethazine and levomepromazine induced sedation in young pullets following intramuscular injections. 2. The best results were obtained with perphenazine at a dose rate of 1-5 mg/kg.
Subject(s)
Antipsychotic Agents/pharmacology , Chickens/physiology , Animals , Female , Heart Rate/drug effects , Methotrimeprazine/pharmacology , Perphenazine/pharmacology , Promethazine/pharmacology , Reserpine/pharmacology , Respiration/drug effectsABSTRACT
5-Substituted 2-amino-1,3,4-thiadiazoles were transformed to their corresponding 2-bromo derivatives. The reaction of the 5-substituted 2-bromo-1,3,4-thiadiazoles with N,N-dialkylaminoethylamines or N-methylpiperazine afforded the corresponding amino-1,3,4-thiadiazole derivatives. All prepared compounds displayed antihistaminic, anticholinergic, and norepinephrine-potentiating activities.
