Pharmacological properties of benzazoles. I. Relationship between structure and paralyzing action.

摘要: An isosteric series of benzazoles was compared for their ability to produce paralysis in animals various species. 1. The effects produced by the were a mixture stimulation and depression. stimulating usually first occur, subsequently followed depressant which predominant. 2. substituted 2-aminobenzothiazoles particular paralyzing agents high potency. Methyl or chloro groups benzene ring 2-aminobenzothiazole depression according following order substitution: position 6 > 5 4 7. 6-Methyl-2-aminobenzothiazole especially free any effects. 3. A 1 2 carbon alkyl chain benzazole had no marked effect on potency but caused more respiratory depression, while lengthening amyl convulsant. azole structure appeared essential properties benzazoles. Opening as phenylthiourea heterocyclic could be 5-membered 6-membered quinoxaline paralysis. Tautomerism apparently one requirement this 4. None curare-like action doses producing While some local anesthesia, intravenous administration hemolysis erythrocytes, anesthetic also hemolytic did not correlate with transient drop blood pressure when given rapidly intravenously, slow oral little effect. This agent central before affecting vasomotor centers.