I. The Ethyl, Isopropyl and Propyl Derivatives
Abstract
A systematic study of a series of 24 β-2,5-dimethoxyphenylalkyl amine and quaternary compounds resulted in the discovery of several powerful, longacting pressor substances of which No. 839, β-2,5-dimethoxyphenyl-β-isopropylamine, is outstanding.
Pressor activity generally was restricted to the primary and the secondary amines of the ethyl and the isopropyl series. Within these limits, the presence of a β-hydroxy group increased pressor activity. The β-methyl group, as manifested by the propyl compounds, always was inhibitory to pressor action. Tertiary and quaternary nitrogen derivatives usually were inactive. The β-hydroxyisopropylamines and compounds containing quaternary nitrogen enhanced epinephrine activity. The depressor effect of acetyicholine was decreased by certain compounds. All compounds contracted the isolated guinea pig and the isolated rabbit uterus, and all relaxed the isolated rabbit intestine.
Pressor activity was correlated strongly with mydriatic potency. Exophthalmos, salivation and piomotor effects in the mouse usually, but not always, were associated with pressor properties.
Footnotes
- Received October 24, 1947.
- 1948 by The American Society for Pharmacology and Experimental Therapeutics
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