Abstract
1. N,N-dimethyl 2-chloro-2-phenylethylamine (DMEA), a compound related to the nitrogen mustards and to Dibenamine, produces a severe acute intoxication in cats with death resulting from respiratory failure. In rats the intoxication is characterized by a delayed progressive damage to the central nervous system.
2. DMEA produces adrenergic blockade of immediate onset and relatively short duration.
3. DMEA, additionally, shows muscarinic, nicotinic and curariform qualities.
4. Under conditions in rivo, DMEA rapidlly cyclizes and its ethyleneimmonium ring form mediates all its actions. This ring form combines firmly with receptor cells and cannot be displaced chemically.
5. The relation of these findlings to previous explanations of the mechanism of action of adrenergic blocking haloalkylamines is discussed.
6. The point is made that DMEA is a structural homologue of the β-phenethylamines whose sympathomimetic activity has long been established. It stands among the known adrenergic blocking agents as the one with the closest structural relationships to adrenergic simulating agents.
Footnotes
- Received May 31, 1950.
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