Abstract
2,6-XYLYLETHER bromide (I), bretylium (II) and guanethidine (III) cause several similar adrenergic neurone blocking effects. The finding of similar properties in the benzyl- and phenoxy-ethylguanidines (IV), (V) and (VI) supported the view that quaternary ammonium and guanidine groups might have similar influences on pharmacological action1. These compounds are strongly basic and almost completely ionized at physiological pH values. It was therefore of interest to examine the compounds (VII) wherein high basicity was conferred by an amidine group. Several of these compounds showed powerful adrenergic neurone blocking properties, one of the most potent being N-[2-(hexahydro-1 -azepinyl)ethyl]acetamidine (VII: n=6, m=2, R = CH3) (BW 1113C60), which was prepared and tested as a stable non-deliquescent dihydrochloride2.
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References
Boura, A. L. A., Copp, F. C., Green, A. F., Hodson, H. F., Ruffell, G. K., Sim, M. F., Walton, E., and Grivsky, E. M., Nature, 191, 1312 (1961).
Copp, F. C., Brit. Pat. App. 2,476/61 (The Wellcome Foundation, Ltd.).
Boura, A. L. A., and Green, A. F., Brit. J. Pharmacol., 19, 13 (1962).
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Mull, R. P., Egbert, M. E., and Dapero, M. R., J. Org. Chem., 25, 1953 (1960).
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BOURA, A., COPP, F. & GREEN, A. Amidines as Adrenergic Neurone Blocking Agents. Nature 195, 1213–1214 (1962). https://doi.org/10.1038/1951213a0
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DOI: https://doi.org/10.1038/1951213a0
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