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Congeners of Pempidine with High Ganglion-blocking Activity

Abstract

RESEARCH in these Laboratories on new hypotensive drugs has in recent years centred on the development of compounds exhibiting both a high level of ganglion-blocking activity and good absorption after oral administration. The first phase of this work culminated in the discovery of 1:2:2:6:6:-pentamethylpiperidine, pempidine1. In clinical use the good absorption and conveniently rapid excretion characteristics of this drug combine to make it a useful advance in the management of essential hypertension2.

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References

  1. Lee, G. E., Wragg, W. R., Corne, S. J., Edge, N. D., and Reading, H. W., Nature, 181, 1717 (1958). Corne, S. J., and Edge, N. D., Brit. J. Pharmacol., 13, 339 (1958). The independent discovery of the ganglion-blocking activity of 1:2:2:6:6-pentamethylpiperidine by an entirely different approach has also been reported by Spinks, A., and Young, E. H. P., Nature, 181, 1397 (1958). Spinks, A., Young, E. H. P., Farrington, J. A., and Dunlop, D., Brit. J. Pharmacol., 13, 501 (1958).

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  2. Harington, M., Kincaid-Smith, P., and Milne, M. D., Lancet, ii, 6 (1958).

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BRETHERICK, L., LEE, G., LUNT, E. et al. Congeners of Pempidine with High Ganglion-blocking Activity. Nature 184, 1707–1709 (1959). https://doi.org/10.1038/1841707a0

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