The blockade of alpha 2-adrenoceptors by the PNMT inhibitaor SK&F 64139

European Journal of Pharmacology
M GoldsteinR G Pendleton

Abstract

Three tetrahydroisoquinolines were tested for activity on central alpha 2-adrenoceptors by determining their ability to inhibit [3H]clonidine binding to rat cerebral cortical membrane homogenates. The compounds included the PNMT inhibitors SK&F 64139 (7,8-dichloro-1,2,3,4-tetrahydroisoquinoline) and SK&F 29661 (1,2,3,4-tetrahydroisoquinoline 7-sulfonamide) as well as SK&F 72223 (5,8-dimethoxy-1,2,3,4-tetrahydroisoquinoline) a structural analogue inactive as a PNMT inhibitor. SK&F 64139 and SK&F 72223 but not SK&F 29661 inhibited [3H]clonidine binding. Studies in the isolated guinea pig atrium confirmed that SK&F 64139 and SK&F 72223 are alpha 2-adrenoceptor antagonists.

References

Nov 1, 1979·Naunyn-Schmiedeberg's Archives of Pharmacology·J P Hieble, R G Pendleton
Mar 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·W S Young, M J Kuhar
Aug 22, 1980·European Journal of Pharmacology·R G PendletonJ M Roesler

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Citations

Apr 1, 1982·Naunyn-Schmiedeberg's Archives of Pharmacology·R G PendletonD A Miller
Nov 5, 1981·European Journal of Pharmacology·R G PendletonJ P Hieble
Sep 1, 1984·Journal of Autonomic Pharmacology·L G Howes
Jun 1, 1989·Journal of Neuroendocrinology·R V GalloD O'Sullivan
Jan 1, 1982·Clinical and Experimental Hypertension. Part A, Theory and Practice·M R GoldbergD Robertson
Nov 12, 2020·International Journal of Molecular Sciences·Marina Arribas-BlázquezAntonio R Artalejo

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