TYRAMINE ANTAGONISTIC PROPERTIES OF AGN 1135, AN IRREVERSIBLE INHIBITOR OF MONOAMINE OXIDASE TYPE B
Open Access
- 1 May 1981
- journal article
- Published by Wiley in British Journal of Pharmacology
- Vol. 73 (1), 65-74
- https://doi.org/10.1111/j.1476-5381.1981.tb16772.x
Abstract
1 The effects of the irreversible monoamine oxidase (MAO) inhibitors, AGN 1133, AGN 1135 and (−)-deprenyl, on tyramine and noradrenaline responses and uptake of [3H]-metaraminol were investigated in the isolated vas deferens of the rat. Uptake of [3H]-metaraminol and [3H]-octopamine was compared in mouse vas deferens. The modification of tyramine and noradrenaline-induced pressor responses by AGN 1133 and AGN 1135 was examined in anaesthetized rats and cats. 2 AGN 1133 (7.5 × 10−6m) greatly potentiated responses to tyramine in the rat isolated vas deferens. Both AGN 1135 and (−)-deprenyl inhibited tyramine responses selectively at concentrations above 10−3m (which caused almost complete inhibition of MAO types A and B) but tyramine responses were potentiated on washing out the inhibitors. 3 AGN 1135 (10−4m) and (−)-deprenyl (10−5m) inhibited [−3H]-metaraminol uptake by about20% in rat and mouse vas deferens; neither inhibitor affected [−3H]-octopamine uptake in mouse vas deferens. Desmethylimipramine (10−6m) inhibited amine uptake by more than 70%. 4 AGN 1133 (1.5 mg/kg) potentiated pressor responses to tyramine in rats and cats whereas AGN 1135 (1.5 mg/kg) did not. 5 AGN 1135 possesses tyramine antagonistic activity which is qualitatively similar to that of (−)-deprenyl but which cannot satisfactorily be explained by inhibition of neuronal or granular amine uptake.Keywords
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