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A comparison of dimaprit, nordimaprit, methylamine and chloroquine as inhibitors of mitogen‐induced lymphocyte activation
Author(s) -
Dale M. Maureen,
Ladd R.
Publication year - 1984
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1984.tb10145.x
Subject(s) - methylamine , dimaprit , chloroquine , histamine , mechanism of action , chemistry , pharmacology , lymphocyte , biology , receptor , biochemistry , histamine h2 receptor , immunology , in vitro , malaria , antagonist
1 Methylamine and chloroquine both ‘lysosomotropic’ agents (i.e. agents which sequester in lysosomes) caused a dose‐related inhibition of mitogen‐induced lymphocyte activation in the concentrations which have previously been shown to increase the pH of lysosomes. 2 The dose‐response curves of inhibition of mitogen‐induced lymphocyte activation for chloroquine and methylamine are very steep and are similar to the dose‐response curves obtained with dimaprit and nordimaprit, but very different from the flat dose‐response curves previously described for histamine. Approximate IC 50 values were methylamine 6.4 m m , dimaprit 0.13 m m , nordimaprit 0.03 m m and chloroquine 18 μ m.3 It is suggested that the mechanism of action of methylamine and chloroquine may be related to their lysosomotropic action and consequent interference with ligand‐receptor processing, and that dimaprit and nordimaprit but not histamine may act by a similar mechanism.