Abstract
Polymyxin B, d-tubocurarine and morphine released granule-bound histamine from rat mast cells, in vitro, but not the cytoplasmic enzyme lactic dehydrogenase. Rat mast cells treated with any of these drugs or with stilbamidine were not stained by the vital dye trypan blue. because of the fluorescence of stilbamidine, release of lactic acid dehydrogenase could not be measured in the presence of this drug. It is concluded that these four drugs release histamine by the "selective" degranulation mechanism described for compound 48/80, rather than the "nonselective" mechanism described for Triton X-100, which is characterized by destruction of cell membranes, resulting in release of cytoplasmic constituents and uptake of trypan blue. The order of potency as histamine releasers in 48/80 ≥ polymyxin B > stilbamidine > d-tubocurarine > morphine. All basic, small-molecule histamine releasers, except the aliphatic amines, may be selective releasers. Some of the clinically observed side effects of these drugs are probaby due to histamine release.
Footnotes
- Received March 25, 1970.
- Accepted July 12, 1970.
- © 1970 by The Williams & Wilkins Co.
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