Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P15088 (mast cell)
 14,925 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Calmodulin content and distribution in rat peritoneal mast cells was determined by radioimmunoassay. Isolated pure mast cells were disrupted by sonication and the total calmodulin content and its distribution were determined. Calmodulin bound to the membranes was released by heating with 0.1% Lubrol PX to 95 degrees C for 5 min. The total calmodulin content of mast cells was found to be 160 +/- 14 ng/10(6) cells (9.4 +/- 0.82 pmoles/10(6) cells). The highest amount (68%) was present in the supernatant representing the cytosol. The next highest amount (26%) was found in the composite fraction consisting of mitochondria, endoplasmic reticulum, Golgi vesicles and plasma membrane (100,000 g pellet). The mast cell granules contained 4% of the total calmodulin. Trifluoperazine (TFP) was used as an antagonist to explore the role of calmodulin in histamine secretion. At 10 microM concentration, TFP caused a negligible spontaneous histamine release by its membrane effect. TFP (10 microM) inhibited histamine release by all the three secretagogues used, but the degree of inhibition varied: 60% with antigen, 40% with compound 48/80 and 20% with ionophore A23187. It is suggested that the TFP effect is due to calmodulin-antagonism and interference with the activation of enzymes, essential to the secretory process.
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PMID:Calmodulin in mast cells and its role in histamine secretion. 240 58

The calmodulin inhibitor trifluoperazine represses compound 48/80-induced histamine release. The effects appear to take place at a step distal to the entrance of calcium into the cell. Trifluoperazine in itself induces histamine release from rat peritoneal mast cells. This release is totally independent of extracellular calcium and at high concentrations of the drug (greater than or equal to 20 microM), it is due to lysis of the cells. Trifluoperazine reduces the compound 48/80-induced decrease in mast cell cyclic AMP content, probably by inhibiting a cyclic nucleotide phosphodiesterase. The trifluoperazine-induced repression of histamine release does not seem to be correlated to the ability of the drug to alter the compound 48/80 induced changes in cyclic AMP.
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PMID:Cyclic AMP levels during stimulation and inhibition of histamine release from rat mast cells by the calmodulin inhibitor trifluoperazine. 618 3