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Histamine release from human basophils by pepstatin A

  • Histamine and Kinins
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Abstract

Pepstatin A, a pentapeptide isolated from cultures of actinomycetes, induced histamine secretion from human basophils in the concentration range of 3×10−7 to 10−4 M. The characteristics of this reaction were similar to those of f-met-peptide-induced histamine release: pepstatin A-induced release required Ca2+ and the release reaction was complete within 2 min at 22 or 37°C, but did not occur at 4°C. Release by both pepstatin a and f-met-peptide was reversibly inhibited by two non-releasing analogs of f-met-peptide, CBZ-Phe-Met and BOC-Met-Leu-Phe, Further, there was complete cross-desensitization between pepstatin A and f-met-peptide, while cells desensitized to pepstatin A released normally with anti-IgE and vice versa. A variety of pharmacological agents had similar effects on both pepstatin A and f-met-peptide-induced release (e.g., no enhancement with D2O; marked enhancement with cytochalasin B). We suggest that pepstatin A induces histamine release from human basophils by activating a cell surface receptor(s), also activated by the synthetic tripeptide f-met-peptide.

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Abbreviations

Anti-IgE:

rabbit anti-Fc

BOC-Met-Leu-Phe:

N-t-BOC-methionyl-l-leucyl-l-phenylalanine

CBZ-Phe-Met:

carbobenzoxy-phenylalanylmethionine

EDTA:

ethylenediaminetertraacetic acid

f-met-peptide:

formyl-methionyl-l-leucyl-l-phenylalanine

PIPES:

piperazine-N,N′-bis(2-ethanesulphonic acid)

P:

25 mM PIPES buffer, 110 mM NaCl, 5 mM KCl, pH 7.4

PC:

PIPES buffer containing 2.0 mM CaCl2.

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Marone, G., Columbo, M., Soppelsa, L. et al. Histamine release from human basophils by pepstatin A. Agents and Actions 16, 306–309 (1985). https://doi.org/10.1007/BF01982863

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  • DOI: https://doi.org/10.1007/BF01982863

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