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H 3 ‐Receptors Control Histamine Release in Human Brain
Author(s) -
Arrang JeanMichel,
Devaux Bertrand,
Chodkiewicz JeanPaul,
Schwartz JeanCharles
Publication year - 1988
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1988.tb04841.x
Subject(s) - histamine , histamine h3 receptor , thioperamide , autoreceptor , histamine receptor , histamine h2 receptor , histamine h1 receptor , chemistry , receptor , extracellular , medicine , pharmacology , endocrinology , biology , biochemistry , antagonist
The regulation of histamine release was studied on slices prepared from pieces of human cerebral cortex removed during neurosurgery and labeled with l‐[ 3 H]‐histidine. Depolarization by increased extracellular K + concentration induced [ 3 H]histamine release, although to a lesser extent than from rat brain slices. Exogenous histamine reduced by up to 60% the K + ‐evoked release, with an EC 50 of 3.5 ± 0.5 × 10 − ‐ 8 M . The H 3 ‐receptor antagonists impromidine and thioperamide reversed the histamine effect in an apparently competitive manner and enhanced the K + ‐evoked release, indicating a participation of endogenous histamine in the release control process. The potencies of histamine and the H 3 ‐receptor antagonists were similar to those of these agents at presynaptic H 3 ‐autoreceptors controlling [ 3 H]histamine release from rat brain slices. It is concluded that H 3 ‐receptors control histamine release in the human brain.