The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons
作者： Haibin Dai , Qiuli Fu , Yao Shen , Weiwei Hu , Zhongmiao Zhang
DOI: 10.1016/J.EJPHAR.2007.01.069
关键词:
摘要: Using the histamine H3 receptor antagonist clobenpropit, roles of receptors in NMDA-induced necrosis were investigated rat cultured cortical neurons. Clobenpropit reversed neurotoxicity a concentration-dependent manner, and showed peak protection at concentration 10(-7) M. This was antagonized by agonist (R)-alpha-methylhistamine, but not H1 pyrilamine or H2 cimetidine. In addition, clobenpropit inhibited GABAA antagonists picrotoxin bicuculline. Further study demonstrated that due to increased GABA release. The inducible release also Furthermore, both adenylyl cyclase inhibitor SQ-22536 protein kinase A (PKA) H-89 clobenpropit. increase intracellular calcium level, which (R)-alpha-methylhistamine. These results indicate enhanced protect against excitotoxicity, induced through cAMP/PKA pathway, reduction level may be involved.
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