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首页> 外文期刊>Biochemical Pharmacology >N-(4-Trifluoromethylphenyl)amide group of the synthetic histamine receptor agonist inhibits nicotinic acetylcholine receptor-mediated catecholamine secretion.
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N-(4-Trifluoromethylphenyl)amide group of the synthetic histamine receptor agonist inhibits nicotinic acetylcholine receptor-mediated catecholamine secretion.

机译：合成组胺受体激动剂的N-（4-三氟甲基苯基）酰胺基抑制烟碱乙酰胆碱受体介导的儿茶酚胺分泌。

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摘要

The therapeutic targeting of nicotinic receptors requires the identification of drugs that selectively activate or inhibit a limited range of nicotine acetylcholine receptors (nAChRs). In this study, we identified N-(4-trifluoromethylphenyl)amide group of the synthetic histamine receptor ligands, histamine-trifluoromethyltoluide, that act as potent inhibitors of nAChRs in bovine adrenal chromaffin cells. Catecholamine secretion induced by the nAChRs agonist, 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP), was significantly inhibited by histamine-trifluoromethyltoluide. Real time carbon-fiber amperometry confirmed the ability of histamine-trifluoromethyltoluide to inhibit DMPP-induced exocytosis in single chromaffin cells. We also found that histamine-trifluoromethyltoluide inhibited DMPP-induced [Ca(2+)](i) and [Na(+)](i) increases, as well as DMPP-induced inward currents in the absence of extracellular calcium. Histamine-trifluoromethyltoluide had no effect on [(3)H]nicotine binding or on calcium increases induced by high K(+), bradykinin, veratridine, histamine, and benzoylbenzoyl ATP. Among the synthetic histamine receptor ligands, clobenpropit exhibited similarity. In addition, 4'-nitroacetanilide also significantly attenuated nAChR-mediated catecholamine secretion. In conclusion, the N-(4-trifluoromethylphenyl)amide group of the histamine-trifluoromethyltoluide might be the critical moiety in the inhibition of nAChR-mediated CA secretion.
机译：烟碱样受体的治疗靶点需要鉴定选择性激活或抑制有限范围的尼古丁乙酰胆碱受体（nAChRs）的药物。在这项研究中，我们确定了合成的组胺受体配体N-（4-三氟甲基苯基）酰胺基团，组胺-三氟甲基甲苯胺，可作为牛肾上腺嗜铬细胞中nAChRs的有效抑制剂。组胺-三氟甲基甲苯胺显着抑制了nAChRs激动剂1,1-二甲基-4-苯基哌嗪碘化物（DMPP）诱导的儿茶酚胺分泌。实时碳纤维电流分析法证实了组胺三氟甲基甲苯在单嗜铬细胞中抑制DMPP诱导的胞吐作用的能力。我们还发现，在没有细胞外钙的情况下，组胺三氟甲基甲苯抑制DMPP诱导的[Ca（2 +）]（i）和[Na（+）]（i）增加，以及DMPP诱导的内向电流。组胺三氟甲基甲苯甲酰对[（3）H]烟碱结合或高K（+），缓激肽，藜芦，组胺和苯甲酰基苯甲酰ATP诱导的钙增加没有影响。在合成的组胺受体配体中，clobenpropit具有相似性。另外，4'-硝基乙酰苯胺也显着减弱了nAChR介导的儿茶酚胺分泌。总之，组胺-三氟甲基甲苯的N-（4-三氟甲基苯基）酰胺基可能是抑制nAChR介导的CA分泌的关键部分。

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