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樟脑对烟碱型乙酰胆碱受体的非竞争性抑制作用。

Noncompetitive inhibition by camphor of nicotinic acetylcholine receptors.

作者信息

Park T J, Seo H K, Kang B J, Kim K T

机构信息

Department of Life Science, Division of Molecular and Life Science, Pohang University of Science and Technology, San 31, Hyoja Dong, 790-784, Pohang, Korea.

出版信息

Biochem Pharmacol. 2001 Apr 1;61(7):787-93. doi: 10.1016/s0006-2952(01)00547-0.

DOI:10.1016/s0006-2952(01)00547-0
PMID:11274963
Abstract

The effect of camphor, a monoterpenoid, on catecholamine secretion was investigated in bovine adrenal chromaffin cells. Camphor inhibited [3H]norepinephrine ([3H]NE) secretion induced by a nicotinic acetylcholine receptor (nAChR) agonist, 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP), with a half-maximal inhibitory concentration (IC50) of 70 +/- 12 microM. In addition, camphor inhibited the rise in cytosolic calcium ([Ca2+]i) and sodium ([Na+]i) induced by DMPP with IC50 values of 88 +/- 32 and 19 +/- 2 microM, respectively, suggesting that the activity of nAChRs is also inhibited by camphor. On the other hand, binding of [3H]nicotine to nAChRs was not affected by camphor. [Ca2+]i increases induced by high K+, veratridine, and bradykinin were not affected by camphor. The data suggest that camphor specifically inhibits catecholamine secretion by blocking nAChRs without affecting agonist binding.

摘要

研究了单萜类化合物樟脑对牛肾上腺嗜铬细胞儿茶酚胺分泌的影响。樟脑抑制了烟碱型乙酰胆碱受体(nAChR)激动剂1,1-二甲基-4-苯基哌嗪碘化物(DMPP)诱导的[3H]去甲肾上腺素([3H]NE)分泌,其半数最大抑制浓度(IC50)为70±12微摩尔。此外,樟脑抑制了DMPP诱导的细胞内钙([Ca2+]i)和钠([Na+]i)浓度升高,IC50值分别为88±32和19±2微摩尔,这表明nAChRs的活性也受到樟脑的抑制。另一方面,[3H]尼古丁与nAChRs的结合不受樟脑影响。高钾、藜芦碱和缓激肽诱导的[Ca2+]i升高不受樟脑影响。数据表明,樟脑通过阻断nAChRs特异性抑制儿茶酚胺分泌,而不影响激动剂结合。

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