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5-羟色胺对非洲爪蟾卵母细胞中表达的神经元乙酰胆碱受体通道的阻断作用。

Block by 5-hydroxytryptamine of neuronal acetylcholine receptor channels expressed in Xenopus oocytes.

作者信息

Nakazawa K, Akiyama T, Inoue K

机构信息

Division of Pharmacology, National Institute of Health Sciences, Tokyo, Japan.

出版信息

Cell Mol Neurobiol. 1995 Aug;15(4):495-500. doi: 10.1007/BF02071882.

Abstract
  1. Effects of 5-hydroxytryptamine (5-HT) on neuronal nicotinic acetylcholine (ACh) receptor channels were investigated by expressing cloned channel subunits in Xenopus oocytes. 2. When channels were expressed with a combination of alpha 3 and beta 4 subunits, 5-HT (10 to 300 microM) reversibly inhibited an inward current activated by 100 microM ACh in a concentration-dependent manner. The inhibition was also observed when alpha 3 subunit was combined with beta 2 subunit instead of beta 4 subunit, or beta 4 subunit was combined with alpha 2 or alpha 4-1 subunit instead of alpha 3 subunit to express channels. 3. Compounds known to antagonize at 5-HT receptors (LY53857, metoclopramide and propranolol) exhibited an agonistic effect: they inhibited the ACh-activated current. 4. The results suggest that 5-HT inhibits recombinant neuronal nicotinic receptor channels through a binding-site distinct from conventional 5-HT receptors. The binding-site may not be attributed to a unique type of channel subunits.
摘要
  1. 通过在非洲爪蟾卵母细胞中表达克隆的通道亚基,研究了5-羟色胺(5-HT)对神经元烟碱型乙酰胆碱(ACh)受体通道的影响。2. 当通道由α3和β4亚基组合表达时,5-HT(10至300微摩尔)以浓度依赖性方式可逆地抑制由100微摩尔ACh激活的内向电流。当α3亚基与β2亚基而非β4亚基组合,或β4亚基与α2或α4-1亚基而非α3亚基组合来表达通道时,也观察到了这种抑制作用。3. 已知能拮抗5-HT受体的化合物(LY53857、甲氧氯普胺和普萘洛尔)表现出激动作用:它们抑制ACh激活的电流。4. 结果表明,5-HT通过一个不同于传统5-HT受体的结合位点抑制重组神经元烟碱型受体通道。该结合位点可能不归因于一种独特类型的通道亚基。

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A proposed new nomenclature for 5-HT receptors.一种关于5-羟色胺受体的新命名提议。
Trends Pharmacol Sci. 1993 Jun;14(6):233-6. doi: 10.1016/0165-6147(93)90016-d.

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