荷包牡丹碱可阻断猪离体中间叶细胞中的烟碱型乙酰胆碱反应。
Bicuculline blocks nicotinic acetylcholine response in isolated intermediate lobe cells of the pig.
作者信息
Zhang Z W, Feltz P
机构信息
Institut de Physiologie (UA309 CNRS), Université Louis Pasteur, Strasbourg, France.
出版信息
Br J Pharmacol. 1991 Jan;102(1):19-22. doi: 10.1111/j.1476-5381.1991.tb12125.x.
Abstract
- The effect of bicuculline on nicotinic acetylcholine (ACh) responses in isolated intermediate lobe (IL) cells of the pig was investigated by use of patch-clamp techniques. Bicuculline was found to reduce ACh-evoked whole-cell currents (IACh) in all cells tested (n = 40). 2. The blocking effect of bicuculline on IACh was dose-dependent, the concentration producing half-maximal blockade being 43.8 microM. 3. The blockade of IACh by bicuculline was not voltage-dependent at membrane potentials above -60 mV, but a slight voltage-dependence was observed at holding potentials (HP) of -80 and -100 mV. 4. The inhibitory effect of bicuculline on IACh was partially competitive at a HP of -60 mV. 5. Neither SR 95531, a pyridazinyl gamma-aminobutyric acid derivative, nor t-butylbicyclophosphorothionate (TBPS) blocked IACh in IL cells. 6. It is concluded that bicuculline interacts directly with the ACh receptor-ionophore complex on porcine IL cells.
摘要
- 运用膜片钳技术研究了荷包牡丹碱对猪离体中间叶（IL）细胞烟碱型乙酰胆碱（ACh）反应的影响。结果发现，荷包牡丹碱可降低所有受试细胞（n = 40）中ACh诱发的全细胞电流（IACh）。2. 荷包牡丹碱对IACh的阻断作用呈剂量依赖性，产生半数最大阻断作用的浓度为43.8微摩尔。3. 在膜电位高于 -60毫伏时，荷包牡丹碱对IACh的阻断不依赖电压，但在 -80和 -100毫伏的钳制电位（HP）下观察到轻微的电压依赖性。4. 在 -60毫伏的钳制电位下，荷包牡丹碱对IACh的抑制作用具有部分竞争性。5. 哒嗪基γ-氨基丁酸衍生物SR 95531和硫代丁基双环磷化物（TBPS）均未阻断IL细胞中的IACh。6. 得出结论：荷包牡丹碱直接与猪IL细胞上的ACh受体-离子通道复合物相互作用。
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