钙通道阻滞剂与非神经元苯二氮䓬结合位点的相互作用。
Interaction of calcium channel blockers with non-neuronal benzodiazepine binding sites.
作者信息
Cantor E H, Kenessey A, Semenuk G, Spector S
出版信息
Proc Natl Acad Sci U S A. 1984 Mar;81(5):1549-52. doi: 10.1073/pnas.81.5.1549.
Abstract
The ability of calcium channel blockers to displace the binding of benzodiazepine ligands was investigated in rat heart, kidney, and brain. The dihydropyridine calcium channel blockers nifedipine and nitrendipine displaced the binding of the non-neuronal-site ligand [3H]Ro5-4864, but not that of the neuronal-site ligands [3H]flurazepam or [3H]clonazepam. The inhibition was competitive, with Ki values in the micromolar range. Other calcium channel blockers--i.e., verapamil and diltiazem--were inactive at both sites. Thus, non-neuronal benzodiazepines bind to a class of sites that also binds dihydropyridines. This implies a role for benzodiazepines in the mediation of calcium-dependent phenomena.
摘要
研究了钙通道阻滞剂在大鼠心脏、肾脏和大脑中取代苯二氮䓬配体结合的能力。二氢吡啶类钙通道阻滞剂硝苯地平和尼群地平能取代非神经元位点配体[3H]Ro5 - 4864的结合，但不能取代神经元位点配体[3H]氟西泮或[3H]氯硝西泮的结合。这种抑制是竞争性的，Ki值在微摩尔范围内。其他钙通道阻滞剂，即维拉帕米和地尔硫䓬，在这两个位点均无活性。因此，非神经元苯二氮䓬类药物与一类也能结合二氢吡啶的位点结合。这意味着苯二氮䓬类药物在钙依赖性现象的介导中发挥作用。
相似文献
1
Interaction of calcium channel blockers with non-neuronal benzodiazepine binding sites.钙通道阻滞剂与非神经元苯二氮䓬结合位点的相互作用。
Proc Natl Acad Sci U S A. 1984 Mar;81(5):1549-52. doi: 10.1073/pnas.81.5.1549.
2
The interaction of phenylalkylamine calcium channel blockers with the 1,4-dihydropyridine binding site.苯烷基胺类钙通道阻滞剂与1,4-二氢吡啶结合位点的相互作用。
J Mol Cell Cardiol. 1986 Sep;18(9):963-74. doi: 10.1016/s0022-2828(86)80010-4.
3
Inhibition of type A GABA receptors by L-type calcium channel blockers.L型钙通道阻滞剂对A型γ-氨基丁酸受体的抑制作用。
Neuroscience. 2004;124(1):195-206. doi: 10.1016/j.neuroscience.2003.12.005.
4
Interaction of verapamil and other calcium channel blockers with alpha 1- and alpha 2-adrenergic receptors.维拉帕米及其他钙通道阻滞剂与α1和α2肾上腺素能受体的相互作用。
Circ Res. 1983 Feb;52(2):226-31. doi: 10.1161/01.res.52.2.226.
5
The binding of [3H]nitrendipine to receptors for calcium channel antagonists in the heart, cerebral cortex, and ileum of rats.[3H]尼群地平与大鼠心脏、大脑皮层及回肠中钙通道拮抗剂受体的结合。
Life Sci. 1982 Jun 21;30(25):2191-202. doi: 10.1016/0024-3205(82)90293-4.
6
7
Allosteric modulation by diltiazem and verapamil of [3H]nitrendipine binding to calcium channel sites in rat brain.地尔硫䓬和维拉帕米对[³H]尼群地平与大鼠脑钙通道位点结合的变构调节作用。
Proc West Pharmacol Soc. 1983;26:219-24.
8
Effects of temperature and allosteric modulators on [3H] nitrendipine binding: methods for detecting potential Ca2+ channel blockers.温度和变构调节剂对[3H]尼群地平结合的影响：检测潜在钙通道阻滞剂的方法
J Recept Res. 1984;4(1-6):557-69. doi: 10.3109/10799898409042573.
9
High-affinity antibodies to the 1,4-dihydropyridine Ca2+-channel blockers.针对1,4 - 二氢吡啶类钙离子通道阻滞剂的高亲和力抗体。
Proc Natl Acad Sci U S A. 1986 May;83(9):2792-6. doi: 10.1073/pnas.83.9.2792.
10
Tissue response selectivity of calcium antagonists is not due to heterogeneity of [3H]-nitrendipine binding sites.钙拮抗剂的组织反应选择性并非源于[3H]-尼群地平结合位点的异质性。
Br J Pharmacol. 1984 Jun;82(2):309-20. doi: 10.1111/j.1476-5381.1984.tb10765.x.
引用本文的文献
1
Developmental expression of translocator protein/peripheral benzodiazepine receptor in reproductive tissues.转位蛋白/外周苯二氮䓬受体在生殖组织中的发育表达。
PLoS One. 2013 Sep 5;8(9):e74509. doi: 10.1371/journal.pone.0074509. eCollection 2013.
2
Specific ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in human colorectal cancer cells.外周苯二氮䓬受体的特异性配体可诱导人结肠癌细胞凋亡并使其细胞周期停滞。
Br J Cancer. 2001 Nov 30;85(11):1771-80. doi: 10.1054/bjoc.2001.2181.
3
Pharmacological relevance of peripheral type benzodiazepine receptors on motor nerve and skeletal muscle.外周型苯二氮䓬受体在运动神经和骨骼肌上的药理学意义。
Br J Pharmacol. 1994 May;112(1):257-61. doi: 10.1111/j.1476-5381.1994.tb13060.x.
4
A novel 1,4-dihydropyridine-binding site on mitochondrial membranes from guinea-pig heart, liver and kidney.豚鼠心脏、肝脏和肾脏线粒体膜上的一个新型1,4 - 二氢吡啶结合位点。
Biochem J. 1988 Jul 1;253(1):49-58. doi: 10.1042/bj2530049.
5
Effect of benzodiazepines on the proliferation of mouse spleen lymphocytes in vitro.苯二氮䓬类药物对小鼠脾淋巴细胞体外增殖的影响。
J Neural Transm. 1988;73(2):161-6. doi: 10.1007/BF01243387.
6
Molecular biology of inhibitory amino acid receptors.抑制性氨基酸受体的分子生物学
Mol Neurobiol. 1987 Spring-Summer;1(1-2):155-89. doi: 10.1007/BF02935267.
7
Nitrendipine decreases benzodiazepine withdrawal seizures but not the development of benzodiazepine tolerance or withdrawal signs.尼群地平可减少苯二氮䓬类药物戒断性癫痫发作，但不能减少苯二氮䓬类药物耐受性的形成或戒断症状。
Br J Pharmacol. 1990 Nov;101(3):691-7. doi: 10.1111/j.1476-5381.1990.tb14142.x.
本文引用的文献
1
Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
J Biol Chem. 1951 Nov;193(1):265-75.
2
Specific calcium antagonist binding sites in brain.大脑中的特异性钙拮抗剂结合位点。
Life Sci. 1982 Oct 11;31(15):1575-85. doi: 10.1016/0024-3205(82)90049-2.
3
The interaction of [3H]nitrendipine with receptors for calcium antagonists in the cerebral cortex and heart of rats.[3H]尼群地平与大鼠大脑皮层及心脏中钙拮抗剂受体的相互作用。
Biochem Biophys Res Commun. 1982 Feb 11;104(3):937-43. doi: 10.1016/0006-291x(82)91339-0.
4
Characterization of binding of the Ca++ channel antagonist, [3H]nitrendipine, to guinea-pig ileal smooth muscle.钙离子通道拮抗剂[3H]尼群地平与豚鼠回肠平滑肌结合的特性研究
J Pharmacol Exp Ther. 1983 May;225(2):291-309.
5
Identification of voltage operated calcium channels by binding studies: differentiation of subclasses of calcium antagonist drugs with 3H-nimodipine radioligand binding.通过结合研究鉴定电压门控钙通道：用3H-尼莫地平放射性配体结合法区分钙拮抗剂药物的亚类。
J Recept Res. 1983;3(1-2):177-90. doi: 10.3109/10799898309041932.
6
Properties of two benzodiazepine binding sites in spinal cord.脊髓中两种苯二氮䓬结合位点的特性
Neuropharmacology. 1983 Jan;22(1):115-8. doi: 10.1016/0028-3908(83)90269-1.
7
Specific binding of [3H]nitrendipine to membranes from coronary arteries and heart in relation to pharmacological effects. Paradoxical stimulation by diltiazem.[3H]尼群地平与冠状动脉及心脏膜的特异性结合及其药理效应。地尔硫䓬的反常刺激作用。
Biochem Biophys Res Commun. 1982 Sep 16;108(1):110-7. doi: 10.1016/0006-291x(82)91838-1.
8
Does the organic calcium channel blocker D600 act from inside or outside on the cardiac cell membrane?有机钙通道阻滞剂D600是在心肌细胞膜内侧还是外侧发挥作用？
Pflugers Arch. 1982 Jun;393(4):287-91. doi: 10.1007/BF00581411.
9
Characterization of peripheral-type benzodiazepine binding sites in brain using [3H]Ro 5-4864.使用[3H]Ro 5-4864对脑中外周型苯二氮䓬结合位点进行表征。
Mol Pharmacol. 1982 Jul;22(1):26-32.
10
Micromolar affinity benzodiazepine receptors: identification and characterization in central nervous system.微摩尔亲和力苯二氮䓬受体：中枢神经系统中的鉴定与特性研究
Science. 1982 Jun 11;216(4551):1247-50. doi: 10.1126/science.6281893.
Zotero 插件