钙拮抗剂对大鼠皮质突触体（Na+ + K+）-ATP酶、Mg2+-ATP酶和Ca2+-ATP酶活性的影响。

Effects of calcium antagonists on (Na+ + K+)-ATPase, Mg2+-ATPase and Ca2+-ATPase activities of rat cortical synaptosomes.

Chiang D H, Wei J W

Institute of Neurosciences, National Yang-Ming Medical College, Taipei, Taiwan, Republic of China.

Gen Pharmacol. 1987;18(5):563-7. doi: 10.1016/0306-3623(87)90082-6.

Abstract

The effects of 11 calcium antagonists on (Na+ + K+)-ATPase, Mg2+-ATPase and Ca2+-ATPase activities of rat cortical synaptosomes were studied. 2. All the calcium antagonists studied had inhibitory effects on ouabain-sensitive (Na+ + K+)-ATPase, Mg2+-ATPase and Ca2+-ATPase activities in synaptosomes at high concentrations (10 or 100 microM). 3. Calcium antagonists such as trifluoperazine, flunarizine and cinnarizine had inhibitory effects on Ca2+-ATPase activity at low concentrations (1-10 microM). 4. Trifluoperazine and La3+ had inhibitory effects on Mg2+-ATPase activity at low concentration (1 microM). 5. Our results suggest that most of the calcium antagonists studied have little effects on neuronal (Na+ + K+)-ATPase, Mg2+-ATPase and Ca2+-ATPase activities at therapeutic dose ranges (1 microM or lower).

摘要

研究了11种钙拮抗剂对大鼠皮质突触体中（钠+钾）-ATP酶、镁离子-ATP酶和钙离子-ATP酶活性的影响。2. 所有研究的钙拮抗剂在高浓度（10或100微摩尔）时对突触体中哇巴因敏感的（钠+钾）-ATP酶、镁离子-ATP酶和钙离子-ATP酶活性均有抑制作用。3. 三氟拉嗪、氟桂利嗪和桂利嗪等钙拮抗剂在低浓度（1-10微摩尔）时对钙离子-ATP酶活性有抑制作用。4. 三氟拉嗪和镧离子在低浓度（1微摩尔）时对镁离子-ATP酶活性有抑制作用。5. 我们的结果表明，大多数研究的钙拮抗剂在治疗剂量范围（1微摩尔或更低）对神经元（钠+钾）-ATP酶、镁离子-ATP酶和钙离子-ATP酶活性影响很小。