Matlib M A, Schwartz A
Life Sci. 1983 Jun 20;32(25):2837-42. doi: 10.1016/0024-3205(83)90319-3.
Diltiazem, diazepam, and clonazepam effectively inhibit Na+-induced Ca2+ release from mitochondria isolated from rabbit heart and rat brain. At 10 mM NaCl, the 50% inhibition of the rate of Ca2+ release occurred at 5, 7, 40 and 350 microM of clonazepam d-cis-diltiazem, diazepam and 1-cis-diltiazem, respectively. Ro 15-1788 (imidazobenzodiazepine), a pharmacological antagonist presumably at the high affinity site of diazepam, had no effect either alone or in combination with diltiazem or diazepam. We suggest that the Na+/Ca2+ exchange carrier in mitochondria may be a common receptor for diltiazem and diazepam.
地尔硫䓬、地西泮和氯硝西泮可有效抑制从兔心脏和大鼠脑部分离出的线粒体中由钠离子诱导的钙离子释放。在10 mM氯化钠存在的情况下,氯硝西泮、d-顺式地尔硫䓬、地西泮和1-顺式地尔硫䓬分别在5、7、40和350 microM时对钙离子释放速率产生50%的抑制作用。Ro 15-1788(咪唑并苯二氮䓬),一种可能作用于地西泮高亲和力位点的药理学拮抗剂,单独使用或与地尔硫䓬或地西泮联合使用均无效果。我们认为线粒体中的钠/钙交换载体可能是地尔硫䓬和地西泮的共同受体。