Mestre M, Carriot T, Belin C, Uzan A, Renault C, Dubroeucq M C, Guérémy C, Le Fur G
Life Sci. 1984 Aug 27;35(9):953-62. doi: 10.1016/0024-3205(84)90661-1.
RO5-4864 decreased in a dose-dependent manner, from 3 X 10(-9) M to 3 X 10(-6) M, the duration of intracellular action potential and the contractility in a guinea pig preparation. Diazepam was less effective and clonazepam inactive. The effects of RO5-4864 were GABA-independent and antagonized by PK 11195 but not by the selective antagonist of the brain type benzodiazepine receptors RO15-1788. These results show the pharmacological relevance of peripheral type benzodiazepine binding sites at the cardiac level.
RO5 - 4864在豚鼠标本中，以剂量依赖性方式降低，从3×10⁻⁹M降至3×10⁻⁶M，细胞内动作电位持续时间和收缩力也随之降低。地西泮效果较差，氯硝西泮则无活性。RO5 - 4864的作用不依赖γ-氨基丁酸（GABA），且被PK 11195拮抗，但不被脑型苯二氮䓬受体的选择性拮抗剂RO15 - 1788拮抗。这些结果表明外周型苯二氮䓬结合位点在心脏水平具有药理学相关性。
