Ro 5-4864 对人心房肌条具有负性肌力作用，且该作用不受 PK 11195 的拮抗。

Ro 5-4864 has a negative inotropic effect on human atrial muscle strips that is not antagonized by PK 11195.

作者信息

Shany E, Hochhauser E, Halpern P, Vidne B, Gavish M, Geller E, Hasharoni A, Barak Y, Yakirevich V

机构信息

Pediatric Division, Soroka Medical Center, Beersheba, Israel.

出版信息

Eur J Pharmacol. 1994 Mar 3;253(3):231-6. doi: 10.1016/0014-2999(94)90196-1.

DOI:10.1016/0014-2999(94)90196-1

PMID:8200417

Abstract

The effects of Ro 5-4864, a peripheral benzodiazepine receptor agonist (9 x 10(-6) M and 9 x 10(-5) M) and of PK 11195, a peripheral benzodiazepine receptor antagonist (3 x 10(-6) M and 3 x 10(-5) M), alone or together, on contraction parameters of human atrial muscle strips were studied. Atrial muscle strips were obtained from patients undergoing cardiac surgery. The strips were suspended in Krebs-Henseleit solution at 36.8 +/- 0.2 degrees C, connected to an isometric force transducer and then stimulated at 15 V above threshold and paced at 1.5 Hz. Ro 5-4864 at its higher concentration, alone or mixed with PK 11195 at both concentrations, depressed the contraction amplitude to 80% of the control value (P < 0.05). In conclusion, Ro 5-4864 had a small but significant depressant effect on the contraction amplitude of human atrial strips. Surprisingly, this effect was not reversed by the peripheral benzodiazepine receptor antagonist PK 11195.

摘要

研究了外周苯二氮䓬受体激动剂Ro 5-4864（9×10⁻⁶ M和9×10⁻⁵ M）以及外周苯二氮䓬受体拮抗剂PK 11195（3×10⁻⁶ M和3×10⁻⁵ M）单独或联合使用对人心房肌条收缩参数的影响。心房肌条取自接受心脏手术的患者。肌条悬浮于36.8±0.2℃的克雷布斯-亨泽莱特溶液中，连接至等长力传感器，然后在高于阈值15 V的电压下刺激，起搏频率为1.5 Hz。较高浓度的Ro 5-4864单独使用或与两种浓度的PK 11195混合使用时，收缩幅度降至对照值的80%（P<0.05）。总之，Ro 5-4864对人心房肌条的收缩幅度有轻微但显著的抑制作用。令人惊讶的是，外周苯二氮䓬受体拮抗剂PK 11195并未逆转这种作用。