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RMI 12330A,一种对医用水蛭节段神经节中腺苷酸环化酶和环磷酸腺苷磷酸二酯酶活性具有抑制作用的物质。

RMI 12330A, an inhibitor of adenylate cyclase and cyclic AMP-phosphodiesterase activities in the segmental ganglia of the leech Hirudo medicinalis.

作者信息

Biondi C, Campi A L, Pareschi M C, Portolan A, Ferretti M E

机构信息

Institute of General Physiology, Ferrara, Italy.

出版信息

Neurosci Lett. 1990 Jun 8;113(3):322-7. doi: 10.1016/0304-3940(90)90605-9.

Abstract

The effect of RMI 12330A, an inhibitor of basal as well as serotonin-stimulated adenylate cyclase in the segmental ganglia of the leech Hirudo medicinalis, has been tested on cyclic AMP-phosphodiesterase activity in the same tissue. The drug dose-dependently inhibits high and low affinity enzyme, an effect first evident at an RMI 12330A concentration of 0.5 mM. For both enzyme activities the drug reduces Vmax without substantially influencing Km values. Both basal and serotonin-stimulated adenylate cyclase as well as cyclic AMP-phosphodiesterase activities are inhibited by RMI 12330A in a non-competitive manner.

摘要

已对水蛭药用水蛭节段神经节中基础及血清素刺激的腺苷酸环化酶的抑制剂RMI 12330A对同一组织中环磷酸腺苷磷酸二酯酶活性的影响进行了测试。该药物剂量依赖性地抑制高亲和力和低亲和力酶,在RMI 12330A浓度为0.5 mM时首次明显出现这种效应。对于这两种酶活性,该药物降低了最大反应速度(Vmax),而对米氏常数(Km)值没有实质性影响。RMI 12330A以非竞争性方式抑制基础及血清素刺激的腺苷酸环化酶以及环磷酸腺苷磷酸二酯酶的活性。

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