可溶性鸟苷酸环化酶的选择性抑制剂对一氧化氮能舒张的抑制作用。
Inhibition of nitrergic relaxations by a selective inhibitor of the soluble guanylate cyclase.
作者信息
Cellek S, Kasakov L, Moncada S
机构信息
Wellcome Research Laboratories, Beckenham, Kent.
出版信息
Br J Pharmacol. 1996 May;118(1):137-40. doi: 10.1111/j.1476-5381.1996.tb15376.x.
Abstract
- The actions of 1H-[1,2,4]oxadiazolo[4,3,-a]quinoxalin-1-one (ODQ), a specific inhibitor of the soluble guanylate cyclase (SGC), were investigated in the rabbit anococcygeus muscle. 2. ODQ (1 nM-1 microM) inhibited in a concentration-dependent manner the relaxations induced by electrical field stimulation (EFS; 50 V, 0.3 ms duration, 1 Hz, for 5 s, every 120 s). 3. ODQ (1 microM) also inhibited the relaxations elicited by EFS (50 V, 0.3 ms duration, 1, 2.5, 5, 10 Hz, for 5 s) and sodium nitroprusside (SNP; 1 microM) without affecting those induced by isoprenaline (1 microM), atrial natriuretic peptide (ANP; 100 nM) or an analogue of cyclic GMP (8-pCPT-cyclic GMP; 500 microM). 4. ODQ (1 microM) inhibited the elevations in the concentration of cyclic GMP induced by SNP or EFS, but not by ANP. ODQ did not affect the concentrations of cyclic AMP. 5. Nitrergic relaxation in this tissue appears, therefore, to be mediated via activation of SGC.
摘要
- 在兔肛门尾骨肌中研究了可溶性鸟苷酸环化酶（SGC）的特异性抑制剂1H-[1,2,4]恶二唑并[4,3,-a]喹喔啉-1-酮（ODQ）的作用。2. ODQ（1 nM - 1 microM）以浓度依赖性方式抑制电场刺激（EFS；50 V，0.3 ms持续时间，1 Hz，持续5 s，每120 s一次）诱导的舒张。3. ODQ（1 microM）也抑制EFS（50 V，0.3 ms持续时间，1、2.5、5、10 Hz，持续5 s）和硝普钠（SNP；1 microM）引起的舒张，而不影响异丙肾上腺素（1 microM）、心钠素（ANP；100 nM）或环鸟苷酸类似物（8 - pCPT - 环鸟苷酸；500 microM）诱导的舒张。4. ODQ（1 microM）抑制SNP或EFS诱导的环鸟苷酸浓度升高，但不抑制ANP诱导的升高。ODQ不影响环磷酸腺苷的浓度。5. 因此，该组织中的一氧化氮能舒张似乎是通过SGC的激活介导的。
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