Department of Pharmacology, Tulane University School of Medicine, New Orleans, LA 70112, USA.
Am J Physiol Heart Circ Physiol. 2013 Jun 15;304(12):H1670-9. doi: 10.1152/ajpheart.00062.2013. Epub 2013 Apr 12.
Nitric oxide (NO) is the principal mediator of penile erection, and soluble guanylate cyclase (sGC) is the receptor for NO. In pathophysiological conditions when sGC is inactivated and not responsive to NO or sGC stimulators a new class of agents called sGC activators increase the activity of NO-insensitive sGC and produce erection. The aim of this study was to investigate erectile responses to BAY 60-2770, a sGC activator, under physiological and pathophysiological conditions. In the present study increases in intracavernosal pressure (ICP) in response to intracavernosal (ic) injections of BAY 60-2770 were investigated under baseline conditions, when sGC was inhibited by 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), when nitric oxide synthase (NOS) was inhibited by N-nitro-L-arginine methyl ester (L-NAME), and after cavernosal nerve crush injury. Under baseline conditions ic injections of BAY 60-2770 increase ICP, ICP/mean arterial pressure (MAP), and area under the ICP curve (AUC) and produce small decreases in MAP at the highest doses studied. BAY 60-2770 was very potent in its ability to induce erection and responses to BAY 60-2770 were enhanced by ODQ which attenuates erectile responses to sodium nitroprusside (SNP), diethylamine NONOate (DEA/NO), and cavernosal nerve stimulation. Responses to BAY 60-2770 were not altered by L-NAME or cavernosal nerve crush injury. These data indicate that BAY 60-2770 has potent erectile activity that is enhanced by ODQ and show that responses to BAY 60-2770 are not attenuated by NOS inhibition or cavernosal nerve injury. These results suggest that BAY 60-2770 would be effective in the treatment of erectile dysfunction when NO bioavailability is reduced, after pelvic nerve injury, and when sGC is oxidized.
一氧化氮(NO)是阴茎勃起的主要介质,而可溶性鸟苷酸环化酶(sGC)是其受体。在病理生理条件下,当 sGC 失活且对 NO 或 sGC 激动剂无反应时,一类新的药物被称为 sGC 激活剂,可增加对 NO 不敏感的 sGC 的活性并产生勃起。本研究旨在研究生理和病理生理条件下,sGC 激活剂 BAY 60-2770 对勃起的反应。在本研究中,在以下情况下研究了 BAY 60-2770 对海绵体内(ic)注射的反应:在基础条件下,当 sGC 被 1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮(ODQ)抑制时,当一氧化氮合酶(NOS)被 N-硝基-L-精氨酸甲酯(L-NAME)抑制时,以及在海绵体神经损伤后。在基础条件下,ic 注射 BAY 60-2770 可增加 ICP、ICP/平均动脉压(MAP)和 ICP 曲线下面积(AUC),并在最高剂量研究中 MAP 略有降低。BAY 60-2770 诱导勃起的能力非常强,ODQ 增强了对 BAY 60-2770 的反应,而 ODQ 减弱了对硝普钠(SNP)、二乙胺 NONOate(DEA/NO)和海绵体神经刺激的勃起反应。L-NAME 或海绵体神经损伤对 BAY 60-2770 的反应没有改变。这些数据表明,BAY 60-2770 具有强大的勃起活性,ODQ 可增强其活性,并表明 BAY 60-2770 的反应不受 NOS 抑制或海绵体神经损伤的影响。这些结果表明,当 NO 生物利用度降低、骨盆神经损伤后以及 sGC 被氧化时,BAY 60-2770 将有效治疗勃起功能障碍。