...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >Activation of dopamine D-4 receptors by ABT-724 induces penile erection in rats
【24h】

Activation of dopamine D-4 receptors by ABT-724 induces penile erection in rats

机译：ABT-724激活多巴胺D-4受体可诱导大鼠阴茎勃起

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Apomorphine, a nonselective dopamine receptor agonist, facilitates penile erection and is effective in patients suffering from erectile dysfunction. The specific dopamine receptor subtype(s) responsible for its erectogenic effect is not known. Here we report that the dopamine D-4 receptor plays a role in the regulation of penile function. ABT-724 is a selective dopamine D4 receptor agonist that activates human dopamine D-4 receptors with an EC50 of 12.4 nM and 61% efficacy, with no effect on dopamine D-1, D-2, D-3, or D-5 receptors. ABT-724 dose-dependently facilitates penile erection when given s.c. to conscious rats, an effect that is blocked by haloperidol and clozapine but not by domperidone. A proerectile effect is observed after intracerebroventricular but not intrathecal administration, suggesting a supraspinal site of action. s.c. injections of ABT-724 increase intracavernosal pressure in awake freely moving rats. In the presence of sildenafil, a potentiation of the proerectile effect of ABT-724 is observed in conscious rats. The ability of ABT-724 to facilitate penile erection together with the favorable side-effect profile indicates that ABT-724 could be useful for the treatment of erectile dysfunction.
机译：阿扑吗啡是一种非选择性的多巴胺受体激动剂，有助于阴茎勃起，对勃起功能障碍的患者有效。负责其勃起作用的特定多巴胺受体亚型是未知的。在这里我们报告说多巴胺D-4受体在调节阴茎功能中起作用。 ABT-724是一种选择性多巴胺D4受体激动剂，可激活人多巴胺D-4受体，EC50为12.4 nM，功效为61％，对多巴胺D-1，D-2，D-3或D-5无影响受体。皮下注射时，ABT-724剂量依赖性地促进阴茎勃起。对有意识的大鼠，这种作用被氟哌啶醇和氯氮平所阻断，但未被多潘立酮所阻断。在脑室内给药后观察到有前列腺肥大作用，但鞘内注射未观察到，表明有脊髓上作用部位。南卡罗来纳州注射ABT-724可增加清醒自由运动大鼠的海绵体内压力。在西地那非的存在下，在有意识的大鼠中观察到ABT-724的生殖作用增强。 ABT-724促进阴茎勃起的能力以及良好的副作用，表明ABT-724可用于治疗勃起功能障碍。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号