Doherty P C, Wisler P A
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285.
Life Sci. 1994;54(7):507-14. doi: 10.1016/0024-3205(94)00410-2.
Quinelorane, a highly selective D2 dopamine agonist, was assessed for its ability to induce the penile erection/stretch-yawn syndrome. Quinelorane (0.1-100 micrograms/kg s.c.) or saline vehicle was administered to adult male Sprague-Dawley rats just prior to a 30 min. observation period. Significant dose-related increases in erections were observed in the drug treated animals at 3-100 micrograms/kg. Yawning was also increased at 3-100 micrograms/kg, with highest levels occurring at 10 micrograms/kg. Defecation was stimulated between 10 and 100 micrograms/kg. The stimulatory effects of 30 micrograms/kg of quinelorane on erection, yawning and defecation were blocked by haloperidol (0.1-0.3 mg/kg) but not by domperidone (0.1-1.0 mg/kg). No significant effects of quinelorane on seminal emission were observed. These findings indicate that in addition to its stimulatory effects on sexual activity, quinelorane also acts on D2 receptors in the central nervous system to stimulate erection in the penile erection/stretch-yawn model.
喹那洛烷是一种高选择性D2多巴胺激动剂，对其诱发阴茎勃起/伸懒腰-打哈欠综合征的能力进行了评估。在30分钟观察期开始前，给成年雄性斯普拉格-道利大鼠皮下注射喹那洛烷（0.1 - 100微克/千克）或生理盐水。在药物处理组动物中，3 - 100微克/千克剂量下观察到勃起显著呈剂量相关性增加。3 - 100微克/千克剂量下打哈欠也增加，最高水平出现在10微克/千克时。10 - 100微克/千克剂量可刺激排便。30微克/千克喹那洛烷对勃起、打哈欠和排便的刺激作用被氟哌啶醇（0.1 - 0.3毫克/千克）阻断，但未被多潘立酮（0.1 - 1.0毫克/千克）阻断。未观察到喹那洛烷对射精有显著影响。这些发现表明，除了对性活动有刺激作用外，喹那洛烷在阴茎勃起/伸懒腰-打哈欠模型中还作用于中枢神经系统的D2受体以刺激勃起。
