Department of Pharmacodynamics, Medical University of Łódź, Muszyńskiego 1, PL 90-151 Łódź, Poland.
Pharmacol Rep. 2011;63(3):717-23. doi: 10.1016/s1734-1140(11)70583-7.
The effects of orexins, which are also named hypocretins, on cAMP formation were examined in primary cultures of rat astrocytes. Orexin A, an agonist of OX₁ and OX₂ receptors, stimulated cAMP production with an EC₅₀ value of 0.68 μM and potentiated the forskolin-induced increase in the nucleotide synthesis. [Ala¹¹-D-Leu¹⁵]orexin B, an agonist of OX₂ receptors, was inactive. The effects of orexin A were antagonized by SB 408124, a selective blocker of OX₁ receptors, but were not affected by TCS OX2 29, a selective antagonist of OX₃ receptors. We hypothesized that the activation of OX₁ receptors stimulated cAMP synthesis in primary rat astrocyte cultures.
我们在原代培养的大鼠星形胶质细胞中研究了食欲素（也称为下丘脑泌素）对 cAMP 形成的影响。食欲素 A 是 OX1 和 OX2 受体的激动剂，以 EC50 值为 0.68 μM 刺激 cAMP 产生，并增强了 forskolin诱导的核苷酸合成增加。[Ala¹¹-D-Leu¹⁵]orexin B 是 OX2 受体的激动剂，没有活性。SB 408124（OX1 受体的选择性阻断剂）拮抗食欲素 A 的作用，但 TCS OX2 29（OX3 受体的选择性拮抗剂）对其作用没有影响。我们假设 OX1 受体的激活刺激了原代大鼠星形胶质细胞培养物中的 cAMP 合成。
