Chen J J, Vasko M R, Wu X, Staeva T P, Baez M, Zgombick J M, Nelson D L
Neuroscience Research, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana, USA.
J Pharmacol Exp Ther. 1998 Dec;287(3):1119-27.
[3H]5-HT revealed the presence of serotonin receptors in cultured rat sensory neurons. [3H]5-CT binding was inhibited by cyanopindolol with an IC50 of 0.87 +/- 0.30 nM, suggesting the expression of the 5-HT1B receptor in these neurons. The presence of 5-HT1B receptors was confirmed by the displacement of [125I]Iodocyanopindolol binding by cyanopindolol with an IC50 of 2.43 +/- 0.81 nM. 5-HT1B receptors are the predominant type of serotonin receptors labeled by [3H]5-HT in cultured DRG neurons, representing approximately 60% of the specific [3H]5-HT binding sites. In addition, 5-HT1D and 5-HT2A receptor binding was also found in these neurons. RT-PCR analysis of RNA isolated from embryonic sensory neurons in culture confirmed the expression of 5-HT1B, 5-HT1D and 5-HT2A receptor mRNA. It also demonstrated the presence of 5-HT1F, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT5B receptor mRNA and the absence of 5-HT1A, 5-HT1E, 5-HT2B, 5-HT6 and 5-HT7 mRNA. The identification of multiple subtypes of serotonin receptors expressed in cultured embryonic sensory neurons suggests that DRG neuronal cultures may be an excellent model to examine the direct effects of serotonin on the activity of these sensory neurons.
[3H]5-羟色胺揭示了培养的大鼠感觉神经元中存在5-羟色胺受体。[3H]5-羧色胺结合被氰吲哚洛尔抑制，IC50为0.87±0.30 nM，表明这些神经元中存在5-HT1B受体。氰吲哚洛尔以2.43±0.81 nM的IC50取代[125I]碘氰吲哚洛尔结合，从而证实了5-HT1B受体的存在。5-HT1B受体是培养的背根神经节（DRG）神经元中被[3H]5-羟色胺标记的主要5-羟色胺受体类型，约占特异性[3H]5-羟色胺结合位点的60%。此外，在这些神经元中还发现了5-HT1D和5-HT2A受体结合。对培养的胚胎感觉神经元分离的RNA进行逆转录-聚合酶链反应（RT-PCR）分析，证实了5-HT1B、5-HT1D和5-HT2A受体mRNA的表达。该分析还表明存在5-HT1F、5-HT2C、5-HT3、5-HT4、5-HT5A和5-HT5B受体mRNA，而不存在5-HT1A、5-HT1E、5-HT2B、5-HT6和5-HT7 mRNA。在培养的胚胎感觉神经元中表达的多种5-羟色胺受体亚型的鉴定表明，DRG神经元培养物可能是研究5-羟色胺对这些感觉神经元活性直接影响的理想模型。
