Niles L P, Brown G M, Mishra R K
Neuropharmacology. 1983 Nov;22(11):1311-4. doi: 10.1016/0028-3908(83)90205-8.
Evidence that the putative pineal hormone, N-acetylserotonin (NAS), is present in diverse areas of the brain of the rat and that this compound is biologically active, prompted a study of its central binding characteristics. [3H]N-acetylserotonin [( 3H]-NAS) exhibits specific, saturable and high affinity binding in synaptosomal fractions from the brain of the rat. In fresh CNS membranes, [3H]N-acetylserotonin appeared to bind to a single population of high affinity sites with a dissociation constant (Kd) of 3-5 nM and a maximal binding site concentration (Bmax) of 250-400 fmol mg-1 protein. A comparison of the regional distribution of the binding of [3H]N-acetylserotonin and [3H]-5-hydroxytryptamine [( 3H]-5-HT) indicated that both radioligands exhibited the greatest binding in the striatum and frontal cortex, while relatively more [3H]N-acetylserotonin was bound in the cerebellum and brainstem. The structural specificity of the binding suggests that [3H]N-acetylserotonin labelled serotonergic receptors in the frontal cortex.
有证据表明，假定的松果体激素N - 乙酰血清素（NAS）存在于大鼠大脑的不同区域，且该化合物具有生物活性，这促使人们对其中枢结合特性进行研究。[3H]N - 乙酰血清素（[3H]-NAS）在大鼠大脑突触体组分中表现出特异性、可饱和且高亲和力的结合。在新鲜的中枢神经系统膜中，[3H]N - 乙酰血清素似乎与单一群体的高亲和力位点结合，解离常数（Kd）为3 - 5 nM，最大结合位点浓度（Bmax）为250 - 400 fmol mg-1蛋白质。对[3H]N - 乙酰血清素和[3H]-5 - 羟色胺（[3H]-5 - HT）结合的区域分布比较表明，两种放射性配体在纹状体和额叶皮质中表现出最大结合，而在小脑中结合的[3H]N - 乙酰血清素相对较多，在脑干中也是如此。结合的结构特异性表明，[3H]N - 乙酰血清素在额叶皮质中标记了5 - 羟色胺能受体。
