褪黑素对叙利亚仓鼠下丘脑腺苷酸环化酶活性的皮摩尔亲和力结合与抑制作用。
Picomolar-affinity binding and inhibition of adenylate cyclase activity by melatonin in Syrian hamster hypothalamus.
作者信息
Niles L P, Hashemi F
机构信息
McMaster University, Department of Biomedical Sciences, Hamilton, Ontario.
出版信息
Cell Mol Neurobiol. 1990 Dec;10(4):553-8. doi: 10.1007/BF00712848.
Abstract
- The effect of melatonin on forskolin-stimulated adenylate cyclase activity was measured in homogenates of Syrian hamster hypothalamus. In addition, the saturation binding characteristics of the melatonin receptor ligand, [125I]iodomelatonin, was examined using an incubation temperature (30 degrees C) similar to that used in enzyme assays. 2. At concentrations ranging from 10 pM to 1 nM, melatonin caused a significant decrease in stimulated adenylate cyclase activity with a maximum inhibition of approximately 22%. 3. Binding experiments utilizing [125I]iodomelatonin in a range of approximately 5-80 pM indicated a single class of high-affinity sites: Kd = 55 +/- 9 pM, Bmax = 1.1 +/- 0.3 fmol/mg protein. 4. The ability of picomolar concentrations of melatonin to inhibit forskolin-stimulated adenylate cyclase activity suggests that this affect is mediated by picomolar-affinity receptor binding sites for this hormone in the hypothalamus.
摘要
- 在叙利亚仓鼠下丘脑匀浆中测定了褪黑素对福司可林刺激的腺苷酸环化酶活性的影响。此外，使用与酶测定中所用温度（30摄氏度）相似的孵育温度，检测了褪黑素受体配体[125I]碘褪黑素的饱和结合特性。2. 在10皮摩尔至1纳摩尔的浓度范围内，褪黑素导致刺激的腺苷酸环化酶活性显著降低，最大抑制率约为22%。3. 利用[125I]碘褪黑素在约5 - 80皮摩尔范围内进行的结合实验表明存在一类单一的高亲和力位点：解离常数（Kd）= 55±9皮摩尔，最大结合容量（Bmax）= 1.1±0.3飞摩尔/毫克蛋白质。4. 皮摩尔浓度的褪黑素抑制福司可林刺激的腺苷酸环化酶活性的能力表明，这种作用是由下丘脑中该激素的皮摩尔亲和力受体结合位点介导的。
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Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
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Melatonin increases cGMP and decreases cAMP levels in rat medial basal hypothalamus in vitro.褪黑素在体外可增加大鼠内侧基底下丘脑的环磷酸鸟苷（cGMP）水平，并降低环磷酸腺苷（cAMP）水平。
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HPLC-purified 2-[125I]iodomelatonin labels multiple binding sites in hamster brain.经高效液相色谱（HPLC）纯化的2-[¹²⁵I]碘褪黑素标记仓鼠脑中的多个结合位点。
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