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编 号：F163546
分子式：C95H146N22O24
分子量：1980.31
分子式：C95H146N22O24
分子量：1980.31
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CAS No: 143896-17-7
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生物活性：
M40 is an antagonist or a weak agonist for galanin receptor depending on different subtypes of galanin receptors in the brain, hypothalamus, hippocampus, amygdala and pancreas.
体内研究：
M40 (0.1-1 nmol，脑室内注射，单剂量) 根据对甘丙肽受体 N 端的识别，选择性地阻断 Sprague-Dawley 大鼠模型中甘丙肽-(1-15) 诱导的中枢心血管反应 。M40 (2-8 nmol，脑室或海马体内注射，单剂量) 在 SD 大鼠模型中表现出对甘丙肽诱导的记忆缺陷的拮抗作用，具有减轻与阿尔茨海默病相关的认知缺陷的潜力。Animal Model:Vasopressor and tachycardia induced by galanin in Sprague-Dawley rats
Dosage:0.1-1 nmol
Administration:Intracisternal injection, single dose
Result:Blocked the feeding effects of galanin in the hypothalamus and amygdala.Reduced vasopressor response and heart rate induced by galanin-(1-15), but not those effects induced by galanin-(1-29).
Animal Model:Memory impairment induced by galanin in rats model
Dosage:2-8 nmol
Administration:intraventricular or intrahippocampal, single dose
Result:Blocked the impairment in choice accuracy.
体外研究：
M40 (1 μM) displaces [mono[125IJodo-Tyr26]galanin from binding sites in the hippocampus, hypothalamus, and spinal cord. M40 has a lower affinity than galanin for all membranes. The IC50 values are 6 nM in the hippocampus, 15 nM in the hypothalamus, 12 nM in the spinal cord, and 3 nM in the insulinoma cells. M40 (1 μM) completely blocks 125I-labeled galanin-binding sites.
M40 is an antagonist or a weak agonist for galanin receptor depending on different subtypes of galanin receptors in the brain, hypothalamus, hippocampus, amygdala and pancreas.
体内研究：
M40 (0.1-1 nmol，脑室内注射，单剂量) 根据对甘丙肽受体 N 端的识别，选择性地阻断 Sprague-Dawley 大鼠模型中甘丙肽-(1-15) 诱导的中枢心血管反应 。M40 (2-8 nmol，脑室或海马体内注射，单剂量) 在 SD 大鼠模型中表现出对甘丙肽诱导的记忆缺陷的拮抗作用，具有减轻与阿尔茨海默病相关的认知缺陷的潜力。Animal Model:Vasopressor and tachycardia induced by galanin in Sprague-Dawley rats
Dosage:0.1-1 nmol
Administration:Intracisternal injection, single dose
Result:Blocked the feeding effects of galanin in the hypothalamus and amygdala.Reduced vasopressor response and heart rate induced by galanin-(1-15), but not those effects induced by galanin-(1-29).
Animal Model:Memory impairment induced by galanin in rats model
Dosage:2-8 nmol
Administration:intraventricular or intrahippocampal, single dose
Result:Blocked the impairment in choice accuracy.
体外研究：
M40 (1 μM) displaces [mono[125IJodo-Tyr26]galanin from binding sites in the hippocampus, hypothalamus, and spinal cord. M40 has a lower affinity than galanin for all membranes. The IC50 values are 6 nM in the hippocampus, 15 nM in the hypothalamus, 12 nM in the spinal cord, and 3 nM in the insulinoma cells. M40 (1 μM) completely blocks 125I-labeled galanin-binding sites.
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