NAS-181

• 常用名: NAS-181
• 英文名: NAS-181
• CAS号: 205242-62-2
• 分子量: 538.63200
• 密度: N/A
• 沸点: 765ºC at 760 mmHg
• 分子式: C₂₁H₃₄N₂O₁₀S₂
• 熔点: N/A
• 闪点: 416.5ºC

NAS-181用途

NAS-181是一种有效和选择性的大鼠5-羟色胺1B(r5-HT1B)拮抗剂,Ki值为47 nM。NAS-181增加了大鼠脑区5-HTP的积累[1]。

NAS-181名称

• 英文名: methanesulfonic acid,(2R)-2-[[3-(morpholin-4-ylmethyl)-2H-chromen-8-yl]oxymethyl]morpholine

NAS-181生物活性

• 描述: NAS-181是一种有效和选择性的大鼠5-羟色胺1B(r5-HT1B)拮抗剂,Ki值为47 nM。NAS-181增加了大鼠脑区5-HTP的积累[1]。
• 相关类别:
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
• 体外研究: NAS-181(化合物(R)-25)(0-1000 nM)增加了K+刺激的大鼠枕皮质切片[3H]-5-HT释放[1]。NAS-181(3 mg/kg；皮下注射)增加了大鼠的湿狗抖动次数,而用色氨酸羟化酶抑制剂对氯苯基丙氨酸(pCPA)(200 mg/kg；i.p.)预处理大鼠可消除这种影响[1]。
• 体内研究: NAS-181(20 mg/kg；皮下注射)增加大鼠脑区5-HTP的积累[1]。动物模型：大鼠[1]剂量：20mg/kg给药：S.c.结果：显著增加了5-HTP在下丘脑、海马、额叶的蓄积 大脑皮层、纹状体和这些区域的5-HIAA/5-HT比值甚至更高(40−60%).
• 参考文献:

  [1]. Berg S, et al. (R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist. J Med Chem. 1998 May 21;41(11):1934-42.

NAS-181物理化学性质

• 沸点: 765ºC at 760 mmHg
• 分子式: C₂₁H₃₄N₂O₁₀S₂
• 分子量: 538.63200
• 闪点: 416.5ºC
• 精确质量: 538.16500
• PSA: 177.69000
• LogP: 2.59810
• InChIKey: JDFGAOJLDPTWBF-UNTBIKODSA-N
• SMILES: C1=C(CN2CCOCC2)COc2c1cccc2OCC1CNCCO1.CS(=O)(=O)O
• 蒸汽压: 1.31E-24mmHg at 25°C

NAS-181靶点实验

查看更多实验

实验名称：Effect on the wet dog shake response(WDS) in rats after 9 determinations at a dose of... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL792471

实验名称：Effect on the wet dog shake response(WDS) in rats after 10 determinations at a dose o... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL792469

实验名称：Effect on 5-HTP turnover in hypothalamus of rat brain, expressed as percent of contro... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL803419

实验名称：Effect on 5-HIAA/5-HT turnover in Frontal cortex of rat brain, expressed as percent o... 来源：ChEMBL 靶标：N/A External Id：CHEMBL681459

实验名称：Effect on 5-HTP turnover in Frontal cortex of rat brain, expressed as percent of cont... 来源：ChEMBL 靶标：N/A External Id：CHEMBL681460

实验名称：Potentiation of K+ stimulated release of [3H]-5-HT from brain slices at a concentrati... 来源：ChEMBL 靶标：N/A External Id：CHEMBL651423

实验名称：Antagonism of the induced potentiation of K+ stimulated [3H]5-HT release from brain s... 来源：ChEMBL 靶标：N/A External Id：CHEMBL651424

实验名称：Antagonism of the induced potentiation of K+ stimulated [3H]5-HT release from brain s... 来源：ChEMBL 靶标：N/A External Id：CHEMBL651425

实验名称：Percent control of the stimulation ratio S2 (second stimulation)/S1(first stimulation... 来源：ChEMBL 靶标：N/A External Id：CHEMBL651426

实验名称：Percent control of the stimulation ratio S2 (second stimulation)/S1(first stimulation... 来源：ChEMBL 靶标：N/A External Id：CHEMBL651427

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NAS-181英文别名

• nas-181