DIPPA hydrochloride

• 常用名: DIPPA hydrochloride
• 英文名: DIPPA hydrochloride
• CAS号: 155512-52-0
• 分子量: 484.870
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₂H₂₄Cl₃N₃OS
• 熔点: N/A
• 闪点: N/A

DIPPA hydrochloride用途

DIPPA(盐酸盐)是一种不可逆、持久、选择性和高亲和力的κ-阿片受体拮抗剂。DIPPA(盐酸盐)可用于研究焦虑和抗抑郁药[1][2][3][4]。

DIPPA hydrochloride名称

• 英文名: 2-(3,4-Dichlorophenyl)-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]-N-methylacetamide hydrochloride (1:1)

DIPPA hydrochloride生物活性

• 描述: DIPPA(盐酸盐)是一种不可逆、持久、选择性和高亲和力的κ-阿片受体拮抗剂。DIPPA(盐酸盐)可用于研究焦虑和抗抑郁药[1][2][3][4]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体
  信号通路 >> 神经信号通路 >> 阿片受体
  研究领域 >> 神经疾病
• 靶点实验:

  κ-opioid receptor[1]

• 体内研究: DIPPA(2.5和5 mg/kg；s.c.)盐酸盐可降低Wistar Kyoto大鼠的进食潜伏期,但治疗并未改变SD大鼠的接近潜伏期[2]。与生理盐水处理的应变对照组相比,高剂量的DIPPA(1和5 mg/kg；s.c.)盐酸盐可增加SD大鼠的不动性[2]。与Wistar Kyoto大鼠的5 mg/kg组相比,SD大鼠的DIPPA(5 mg/kg)盐酸盐消耗量减少。盐酸双酚A显著缩短两种菌株的掩埋时间。与菌株内对照组相比,两种菌株中的盐酸二苯丙胺(5 mg/kg)减少了埋伏。DIPPA盐酸盐倾向于减少家中笼中SD大鼠的进食量,但显著增加新型笼中的进食量,其中DIPPA盐酸盐的潜在抗焦虑作用可能与化合物的低吞噬作用相反[2]。动物模型：Wistar Kyoto大鼠和SD大鼠(250–300 g)[2]剂量：2.5和5 mg/kg给药：皮下注射。结果：降低了Wistar Kyoto大鼠的进食潜伏期,但治疗并未改变SD大鼠的接近潜伏期。动物模型：Wistar Kyoto大鼠和SD大鼠(250–300 g)[2]剂量：1和5 mg/kg给药：皮下注射。结果：与生理盐水处理的品系对照组相比,高剂量增加了SD大鼠的不动性。
• 参考文献:

  [1]. Jones DC, et al. Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis. Biochem Pharmacol. 2010;80(10):1478-1486.

  [2]. Carr GV, et al. Comparison of the kappa-opioid receptor antagonist DIPPA in tests of anxiety-like behavior between Wistar Kyoto and Sprague Dawley rats. Psychopharmacology (Berl). 2010;210(2):295-302.

  [3]. Costello GF, et al. 2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists. J Med Chem. 1991;34(1):181-189.

  [4]. Chang AC, et al. kappa Opioid receptor selective affinity labels: electrophilic benzeneacetamides as kappa-selective opioid antagonists. J Med Chem. 1994;37(26):4490-4498.

DIPPA hydrochloride物理化学性质

• 分子式: C₂₂H₂₄Cl₃N₃OS
• 分子量: 484.870
• 精确质量: 483.070557
• InChIKey: BNWYENYHNOESCX-ZMBIFBSDSA-N
• SMILES: CN(C(=O)Cc1ccc(Cl)c(Cl)c1)C(CN1CCCC1)c1cccc(N=C=S)c1.Cl

DIPPA hydrochloride靶点实验

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实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify activators of... 来源：The Scripps Research Institute Molecular Screening Center 靶标：N/A External Id：FBW7_ACT_ALPHA_1536_1X%ACT PRUN

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify inhibitors of... 来源：The Scripps Research Institute Molecular Screening Center External Id：MITF_INH_Alpha_1536_1X%INH PRUN

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DIPPA hydrochloride英文别名

• Benzeneacetamide, 3,4-dichloro-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]-N-methyl-, hydrochloride (1:1)
• 2-(3,4-Dichlorophenyl)-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]-N-methylacetamide hydrochloride (1:1)
• 2-(3,4-Dichlorophenyl)-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(pyrrolidin-1-yl)ethyl]-N-methylacetamide hydrochloride (1:1)