达非那新

• 常用名: 达非那新
• 英文名: Darifenacin
• CAS号: 133099-04-4
• 分子量: 426.550
• 密度: 1.2±0.1 g/cm3
• 沸点: 614.3±55.0 °C at 760 mmHg
• 分子式: C₂₈H₃₀N₂O₂
• 熔点: N/A
• 闪点: 325.3±31.5 °C

达非那新用途

Darifenacin(UK88525)是M3毒蕈碱型受体拮抗剂,pKi为8.9。

达非那新名称

• 中文名: 达非那新
• 英文名: darifenacin
• 中文别名: 2-[1-[2-(2,3-二氢苯并呋喃-5-基)乙基]-3-吡咯烷基]-2,2-二苯基乙酰胺

达非那新生物活性

• 描述: Darifenacin(UK88525)是M3毒蕈碱型受体拮抗剂,pKi为8.9。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR
  信号通路 >> 神经信号通路 >> mAChR
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Hegde SS, et al. Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol, 1997, 120(8), 1409-1418.

  [2]. Miller DW, et al. Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers. Neurourol Urodyn, 2011, 30(8), 1633-1638.

  [3]. Iijima K, et al. Effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. Eur Urol, 2007, 52(3), 842-847.

  [4]. Lu XZ, et al. Activation of M3 cholinoceptors attenuates vascular injury after ischaemia/reperfusion by inhibiting the Ca2+/calmodulin-dependent protein kinase II pathway. Br J Pharmacol. 2015 Dec;172(23):5619-33.

  [5]. Yu H, et al.Acetylcholine acts through M3 muscarinic receptor to activate the EGFR signaling and promotes gastric cancer cell proliferation. Sci Rep. 2017 Jan 19;7:40802.

达非那新物理化学性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 614.3±55.0 °C at 760 mmHg
• 分子式: C₂₈H₃₀N₂O₂
• 分子量: 426.550
• 闪点: 325.3±31.5 °C
• 精确质量: 426.230713
• PSA: 55.56000
• LogP: 4.50
• InChIKey: HXGBXQDTNZMWGS-RUZDIDTESA-N
• SMILES: NC(=O)C(c1ccccc1)(c1ccccc1)C1CCN(CCc2ccc3c(c2)CCO3)C1
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.624
• 储存条件: 2-8℃

达非那新靶点实验

查看更多实验

实验名称：Intravenous dose required to inhibit oxotremorine induced salivary secretion in ureth... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL884209

实验名称：Human M5 receptor (Acetylcholine receptors (muscarinic)) 来源：IUPHAR-DB 靶标：M5 receptor (Acetylcholine receptors (muscarinic)) [Homo sapiens] External Id：17_Human

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

实验名称：Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expre... 来源：ChEMBL 靶标：Muscarinic acetylcholine receptor M4 External Id：CHEMBL749860

实验名称：Volume of distribution at steady state in human after iv administration 来源：ChEMBL 靶标：N/A External Id：CHEMBL1614670

实验名称：Clearance in human after iv administration 来源：ChEMBL 靶标：N/A External Id：CHEMBL1614671

实验名称：Fraction unbound in human after iv administration 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL1614672

实验名称：Mean residence time in human after iv administration 来源：ChEMBL 靶标：N/A External Id：CHEMBL1614673

实验名称：Half life in human after iv administration 来源：ChEMBL 靶标：N/A External Id：CHEMBL1614674

实验名称：Fluorescence-based biochemical high throughput primary assay to identify inhibitors o... 来源：The Scripps Research Institute Molecular Screening Center 靶标：Trypanosoma brucei RNA editing ligase 1 External Id：TBREL1_INH_FRET_1536_1X%INH PRUN

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达非那新英文别名

• 2-(1-(2-(2,3-Dihydrobenzofuran-5-yl)ethyl)pyrrolidin-3-yl)-2,2-diphenylacetamide
• 2-{(3S)-1-[2-(2,3-Dihydro-1-benzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphenylacetamide
• (S)-1-(2-(2,3-Dihydro-5-benzofuranyl)ethyl)-α,α-diphenyl-3-pyrrolidineacetamide
• 2-{(3S)-1-[2-(2,3-Dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl}-2,2-diphenylacetamide
• Darifenacin
• (S)-1-(2-(2,3-Dihydro-5-benzofuranyl)ethyl)-a,a-diphenyl-3-pyrrolidineacetamide
• 2-((3S)-1-(2-(2,3-Dihydro-1-benzofuran-5-yl)ethyl)-3-pyrrolidinyl)-2,2-diphenylacetamide