Darifenacin (BioDeep_00000614956)
代谢物信息卡片
化学式: C28H30N2O2 (426.2307)
中文名称: 达非那新
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5
InChI: InChI=1S/C28H30N2O2/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26/h1-12,19,25H,13-18,20H2,(H2,29,31)/t25-/m1/s1
描述信息
G - Genito urinary system and sex hormones > G04 - Urologicals > G04B - Urologicals > G04BD - Drugs for urinary frequency and incontinence
C78272 - Agent Affecting Nervous System > C66880 - Anticholinergic Agent > C29704 - Antimuscarinic Agent
D018377 - Neurotransmitter Agents > D018678 - Cholinergic Agents > D018680 - Cholinergic Antagonists
C78272 - Agent Affecting Nervous System > C29698 - Antispasmodic Agent
D000089162 - Genitourinary Agents > D064804 - Urological Agents
Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi) [1] Target: M3 receptor in vitro: Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat [1]. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 μM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6 [2]. in vivo: Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35\% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55\% [1]. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers [3].
同义名列表
数据库引用编号
8 个数据库交叉引用编号
- ChEBI: CHEBI:391960
- KEGGdrug: D03654
- PubChem: 444031
- Metlin: METLIN85389
- DrugBank: DB00496
- ChEMBL: CHEMBL1346
- CAS: 133099-04-4
- medchemexpress: HY-A0033
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
文献列表
- Xuelin Zhou, Wai Ping Lam, Hong Chai Tang, Chi-Man Koon, Ling Cheng, Clara Bik-San Lau, Willmann Liang, Ping-Chung Leung. Effects of Gegen (Puerariae lobatae Radix) water extract on improving detrusor overactivity in spontaneously hypertensive rats.
Phytomedicine : international journal of phytotherapy and phytopharmacology.
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Talanta.
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Neurourology and urodynamics.
2011 Nov; 30(8):1633-8. doi:
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British journal of clinical pharmacology.
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2008 Jul; 36(7):1385-405. doi:
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Naunyn-Schmiedeberg's archives of pharmacology.
2008 Jun; 377(4-6):449-62. doi:
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2008 May; 44(5):381-9. doi:
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2007 Jul; 20(3):307-14. doi:
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BJU international.
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2006 Apr; 15(3):251-60. doi:
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The American journal of medicine.
2006 Mar; 119(3 Suppl 1):29-36. doi:
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Methods and findings in experimental and clinical pharmacology.
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British journal of pharmacology.
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Drugs & aging.
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Paediatric drugs.
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Urology.
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10.1016/j.urology.2003.11.004. [PMID: 15013652] - Thomas Kerbusch, Ulrika Wählby, Peter A Milligan, Mats O Karlsson. Population pharmacokinetic modelling of darifenacin and its hydroxylated metabolite using pooled data, incorporating saturable first-pass metabolism, CYP2D6 genotype and formulation-dependent bioavailability.
British journal of clinical pharmacology.
2003 Dec; 56(6):639-52. doi:
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The Journal of pharmacology and experimental therapeutics.
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Xenobiotica; the fate of foreign compounds in biological systems.
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