Desfesoterodine|207679-81-0|((R)-5-羟甲基托特罗定; PNU-200577; 5-Hydroxymethyl Tolterodine)-陌孚医药/Medlife

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Desfesoterodine (Synonyms: (R)-5-羟甲基托特罗定; PNU-200577; 5-Hydroxymethyl Tolterodine)

目录号: PL06858 纯度: ≥98%

CAS No. :207679-81-0

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中文名称	Desfesoterodine
中文别名	(R)-5-羟甲基托特罗定;(R)5 - 羟基甲基托特罗定标准品;1,1’-[(4-甲基苯基)亚氨基]二-2-丙醇;3-[(1R)-3-[双(1-甲基乙基)氨基]-1-苯基丙基]-4-羟基苯甲醇
英文名称	Desfesoterodine
英文别名	(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol;3-[(1R)-3-[Bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxybenzenemethanol;5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM);(R)-5-HYDROXYMETHYL TOLTERODINE;3-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxy-Benzenemethanol;5-hydroxymethyl Tolterodine;R-(+)-2(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenol;Desfesoterodine;PNU 200577;PNU-200577
Cas No.	207679-81-0
分子式	C₂₂H₃₁NO₂
分子量	341.49
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	Desfesoterodine (PNU-200577) 是一种有效的，选择性毒蕈碱受体 (mAChR) 拮抗剂，K_B 和 pA₂ 分别为 0.84 nM 和 9.14。Desfesoterodine 是 Tolterodine (PNU-200583; HY-A0024) 和 Fesoterodine (HY-70053) 的主要药理活性代谢产物。Desfesoterodine 改善大鼠脑梗死诱导膀胱过度活动。
生物活性	Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a K B and a pA 2 of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.
性状	Solid
IC50 & Target[1][2]	Kb: 0.84 nM (mAChR).
体外研究(In Vitro)	In vitro, Desfesoterodine preventes carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In radioligand binding studies carries out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, Desfesoterodine is not selective for any muscarinic receptor subtype. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Desfesoterodine (PNU-200577; 5-Hydroxymethyl Tolterodine; 0.1 and 1 mg/kg; IV) significantly increases bladder compliance after moderate and high doses. In vivo, Desfesoterodine is significantly more potent at suppressing acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50=15 and 40 nmol/kg, respectively) . has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Nilvebrant L, Gillberg PG, Sparf B. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72. [2]. Fullhase, Claudius; Soler, Roberto; Gratzke, Christian et al. Spinal effects of the fesoterodine metabolite 5-hydroxymethyl tolterodine and/or doxazosin in rats with or without partial urethral obstruction. Journal of Urology (New York, NY, United States)

溶解度数据	In Vitro: H₂O : 100 mg/mL (292.83 mM; Need ultrasonic)DMSO : 50 mg/mL (146.42 mM; Need ultrasonic)配制储备液

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