|(R)-5-羟甲基托特罗定|CsnPharm

CAS No.: 207679-81-0

Desfesoterodine/(R)-5-羟甲基托特罗定 Catalog No. CSN12360

Synonyms: PNU-200577;5-Hydroxymethyl Tolterodine;5-HMT

(R)-5-Hydroxymethyl tolterodine is a potent and selective muscarinic receptor antagonist with a Kb and a pA2 of 0.84 nM and 9.14, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述(R)-5-Hydroxymethyl tolterodine is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo. mAChR in vitro: Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 = 14 nM) and 5-HM (IC50 = 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels^[3]. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased^[4].
参考文献

[1] Modiri AR, Alberts P, et al. Effect of muscarinic antagonists on micturition pressure measured by cystometry in normal, conscious rats. Urology. 2002 Jun;59(6):963-8.
[2] Nilvebrant L, Gillberg PG, et al. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72.
[3] Nilvebrant L. Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002;90(5):260-267
[4] Cappon GD, Bush B, Newgreen D, Finch GL, Alper RH. Tolterodine does not affect memory assessed by passive-avoidance response test in mice. Eur J Pharmacol. 2008;579(1-3):225-228

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9284 mL
- 14.6418 mL
- 29.2837 mL
- 5 mM
- 0.5857 mL
- 2.9284 mL
- 5.8567 mL
- 10 mM
- 0.2928 mL
- 1.4642 mL
- 2.9284 mL

技术信息

CAS号

207679-81-0

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H31NO2

运输

蓝冰

分子量

341.49

别名

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

溶解度

DMSO	460.0 mg/mL (1347.0 mM)
Water	insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Desfesoterodine/(R)-5-羟甲基托特罗定 Catalog No. CSN12360

靶点选择性

请登录您的专属账户

确认信息