Desfesoterodine (BioDeep_00000855670)

   


代谢物信息卡片


5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)

化学式: C22H31NO2 (341.2354666)
中文名称: (R)-5-羟甲基托特罗定
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: CC(C)N(CCC(C1=CC=CC=C1)C2=C(C=CC(=C2)CO)O)C(C)C
InChI: InChI=1S/C22H31NO2/c1-16(2)23(17(3)4)13-12-20(19-8-6-5-7-9-19)21-14-18(15-24)10-11-22(21)25/h5-11,14,16-17,20,24-25H,12-13,15H2,1-4H3/t20-/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
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively[1]. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053)[2][3]. Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats[4].

同义名列表

4 个代谢物同义名

5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM); Desfesoterodine; PNU-200577; 5-Hydroxymethyl Tolterodine



数据库引用编号

7 个数据库交叉引用编号

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文献列表

  • Young Seok Ji, In Sook Kim, Tae Kon Kim, Hye Hyun Yoo. Plasma concentration profile of tolterodine and 5-hydroxymethyl tolterodine following transdermal administration of tolterodine in rats. Die Pharmazie. 2018 07; 73(7):375-378. doi: 10.1691/ph.2018.8033. [PMID: 30001770]
  • Wenhua Liu, Lirong Teng, Kongtong Yu, Xiangshi Sun, Chunyu Fan, Chaoxing Long, Na Liu, Shuang Li, Bing Wu, Qingji Xu, Fengying Sun, Youxin Li. Design of hydrogels of 5-hydroxymethyl tolterodine and their studies on pharmacokinetics, pharmacodynamics and transdermal mechanism. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2017 Jan; 96(?):530-541. doi: 10.1016/j.ejps.2016.10.024. [PMID: 27789373]
  • Masayo Oishi, Yoshiro Tomono, Hidetomi Yamagami, Bimal Malhotra. Population pharmacokinetics of the 5-hydroxymethyl metabolite of tolterodine after administration of fesoterodine sustained release tablet in Western and East Asian populations. Journal of clinical pharmacology. 2014 Aug; 54(8):928-36. doi: 10.1002/jcph.274. [PMID: 24619889]
  • Jignesh M Parekh, Mallika Sanyal, Manish Yadav, Pranav S Shrivastav. Investigation of ex vivo stability of fesoterodine in human plasma and its simultaneous determination together with its active metabolite 5-HMT by LC-ESI-MS/MS: Application to a bioequivalence study. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2013 Jan; 913-914(?):1-11. doi: 10.1016/j.jchromb.2012.11.010. [PMID: 23266359]
  • Christian de Mey, Lyudmila Mateva, Zahariy Krastev, Richard Sachse, Nolan Wood, Bimal Malhotra. Effects of hepatic dysfunction on the single-dose pharmacokinetics of fesoterodine. Journal of clinical pharmacology. 2011 Mar; 51(3):397-405. doi: 10.1177/0091270010365547. [PMID: 20371737]
  • Bimal K Malhotra, Penelope H Crownover, Robert LaBadie, Paul Glue, Scott A MacDiarmid. The pharmacokinetic profile of fesoterodine 8 mg with daytime or nighttime dosing. European journal of clinical pharmacology. 2010 Feb; 66(2):171-6. doi: 10.1007/s00228-009-0748-y. [PMID: 19915829]
  • B Malhotra, Z Guan, N Wood, K Gandelman. Pharmacokinetic profile of fesoterodine. International journal of clinical pharmacology and therapeutics. 2008 Nov; 46(11):556-63. doi: 10.5414/cpp46556. [PMID: 19000553]
  • B Olsson, B M Landgren. The effect of tolterodine on the pharmacokinetics and pharmacodynamics of a combination oral contraceptive containing ethinyl estradiol and levonorgestrel. Clinical therapeutics. 2001 Nov; 23(11):1876-88. doi: 10.1016/s0149-2918(00)89083-9. [PMID: 11768839]
  • B Olsson, N Brynne, C Johansson, H Arnberg. Food increases the bioavailability of tolterodine but not effective exposure. Journal of clinical pharmacology. 2001 Mar; 41(3):298-304. doi: 10.1177/00912700122010113. [PMID: 11269570]
  • I Påhlman, P Gozzi. Serum protein binding of tolterodine and its major metabolites in humans and several animal species. Biopharmaceutics & drug disposition. 1999 Mar; 20(2):91-9. doi: 10.1002/(sici)1099-081x(199903)20:2<91::aid-bdd162>3.0.co;2-y. [PMID: 10206324]
  • L Nilvebrant, P G Gillberg, B Sparf. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacology & toxicology. 1997 Oct; 81(4):169-72. doi: 10.1111/j.1600-0773.1997.tb02064.x. [PMID: 9353847]
  • L Palmér, L Andersson, T Andersson, U Stenberg. Determination of tolterodine and the 5-hydroxymethyl metabolite in plasma, serum and urine using gas chromatography-mass spectrometry. Journal of pharmaceutical and biomedical analysis. 1997 Sep; 16(1):155-65. doi: 10.1016/s0731-7085(97)00023-x. [PMID: 9447563]