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Oxybutynin

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Chemical Structure| 5633-20-5 同义名 : -
CAS号 : 5633-20-5
货号 : A144038
分子式 : C22H31NO3
纯度 : 98%
分子量 : 357.486
MDL号 : MFCD00865252
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(293.72 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(139.87 mM)

动物实验配方:
生物活性
靶点
  • AChR

描述 Oxybutynin (OXY) is a competitive acetylcholine antagonist that relaxes the bladder smooth muscle. In patients with involuntary detrusor contractions, OXY increases bladder capacity and volume to first detrusor contraction, thus decreasing urinary urgency and frequency of urination[3]. Moreover, Oxybutynin inhibited vascular Kv channels in a concentration-dependent manner, with an IC50 value of 11.51 ± 0.38 μM and a Hill coefficient (n) of 2.25 ± 0.12[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02809274 - Unknown August 2018 Israel ... 展开 >> Emek Medical center Not yet recruiting Afula, Israel Contact: Evgeni Chubar, Dr          Soroka medical center Not yet recruiting Beer Sheva, Israel Contact: Anna Gurevich          Hillel Yaffe Medical Center Not yet recruiting Hadera, Israel Contact: Lea Arbov          Bnei Zion medical center Not yet recruiting Haifa, Israel Contact: Yelena Mischenko, Dr          Rambam Medical center Not yet recruiting Haifa, Israel Contact: Noa Lavi          Meir Medical center Not yet recruiting Kfar Saba, Israel Contact: Martin Ellis, Prof          Principal Investigator: Martin Ellis          Sheba medical center Not yet recruiting Ramat Gan, Israel Contact: Adrian Duek          Kaplan medical center Not yet recruiting Rehovot, Israel Contact: Anfisa Santevsky, Dr          Maccabi Not yet recruiting Tel Aviv, Israel Contact: Sigal Tavor, Dr          Sub-Investigator: Shirly Shapira, Dr          Tel Aviv Sourasky Not yet recruiting Tel Aviv, Israel Contact: Irit Avivi, Prof          Ziv Medical center Not yet recruiting Zefat, Israel Contact: Nagib Dali          Assaf Harofeh Medical Center Not yet recruiting Zerifin, Israel Contact: Odit Gotvin, Dr 收起 <<
NCT02386072 - Completed - -
NCT00547378 Urinary Incontinence, Urgency-... 展开 >>frequency Overactive Bladder 收起 << Phase 4 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.80mL

0.56mL

0.28mL

13.99mL

2.80mL

1.40mL

27.97mL

5.59mL

2.80mL

参考文献

[1]Lukkari E, Taavitsainen P, et al. Cytochrome P450 specificity of metabolism and interactions of oxybutynin in human liver microsomes. Pharmacol Toxicol. 1998 Apr;82(4):161-6.

[2]Tonini M, Rizzi CA, et al. Depressant action of oxybutynin on the contractility of intestinal and urinary tract smooth muscle. J Pharm Pharmacol. 1987 Feb;39(2):103-7.

[3]Davila GW. Transdermal oxybutynin in the treatment of overactive bladder. Clin Interv Aging. 2006;1(2):99-105. doi: 10.2147/ciia.2006.1.2.99. PMID: 18044106; PMCID: PMC2695169.

[4]Li H, Seo MS, An JR, Jung HS, Ha KS, Han ET, Hong SH, Bae YM, Ryu DR, Park WS. The anticholinergic drug oxybutynin inhibits voltage-dependent K+ channels in coronary arterial smooth muscle cells. Clin Exp Pharmacol Physiol. 2019 Nov;46(11):1030-1036. doi: 10.1111/1440-1681.13138. Epub 2019 Aug 9. PMID: 31330060.