rac-Desethyl Oxybutynin (hydrochloride)
(Synonyms: (R,S)-DEOB) 目录号 : GC49203
An active metabolite of oxybutynin
Cas No.:81039-77-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
rac-Desethyl oxybutynin is an active metabolite of the muscarinic acetylcholine receptor (mAChR) antagonist oxybutynin .1,2,3 rac-Desethyl oxybutynin is formed from oxybutynin by the cytochrome P450 (CYP) isoform CYP3A4.2 It binds to mAChRs in isolated rat bladder, submaxillary gland, heart, and colon with Ki values of 5.38, 3.12, 16, and 5.59 nM, respectively. rac-Desethyl oxybutynin (0.4 and 0.8 mg/kg) reduces micturition pressure in rats.3
1.Lindeke, B., HallstrÖm, G., Johansson, C., et al.Metabolism of Oxybutynin: Establishment of desethyloxybutynin and oxybutynin N-oxide formation in rat liver preparation using deuterium substitution and gas chromatographic mass spectrometric analysisBiomed. Mass Spectrom.8(10)506-513(1981) 2.Oki, T., Kawashima, A., Uchida, M., et al.In vivo demonstration of muscarinic receptor binding activity of N-desethyl-oxybutynin, active metabolite of oxybutyninLife Sci.76(21)2445-2456(2005) 3.Mizushima, H., Kinoshita, K., Abe, K., et al.Pharmacokinetics/pharmacodynamics analysis of the relationship between the in vivo micturition pressure and receptor occupancy of (R)-oxybutynin and its metabolite in ratsBiol. Pharm. Bull.30(5)955-962(2007)
| Cas No. | 81039-77-2 | SDF | |
| 别名 | (R,S)-DEOB | ||
| Canonical SMILES | O=C(C(C1CCCCC1)(C2=CC=CC=C2)O)OCC#CCNCC.Cl | ||
| 分子式 | C20H27NO3·HCl | 分子量 | 365.9 |
| 溶解度 | Chloroform: slightly soluble,Methanol: slightly soluble | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.733 mL | 13.6649 mL | 27.3299 mL |
| 5 mM | 0.5466 mL | 2.733 mL | 5.466 mL |
| 10 mM | 0.2733 mL | 1.3665 mL | 2.733 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Factorial design-assisted spectroscopic determination of oxybutynin hydrochloride
R Soc Open Sci 2021 Nov 24;8(11):211027.PMID:34849244DOI:10.1098/rsos.211027.
In this study, we have developed two facile spectroscopic methods for quantifying oxybutynin (OBT) hydrochloride in its pure form and tablets using design of experiments (DOEs). The spectroscopic methods depended on the ion-pair complex formation between the tertiary amino group in the drug and eosin in 0.2 M acetate buffer of pH 4. Method I involves spectrophotometric measurement of the absorbance of the developed complex at 550 nm and showed linearity through 1.0-10.0 µg ml-1. Method II involves spectrofluorometric measurement of the quenching influence of OBT on the native fluorescence of eosin (λ excitation/λ emission of 304/548 nm) and showed linearity through 1.0-6.0 µg ml-1. Critical parameters were identified through preliminary trials and optimized using the DOE. Additionally, the quenching mechanism was investigated and the pathway of the reaction was postulated. The fluorescence quenching constant and thermodynamic parameters were explored using the Stern-Volmer plot and Van't Hoff graph, respectively. Assessments conducted via analytical ecoscale revealed the 'excellent-greenness' of the methodology. The two methods have the potentials of being green and fast compared with other reported methods.
Current treatment options for craniofacial hyperhidrosis
J Vasc Bras 2020 Nov 16;19:e20190152.PMID:34211510DOI:10.1590/1677-5449.200152.
Hyperhidrosis (HH) is characterized by sweating exceeding the amount necessary to meet the thermal regulation and physiological needs of the body. Approximately 9.41% of individuals with HH have craniofacial hyperhidrosis (FH). The present study aims to review the most current data in the literature regarding craniofacial hyperhidrosis, including pathophysiology, diagnosis and clinical presentation, treatment options (clinical and surgical), and outcomes. VATS (videothoracoscopy sympathectomy) is considered the gold standard for definitive treatment of axillary or palmar hyperhidrosis. Recently, several studies have shown the usefulness of clinical treatment with oxybutynin hydrochloride, leading to clinical improvement of HH in more than 70% of users. Both clinical and surgical treatment of craniofacial hyperhidrosis have good results. However, surgical treatment of FH is associated with more complications. Clinical treatment with oxybutynin hydrochloride yields good results and can be the first therapeutic option. When the patient is not satisfied with this treatment and has good clinical conditions, surgical treatment can be used safely.
Adjustment of Conditions for Combining Oxybutynin Transdermal Patch with Heparinoid Cream in Mice by Analyzing Blood Concentrations of Oxybutynin hydrochloride
Biol Pharm Bull 2019 Apr 1;42(4):586-593.PMID:30686806DOI:10.1248/bpb.b18-00690.
The combination of skin external preparation and transdermal patch is influenced by drug absorption through the skin. We investigated the effect of heparinoid cream on the transdermal absorption of oxybutynin hydrochloride using an oxybutynin transdermal patch and determined the combined effect of these medications. Normal skin and dry dorsal skin in hairless mice were treated with heparinoid cream, followed by the application of the oxybutynin transdermal patch. A blood sample was collected from the mouse tail vein and the blood concentration of oxybutynin hydrochloride was analyzed by LC-MS/MS. Transepidermal water loss, the hydration level of the stratum corneum, and the stratum corneum thickness in the dorsal skin were measured. The blood concentration and area under the curve (AUC)0→24 of oxybutynin hydrochloride increased when the 4.0-cm2 oxybutynin transdermal patch was applied 1 h after the application of the moisturizer, compared to the values without moisturizer. Normal skin and dry skin did not affect this result. As the hydration level of the stratum corneum and stratum corneum thickness increased before patch application by pre-treatment with moisturizer, it was suggested that transdermal absorption of oxybutynin hydrochloride was increased by skin hydration. The increased blood concentration of oxybutynin hydrochloride was regulated by changing the effective area of the patch and applying additional moisturizer at intervals. The pharmacokinetics of oxybutynin hydrochloride under the regulation of combination treatment was similar to that of treatment without moisturizer. These findings indicate that the application conditions of the oxybutynin transdermal patch and heparinoid cream influence the proper use of the patch.
Injectable, Adhesive, and Self-Healing Composite Hydrogels Loaded With Oxybutynin hydrochloride for the Treatment of Overactive Bladder in Rats
Front Bioeng Biotechnol 2022 Jun 27;10:906835.PMID:35832402DOI:10.3389/fbioe.2022.906835.
Object: The aim of this study was to prepare injectable, adhesive, and self-healing composite hydrogels loaded with oxybutynin hydrochloride and verify its function in the treatment of overactive bladder. Method: The ultraviolet (UV) absorption of oxybutynin (Oxy) in the solution was detected using a UV spectrophotometer at 233 nm, and the cumulative drug release was calculated using Origin software. L929 mouse fibroblasts were used to test cell adhesion to OCP50 and OCP100 hydrogels. Both FT-IR and NMR overactive bladder demonstrated that Dex was oxidized to PDA with aldehyde groups. Urodynamic examinations were performed 24 h after intraperitoneal injection in the rat model. The relative expression levels of Orai1 and STIM1 were detected by western blot (WB) and QPCR. Results: After loading Oxy, the shear adhesion under the wet conditions of OCP50 and OCP100 was higher than CP50 and CP100 (p < 0.05), and both were suitable for intravaginal administration. After 72 h of release, oxybutynin released 82.8% in OCP100 hydrogel and 70% in OCP50. Compared to the model, OCP50, CP100, and OCP100 relieved the overactive bladder and inhibited the expression of Orail and STIM1. Conclusions: Oxybutynin hydrogel could provide relief to overactive bladder by decreasing the expression of Orail and STIM1 in rats.
Does oxybutynin hydrochloride cause arrhythmia in children with bladder dysfunction?
Med Arch 2013;67(3):202-4.PMID:23848044DOI:10.5455/medarh.2013.67.202-204.
Aim: Pediatric surgeons frequently encounter children presenting with voiding dysfunction symptoms, including urgency, frequency, and incontinence. Antimuscarinic agents Oxybutynin) are the main drugs used to treat patients with overactive bladder (OAB) syndrome, defined as urgency, with or without urgency incontinence, usually with increased daytime frequency and nocturia. Increased QT dispersion is known to be the cause of ventricular arrhythmia in various systemic diseases and leads to increased mortality and morbidity. Method: This study represents a subset of a complete data set, considering only those children aged admitted to the Pediatric Surgery and Pediatric Nephrology Clinics during the period January 2011 to July 2012. Result: In this study, we have determined that the QT interval changes significantly depending on the use of oxybutynin. The QT changes increased cardiac arrhythmia in children. Conclusion: For this reason, children using such drugs should be closely monitored for cardiac arrhythmia.