Carbamazepine 10,11-epoxide
(Synonyms: 卡马西平10,11-环氧化物) 目录号 : GC49111
An active metabolite of carbamazepine
Cas No.:36507-30-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine.1,2 It is formed from carbamazepine by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes prepared from HepG2 cells expressing CYP3A4 or CYP2C8, respectively.1 Carbamazepine 10,11-epoxide has anticonvulsant activity against maximal electroshock-induced seizures in mice.2 It has been found in wastewater effluent.3
1.Kerr, B.M., Thummel, K.E., Wurden, C.J., et al.Human liver carbamazepine metabolism. Role of CYP3A4 and CYP2C8 in 10,11-epoxide formationBiochem. Pharmacol.47(11)1969-1979(1994) 2.Bourgeois, B.F., and Wad, N.Individual and combined antiepileptic and neurotoxic activity of carbamazepine and carbamazepine-10,11-epoxide in miceJ. Pharmacol. Exp. Ther.231(2)411-415(1984) 3.Miao, X.-S., Yang, J.-J., and Metcalfe, C.D.Carbamazepine and its metabolites in wastewater and in biosolids in a municipal wastewater treatment plantEnviron. Sci. Technol.39(19)7469-7475(2005)
| Cas No. | 36507-30-9 | SDF | |
| 别名 | 卡马西平10,11-环氧化物 | ||
| Canonical SMILES | O=C(N1C2=C(C3OC3C4=C1C=CC=C4)C=CC=C2)N | ||
| 分子式 | C15H12N2O2 | 分子量 | 252.3 |
| 溶解度 | DMF: 5 mg/ml,DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml,DMSO: 1 mg/ml | 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 | 3.9635 mL | 19.8177 mL | 39.6354 mL |
| 5 mM | 0.7927 mL | 3.9635 mL | 7.9271 mL |
| 10 mM | 0.3964 mL | 1.9818 mL | 3.9635 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。
Carbamazepine 10,11-epoxide in children
Br J Clin Pharmacol 1984 Dec;18(6):935-9.PMID:6529533DOI:10.1111/j.1365-2125.1984.tb02566.x.
Concentrations of carbamazepine (CBZ) and its 10,11-epoxide metabolite (CBZ-E) were measured in simultaneously collected plasma and mixed saliva samples from 15 children (aged 1-13 years). Saliva concentrations of CBZ and CBZ-E were measured in hourly samples taken from six of these children during dose intervals whilst on different dose or dose-frequency regimens. Saliva and plasma CBZ (r = 0.91; P less than 0.001) and CBZ-E (r = 0.91; P less than 0.001) concentrations were significantly correlated. The mean +/- s.d. steady state CBZ-E/CBZ concentration ratio in the six children was 0.40 +/- 0.21 and was similar at all times within the 12 h dose interval. The mean +/- s.d. percentage fluctuation of the combined CBZ + CBZ-E (103.0 +/-28.9) was significantly less than that of CBZ-E (145.5 +/- 52.8) but not CBZ (109.6 +/- 31.1). If CBZ and CBZ-E have equipotent anticonvulsant activity in man, the contribution of CBZ-E approximates to 30% of total anticonvulsant effect in children taking CBZ alone.
Plasma concentrations of carbamazepine and Carbamazepine 10,11-epoxide during pregnancy and after delivery
Clin Pharmacokinet 1985 May-Jun;10(3):279-84.PMID:4017398DOI:10.2165/00003088-198510030-00007.
Plasma concentrations of carbamazepine were monitored in 9 pregnant epileptic patients treated with the drug alone at constant doses during pregnancy and for at least 3 months after delivery. In addition, plasma concentrations of the metabolite, Carbamazepine 10,11-epoxide were measured in 6 of the 9 patients. Plasma carbamazepine concentrations were fairly stable during pregnancy, and carbamazepine relative plasma clearances were significantly higher in weeks 4 to 24 than in weeks 25 to 32. After the end of the second trimester, there were no variations in plasma Carbamazepine 10,11-epoxide concentrations and Carbamazepine 10,11-epoxide:carbamazepine ratios. Both parameters were significantly higher in weeks 4 to 24 than in weeks 25 to 32 of pregnancy.
Determinants of carbamazepine and Carbamazepine 10,11-epoxide binding to serum protein, albumin and alpha 1-acid glycoprotein
Br J Clin Pharmacol 1984 Oct;18(4):487-93.PMID:6487490DOI:10.1111/j.1365-2125.1984.tb02496.x.
The binding of carbamazepine and Carbamazepine 10,11-epoxide to serum, albumin and alpha 1-acid glycoprotein (AAG) was determined and compared at drug concentrations ranging from 0.5 to 400 mg/l using equilibrium dialysis and liquid chromatography. The total binding of carbamazepine in serum was determined primarily by albumin and to a lesser extent (20-30%) by AAG. Modified Scatchard plots for carbamazepine binding in serum were biphasic, suggesting the presence of two binding sites on serum protein. Association constants characterizing the first (k1 = 2.4 X 10(4) l/mol) and second (k2 = 4.6 X 10(2) l/mol) binding sites agreed with those measured for AAG and albumin respectively. Modified Scatchard plots for Carbamazepine 10,11-epoxide binding in serum were linear and serum binding was largely accounted for by binding to albumin. The epoxide metabolite did not bind to AAG. Carbamazepine binding to AAG was drug concentration-dependent over the concentration range considered to be therapeutic, while the percent binding values for carbamazepine and epoxide binding to albumin and serum from a normal individual were constant over this range. Computer simulations showed that physiological extremes in AAG and albumin concentrations can result in a range of carbamazepine unbound fractions of 0.17 to 0.47. These data suggest that normal variations in concentrations of both proteins may be the principal cause of interpatient variability in serum protein binding of carbamazepine.