Odapipam
(Synonyms: 奥达匹泮,NNC 756) 目录号 : GC38405
Odapipam (NNC 756) 是一种选择性，高亲和力的苯并氮杂卓多巴胺 D1 受体拮抗剂，Kd 为 0.18 nM。Odapipam 还是一种出色的正电子发射断层扫描 (PET) 放射性示踪剂。
Cas No.:131796-63-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Odapipam (NNC 756) is a selective, high affinity and benzazepine dopamine D1 receptor antagonist with a Kd of 0.18 nM. Odapipam is also a superior positron emission tomography (PET) radiotracer[1][2].
The metabolism of Odapipam has been studied with phenobarbital-induced rat liver microsomes. During the incubation of Odapipam, five different metabolites are formed. The electron-ionization (EI+) mass spectra of the metabolites indicated the formation of N-desmethyl-Odapipam, 1-hydroxy-Odapipam, the two isomers of 3′-hydroxy-Odapipam and a metabolite which is dehydrogenated in the dihydrobenzofuran moiety[3].
[1]. Abi-Dargham A, et al. PET studies of binding competition between endogenous dopamine and the D1 radiotracer [11C]NNC 756. Synapse. 1999 May;32(2):93-109. [2]. Nielsen EB, et al. Dopamine receptor occupancy in vivo: behavioral correlates using NNC-112, NNC-687 and NNC-756, new selective dopamine D1 receptor antagonists. Eur J Pharmacol. 1992 Aug 14;219(1):35-44. [3]. J. VANGGAARD ANDERSEN, et al. Normal-phase liquid chromatography-particle-beam mass spectrometry in drug metabolism studies of the dopamine receptor antagonist Odapipam and the muscarine M1 receptor agonist Xanomeline. Xenobiotica. 1997, 27: 901-912.
| Cas No. | 131796-63-9 | SDF | |
| 别名 | 奥达匹泮,NNC 756 | ||
| Canonical SMILES | OC1=C(Cl)C=C2CCN(C)C[C@H](C3=C(OCC4)C4=CC=C3)C2=C1 | ||
| 分子式 | C19H20ClNO2 | 分子量 | 329.82 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -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 | 3.032 mL | 15.1598 mL | 30.3196 mL |
| 5 mM | 0.6064 mL | 3.032 mL | 6.0639 mL |
| 10 mM | 0.3032 mL | 1.516 mL | 3.032 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。
Normal-phase liquid chromatography-particle-beam mass spectrometry in drug metabolism studies of the dopamine receptor antagonist Odapipam and the muscarine M1 receptor agonist Xanomeline
Xenobiotica 1997 Sep;27(9):901-12.PMID:9381731DOI:10.1080/004982597240073.
1. The metabolism of Odapipam has been studied with phenobarbital-induced rat liver microsomes, followed by analysis with normal-phase hplc in combination with particle-beam mass spectrometry. 2. During the incubation of Odapipam, five different metabolites were formed. The EI+ mass spectra of the metabolites indicated the formation of N-desmethyl-Odapipam, 1-hydroxy-Odapipam, the two isomers of 3'-hydroxy-Odapipam and a metabolite which was dehydrogenated in the dihydrobenzofuran moiety. 3. The intrinsic hepatic extraction ratio and metabolism of Xanomeline has been studied in the perfused rat liver. Increasing the input concentration resulted in measurable concentrations of Xanomeline in the perfusate, although the extraction ratio was still > 0.9 at 140 microM. 4. Analysis of the perfusate by normal-phase hplc and particle-beam mass spectrometry showed the formation of at least six metabolites. The EI+ mass spectrum of the metabolites indicated the formation of omega-3 hydroxy-, omega-2 hydroxy-, omega-1 hydroxy-, omega-1 keto-Xanomeline in addition to omega-1 hydroxy-N-desmethyl-Xanomeline and an N-oxide of Xanomeline. 5. The results show that normal-phase hplc based on silica material is superior to reversed-phase-based systems in terms of selectivity. Furthermore, the use of non-aqueous solvents in combination with particle-beam mass spectrometry is advantageous compared with reversed-phase hplc since changing between different solvents in normal-phase hplc results only in minor changes in the particle-beam interface parameters such as nebulizer position, helium pressure and interface temperature.
Characterization of benzazepine UDP-glucuronosyl-transferases in laboratory animals and man
Xenobiotica 1995 Jun;25(6):611-22.PMID:7483661DOI:10.3109/00498259509061879.
1. The O-glucuronidation of two dopamine D1 receptor antagonists, Odapipam and Berupipam, were studied in hepatic microsomal fractions from mouse, rat, rabbit, dog, pig, and man using 14C-UDP-glucuronic acid. 2. The influence of pH, detergent, gender, drug-metabolizing enzyme inducers, and age were examined. Detergents like the zwitterionic CHAPS and non-ionic Tween 20, Triton X-100, and Brij 35 stimulated the glucuronidation rate by up to 600% of native activity with the latter being most effective. Both apparent Km and Vmax increased following detergent treatment in rat hepatic microsomes. Less marked activation of UDP glucuronosyltransferase activity was observed with Brij 35 in mouse, rabbit, dog, and pig compared with rat. In contrast, human hepatic microsomes were not stimulated by detergent treatment. 3. Marked species-dependent UDP-glucuronosyltransferase activity were observed for the two compounds. In general, Odapipam exhibited higher Vmax and Km compared with Berupipam with the exception of rabbit where the reverse was true. Similar kinetic parameters were, however, observed in human hepatic microsomes. Highest glucuronidation rate (in general) was observed in mouse followed by dog, pig, rabbit, man, and rat. 4. UGT activity in human livers showed up to a seven-fold variation. Conjugation of each compound were highly correlated (r = 0.92; n = 20) suggesting that identical isoform(s) were involved in this reaction. A significant age-related decrease in UDP-glucuronosyltranferase activity was observed, which partly could be explained by a preponderance in elderly female donor liver samples.