(E)-Alprenoxime (CDDD-1815)
(Synonyms: CDDD-1815) 目录号 : GC32522
(E)-Alprenoxime (CDDD-1815) 是 Alprenoxime 的异构体。
Cas No.:125720-84-5
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
Animal experiment: | Dogs[1] Seven adult mongrel dogs (20-27 kg) are used in this study. A loading dose of Alprenoxime is administered (1 mg/kg, i.v.) followed by Alprenoxime infusion (150 μg/kg/min) after recording baseline electrophysiological parameters. Cardiac electrophysiological testing is then repeated 10 min after beginning Alprenoxime infusion. Alprenoxime (1 or 5 mg/kg, i.v.) is injected as a bolus injection and cardiac electrophysiological response is monitored. Different dogs with isoproterenol induced tachycardia are evaluated at each Alprenoxime dose. |
References: [1]. Polgar P, et al. Minimal cardiac electrophysiological activity of alprenoxime, a site-activated ocular beta-blocker, in dogs. Life Sci. 1995;56(14):1207-13. | |
(E)-Alprenoxime is the isomer of the Alprenoxime. Alprenoxime is a site-activated ocular β-blocker.
The purpose of the present study is to explore the pharmacological significance of Alprenoxime peripheral /βblocking activity in a non-rodent animal model. Interspecies scaling considerations predict that the doses selected in this study (1 and 5 mg/kg) are pharmacologically comparable or greater than doses used in rodent studies (2 and 6 mg/kg). More importantly, the prolonged ocular antihypertensive effects that are shown with 1% ophthalmic solutions indicate that the i.v. dose tested in the present study is likely to be more than two orders of magnitude greater than probable therapeutic doses[1].
[1]. Polgar P, et al. Minimal cardiac electrophysiological activity of alprenoxime, a site-activated ocular beta-blocker, in dogs. Life Sci. 1995;56(14):1207-13.
| Cas No. | 125720-84-5 | SDF | |
| 别名 | CDDD-1815 | ||
| Canonical SMILES | C=CCC1=CC=CC=C1OC/C(CNC(C)C)=N/O | ||
| 分子式 | C15H22N2O2 | 分子量 | 262.35 |
| 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 | 3.8117 mL | 19.0585 mL | 38.117 mL |
| 5 mM | 0.7623 mL | 3.8117 mL | 7.6234 mL |
| 10 mM | 0.3812 mL | 1.9059 mL | 3.8117 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。
Improved delivery through biological membranes. LVI. Pharmacological evaluation of alprenoxime--a new potential antiglaucoma agent
Pharm Res 1991 Nov;8(11):1389-95.PMID:1798675DOI:10.1023/a:1015849123020
A new site-specific chemical delivery system (CDS) for alprenolol was designed and investigated as a potential novel antiglaucoma agent. The effect of this compound, alprenoxime (AO), on the intraocular pressure (IOP) of rabbits was evaluated after its uni- and bilateral administration. AO produced significant reduction of the IOP starting at 30 min and lasting for more than 6 hr after its topical administration. Both in rats and in rabbits the i.v. bolus injection of AO (6 mg/kg) led to insignificant transient bradycardia, while no activity was found after oral or topical administration. Alprenolol (ALP) in a similar dose produced a sustained and significant bradycardia for more than 30 min. When the beta-adrenergic blocking activity was assessed against isoprenaline-tachycardia, the same results were obtained, i.E., AO led to a transient brief activity, whereas ALP produced a significant long-lasting beta blockade. These results support the potent ocular hypotensive action and the weak systemic beta-adrenergic blocking and cardiovascular activity of AO: a significant improvement in the therapeutic index. This finding recommends alprenoxime as a potent site-specific antiglaucoma agent with minimal systemic side effects.