Moxisylyte hydrochloride (Thymoxamine hydrochloride)
(Synonyms: 4-(2-二甲氨基乙氧基)-5-异丙基-2-甲基酯盐酸盐,Thymoxamine hydrochloride) 目录号 : GC32485
Moxisylyte hydrochloride (thymoxamine) is an alpha-adrenergic blocking agent used for the treatment of Raynaud's disease.
Cas No.:964-52-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Moxisylyte hydrochloride (thymoxamine) is an alpha-adrenergic blocking agent used for the treatment of Raynaud's disease.
| Cas No. | 964-52-3 | SDF | |
| 别名 | 4-(2-二甲氨基乙氧基)-5-异丙基-2-甲基酯盐酸盐,Thymoxamine hydrochloride | ||
| Canonical SMILES | CC(C1=C(OCCN(C)C)C=C(C)C(OC(C)=O)=C1)C.[H]Cl | ||
| 分子式 | C16H26ClNO3 | 分子量 | 315.84 |
| 溶解度 | Water : ≥ 50 mg/mL (158.31 mM);DMSO : 20 mg/mL (63.32 mM) | 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 | 3.1662 mL | 15.8308 mL | 31.6616 mL |
| 5 mM | 0.6332 mL | 3.1662 mL | 6.3323 mL |
| 10 mM | 0.3166 mL | 1.5831 mL | 3.1662 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。
Thymoxamine hydrochloride: an alpha-adrenergic blocker
Surv Ophthalmol 1980 Sep-Oct;25(2):75-84.PMID:6108620DOI:10.1016/0039-6257(80)90150-2.
Thymoxamine is an alpha-adrenergic blocking agent which works by competitive antagonism of norepinephrine. It is the only alpha-adrenergic blocker available which has tolerable side effects when used as an ophthalmic solution. When used as a 0.5% solution it consistently produces miosis without affecting the intraocular pressure or the ciliary muscle-controlled facility of outflow. The only regularly reported side-effects at this concentration are transient burning and conjunctival hyperemia. Potential applications of thymoxamine include reversal of phenylephrine mydriasis, treatment of angle-closure glaucoma, treatment of persistent mydriasis after penetrating keratoplasty for keratoconus, reversal of lid retraction in thyroid ophthalmopathy, testing to differentiate angle-closure glaucoma from open-angle glaucoma with narrow angles, aiding in repositioning and maintaining the position of intraocular lenses, treatment of pigmentary glaucoma. Thymoxamine may also contribute to a better understanding of the adrenergic nervous system on aqueous dynamics.
Effect of Moxisylyte hydrochloride on isolated human penile corpus cavernosum tissue
Life Sci 1989;44(9):619-23.PMID:2522580DOI:10.1016/0024-3205(89)90194-x.
The effect of Moxisylyte hydrochloride on isolated human penile corpus cavernosum tissue was investigated and compared with other a-adrenergic antagonists. Moxisylyte produced a concentration-dependent relaxation of a norepinephrine-induced (1 x 10(-5) M) contraction of the corpus cavernosum tissue. Pretreatment with 1 x 10(-6) M doses of moxisylyte reduced competitively the norepinephrine-induced contraction. The competitive effect of prazosin was strongest among four tested agents, followed by phentolamine, moxisylyte, and then yohimbine. The activity ratio for each antagonist is 2.4 for moxisylyte, as compared with 28.2 for prazosin, 6.7 for phentolamine, and 1.6 for yohimbine respectively. Moxisylyte hydrochloride is an agent with potential clinical and research uses capable of producing erection when injected intra-cavernously.
Effect of Moxisylyte hydrochloride (alpha 1-blocker) on the retinal circulation of patients with diabetes mellitus
Ophthalmic Res 1992;24(5):274-9.PMID:1475074DOI:10.1159/000267178.
Moxisylyte hydrochloride (alpha 1-blocker) selectively vasodilates cerebral vessels without reducing blood pressure. We investigated the effect of the drug on retinal circulation in 15 patients (17 eyes) with diabetes mellitus, using the video-densitometric image analysis of fluorescein angiography. We compared the build-up time (BT), the time constant of washout rate (TC) and the mean circulation time (MCT) before and after oral therapy with moxisylyte. In 16 eyes, BT was shortened significantly and MCT was only slightly shortened 1 h after oral therapy with moxisylyte. After 2 weeks of daily administration, MCT was shortened and TC of the artery was increased significantly in 6 eyes. Since retinal circulation in patients with diabetes mellitus was improved by moxisylyte, the drug may be useful to treat ocular disorders such as diabetic retinopathy.
[Acute and chronic effect of Moxisylyte hydrochloride on the retinal circulation in diabetes mellitus]
Nippon Ganka Gakkai Zasshi 1991 Nov;95(11):1135-41.PMID:1836935doi
The effect of Moxisylyte hydrochloride, a new type alpha 1-blocking vasodilator, on the retinal circulation was investigated in 14 diabetics, using the video-densitometric image analysis of fluorescein angiography. The build-up time (BT) and the mean circulation time (MCT) were compared before and after oral administration of moxisylyte. The BT one hour after oral administration of 30 mg moxisylyte was significantly shorter than that before therapy (artery; before 5.2 +/- 1.5 vs after 4.6 +/- 1.0 sec; p = 0.0001, vein; before 6.9 +/- 1.3 vs 6.3 +/- 1.1 sec; p = 0.0005). The MCT two weeks after oral administration of 90 mg per day moxisylyte was significantly shortened (before 3.6 +/- 2.3 vs after 2.6 +/- 1.4 sec; p = 0.0180). These results suggested that oral moxisylyte improved the retinal circulation and might support the concept that Moxisylyte hydrochloride has clinical usefulness in patients with diabetes mellitus.
Effect of thymoxamine on the human pupil
Exp Eye Res 1983 May;36(5):655-62.PMID:6221938DOI:10.1016/0014-4835(83)90103-3.
The specificity of thymoxamine, an alpha-adrenoceptor antagonist was determined from in vitro organ bath studies using isolated preparations of canine saphenous and portal mesenteric veins. It was found that thymoxamine interacts mainly with postjunctional alpha-adrenoceptors. The miotic effects of topical Thymoxamine hydrochloride were measured in normal human eyes using infrared pupillography. The effects of five different concentrations of thymoxamine were measured over time. Time-response and concentration-response relationships were calculated. The maximal pupillary response occurs at 60 min after instillation of the drug and has a half-life of 10 hr. The minimum effective concentration of thymoxamine is 0.01%, and the maximum effective concentration is 1.3%. Thymoxamine's properties could make it a clinically useful drug to diagnose angle-closure glaucoma, and also to reverse drug-induced mydriasis.