Dextrorphan (tartrate)
(Synonyms: 去甲右美沙芬酒石酸盐,d-3-hydroxy-N-Methylmorphinan tartrate) 目录号 : GC18213
右啡烷（酒石酸盐）是右美沙芬的苯环利定样代谢物，在止咳药中用作镇咳剂。
Cas No.:143-98-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Dextrorphan (tartrate) is a phencyclidine-like metabolite of dextromethorphan, kwoun as an antitussive in cough medicines [1]. Dextrorphan (tartrate) is a noncompetitive N-methyl-d-aspartate (NMDA) antagonist that is neuroprotective in experimental models of focal brain ischemia [2]. Dextrorphan (tartrate) concentrations producing IC50 of K+-stimulated 45Ca 2+ uptake into brain synaptosomes was 200±27μM [3].
Dextrorphan (tartrate) inhibit excitatory amino acid (EAA) evoked neuronal responses, apparently by acting at a site on the NMDA-preferring EAA receptor or its associated Ca 2+ channel. Dextromethorphan and dextrorphan (tartrate) protect neurons from EAA-induced cytotoxicity [3].
In dextrorphan-treated patients, transient and reversible adverse effects, including nystagmus, nausea, vomiting, somnolence, hallucinations, and agitation, commonly occurred. Loading-dose escalation was stopped because of rapid-onset, reversible, symptomatic hypotension in 7 of 21 patients treated with doses of 200 to 260 mg/h. Maximum plasma levels of 750 to 1000 ng/mL were obtained in 9 patients [2].
References:
[1]. Shin, E.J., Lee, P.H., Kim, H.J., et al. Neuropsychotoxicity of abused drugs: Potential of dextromethorphan and novel neuroprotective analogs of dextromethorphan with improved safety profiles in terms of abuse and neuroprotective effects. Journal of Pharmacological Sciences 106(1), 22-27 (2008).
[2]. Albers GW, Atkinson RP, Kelley RE, Rosenbaum DM; Dextrorphan Study Group. Safety, tolerability, and pharmacokinetics of the N-methyl-d-aspartate antagonist dextrorphan in patients with acute stroke.Stroke. 1995; 26:254-258.
[3]. Carpenter CL, Marks SS, Watson DL, Greenberg DA. Dextromethorphan and dextrorphan as calcium channel antagonists. Brain Res.1988; 439:372-375.
右啡烷（酒石酸盐）是右美沙芬的苯环利定样代谢物，在止咳药中用作镇咳剂 [1]。右啡烷（酒石酸盐）是一种非竞争性 N-甲基-d-天冬氨酸 (NMDA) 拮抗剂，在局灶性脑缺血的实验模型中具有神经保护作用[2]。产生 K+- 刺激 45Ca 2+ 摄入脑突触体的 IC50 的右啡烷（酒石酸盐）浓度为 200±27μM [3]。
右啡烷（酒石酸盐）抑制兴奋性氨基酸 (EAA) 诱发的神经元反应，显然是通过作用于偏好 NMDA 的 EAA 受体或其相关 Ca 2+ 通道上的一个位点。右美沙芬和右啡烷（酒石酸盐）保护神经元免受 EAA 诱导的细胞毒性[3]。
在接受右啡烷治疗的患者中，通常会发生短暂和可逆的不良反应，包括眼球震颤、恶心、呕吐、嗜睡、幻觉和激越。在接受 200 至 260 mg/h 剂量治疗的 21 名患者中，有 7 名因快速发作、可逆、有症状的低血压而停止负荷剂量增加。 9 名患者[2] 的最大血浆浓度为 750 至 1000 ng/mL。
| Animal experiment [1]: | |
|
Animal models |
Rat |
|
Preparation Method |
Slow i.v. injection of 4-6 mg/kg of dextrorphan (tartrate) |
|
Dosage form |
Intravenous injection, 4-6 mg/kg |
|
Applications |
I.v. injection of 4-6 mg/kg of dextrorphan (tartrate) resulted in a selective reduction of NMA-induced excitation similar to that seen during the local administration of the drug by electrophoresis. |
|
References: [1]: J.D. Church, D. Lodge, S.C. Berry.Differential effects of dextrorphan and levorphanol on the excitation of rat spinal neurons by amino acids.Eur J Pharmacol, 111 (1985), pp. 185-190 |
|
| Cas No. | 143-98-6 | SDF | |
| 别名 | 去甲右美沙芬酒石酸盐,d-3-hydroxy-N-Methylmorphinan tartrate | ||
| 化学名 | (9α,13α,14α)-17-methyl-morphinan-3-ol 2R,3R-dihydroxybutanedioate | ||
| Canonical SMILES | CN1[C@@H]2[C@@]3([H])CCCC[C@@]3(CC1)C4=CC(O)=CC=C4C2.O[C@H]([C@@H](O)C(O)=O)C(O)=O | ||
| 分子式 | C17H23NO.C4H6O6 | 分子量 | 407.5 |
| 溶解度 | 20mg/mL in DMSO, 10mg/mL in DMF | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.454 mL | 12.2699 mL | 24.5399 mL |
| 5 mM | 0.4908 mL | 2.454 mL | 4.908 mL |
| 10 mM | 0.2454 mL | 1.227 mL | 2.454 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet