Methocinnamox

甲氧基肉桂酸与小鼠脑组织中的μ受体紧密结合，解离速度非常缓慢，但对δ和κ受体的结合位点没有影响[3]。甲氧基肉桂酸可以不可逆地阻断DAMG、精神活性化合物和吗啡对转染人μ阿片受体的HEK293细胞中cAMP积累的抑制作用[3]。

Methocinnamox (10 mg/kg，皮下注射，单剂量)可有效应对在吗啡介导的多种作用(镇痛、呼吸抑制、胃肠道抑制和睡眠变化)，且单次后拮抗抗作用可持续超过数千[1]。 Methocinnamox (0.0001-10 mg/kg，静脉注射或10 mg/kg，静脉注射和下皮注射，单次注射) Methocinnamox (0.32 mg/kg，皮下注射，单次，或每12天一次，共5次；0.032 mg/kg，每日一次，共21天)可降低恒猴阿片类药物的自我行为阿富汗[3]。

Animal/Disease Models: Paw inflammation and mechanical sensitivity, gastrointestinal transit and physical dependence and withdrawal model established in male Sprague-Dawley rats[1]
Doses: 10 mg/kg
Route of Administration: Subcutaneous injection (s.c.), single dose
Experimental Results: Significantly reduced the analgesic effect of morphine on paw inflammation and this antagonistic effect persisted for at least 15 days. Blocked the increase in body temperature caused by morphine, with the effect lasting for more than 15 days. Completely blocked the inhibitory effect of morphine on gastrointestinal peristalsis until 21 days. Did not result in a longer or more severe withdrawal syndrome.

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Animal/Disease Models: Reversal of psychoactive compound assay established in adult male Sprague-Dawley rats[2]
Doses: 0.0001, 0.001, 0.01, 0.1, 1, 10 mg/kg (i.v.) and 10 mg/kg (i.v.) and (s.c)
Route of Administration: Intravenous injection (i.v.) and subcutaneous injection (s.c.), single dose
Experimental Results: Dose-dependently rapidly reversed severe respiratory depression. Provide long-lasting protection and effectively prevent the "re-anesthesia" phenomenon that occurs after rescue. Exhibited a significantly longer duration of action when administered subcutaneously (s.c.) compared to intravenous (i.v.) administration at the same dose.

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Animal/Disease Models: Self-Administration model established in rhesus monkeys[3]
Doses: 0.032 mg/kg and 0.32 mg/kg
Route of Administration: Subcutaneous injection (s.c.), single dose, or once every 12 days for 5 doses (0.32 mg/kg); once daily for 21 days (0.032 mg/kg)
Experimental Results: Effectively and selectively blocked the reinforcing effects (euphoria) of opioid agent. Reduced the relative reinforcing value of opioid drugs, making non-drug rewards (such as food) more attractive. Did not impair advanced cognitive functions such as working memory or attention. had no significant effect on the cardiovascular system and body temperature regulation at 3.2 mg/kg.

C30H32N2O4

484.59

117339-76-1

Typically exists as solids at room temperature

M-CAM

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。