(E)-3,4,5-Trimethoxycinnamic acid (TMCA) 是一种被多甲氧基取代的肉桂酸。(E)-3,4,5-Trimethoxycinnamic acid 是一种口服有效的GABAA/BZ受体激动剂。(E)-3,4,5-Trimethoxycinnamic acid 与5-HT2C和5-HT1A受体具有良好的结合亲和力,其IC50值分别为 2.5 和 7.6 μM。(E)-3,4,5-Trimethoxycinnamic acid 具有抗惊厥和镇静活性。(E)-3,4,5-Trimethoxycinnamic acid 可用于失眠、头痛、癫痫的研究。
生物活性 | (E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potentGABAA/BZreceptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to5-HT2Cand5-HT1Areceptor, withIC50values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy[1][2][3]. |
体外研究 (In Vitro) | (E)-3,4,5-Trimethoxycinnamic acid (10 μg/mL, 1 h) increases the expressions of GAD65and γ-subunit of GABAAreceptors in the cerebellar granule cells[3]. (E)-3,4,5-Trimethoxycinnamic acid (0-10 μg/mL, 1 h) shows a significant increase in Cl-influx[3].
Western Blot Analysis[3] Cell Line: | Primary cultured cerebellar granule cells | Concentration: | 10 μg/mL | Incubation Time: | 1 h | Result: | Increased expression of GAD65(glutamic acid decarboxylase) and γ-subunit of GABAA receptors, but did not influence the amounts of a-, b-subunits in the GABAA receptors. |
Cell Viability Assay[3] Cell Line: | Primary cultured cerebellar granule cells | Concentration: | 1, 3, 5, 10 μg/mL | Incubation Time: | 1 h | Result: | Produced a significant increase in Cl-influx. |
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体内研究 (In Vivo) | (E)-3,4,5-Trimethoxycinnamic acid (0-20 mg/kg, IP, once) shows anti-seizure effects[2]. (E)-3,4,5-Trimethoxycinnamic acid (0-10 mg/kg, Orally, once) enhances hypnotic effects in pentobarbital-treated mice[3].
Animal Model: | Ault male KunMing-strain mice (18-20 g, maximal electroshock (MES) and pentylenetetrazol (PTZ) models)[2] | Dosage: | 5, 10 and 20 mg/kg; 10 mL/kg | Administration: | IP, once | Result: | Significantly decreased the incidence of MES-induced THE (tonic hindlimb extension) to 50% and 20% of the value of the vehicle controls at 10 and 20 mg/kg. Decreased the incidence of MES-induced THE to only 80% at 5 mg/kg. Significantly delayed the onset of myoclonic jerks (MJ), and decreased the seizure severity and mortality compared with the vehicle-treated animals in PTZ seizure model. The incidence of generalized clonic convulsions (stage 4) disappeared at doses of both 10 and 20 mg/kg. |
Animal Model: | ICR male mice (25-28 g, 10-12 in each group)[3] | Dosage: | 2, 5 and 10 mg/kg | Administration: | Orally (p.o.), once, 15 min and 1 h prior to pentobarbital injection | Result: | Significantly decreased locomotor activity at 10 mg/kg. Increased NREM and total sleep, but decreased wakefulness. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(419.74 mM;Need ultrasonic) 配制储备液 1 mM | 4.1974 mL | 20.9872 mL | 41.9745 mL | 5 mM | 0.8395 mL | 4.1974 mL | 8.3949 mL | 10 mM | 0.4197 mL | 2.0987 mL | 4.1974 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (10.49 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.49 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (10.49 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.49 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (10.49 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.49 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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