(E)-3,4,5-Trimethoxycinnamic acid (Synonyms: TMCA) |
| カタログ番号GC66255 |
(E)-3,4,5-トリメトキシ桂皮酸 (TMCA) は、マルチメトキシ基で置換された桂皮酸です。 (E)-3,4,5-トリメトキシ桂皮酸は、経口で有効な強力な GABAA/BZ 受容体アゴニストです。 (E)-3,4,5-トリメトキシシンナミックは、5-HT2C および 5-HT1A 受容体に対して好ましい結合親和性を示し、IC50 値はそれぞれ 2.5 および 7.6 μM です。 (E)-3,4,5-トリメトキシ桂皮酸は、抗けいれん作用と鎮静作用を示します。 (E)-3,4,5-トリメトキシ桂皮酸は、不眠症、頭痛、てんかんの研究に使用できます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 20329-98-0
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');)
;)
(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 potent GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A receptor, with IC50 values 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].
(E)-3,4,5-Trimethoxycinnamic acid (10 μg/mL, 1 h) increases the expressions of GAD65 and γ-subunit of GABAA receptors 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. |
(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. |
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *