(E)-3,4,5-Trimethoxycinnamic acid (Synonyms: TMCA) |
| Catalog No.GC66255 |
L'acide (E)-3,4,5-triméthoxycinnamique (TMCA) est un acide cinnamique substitué par des groupes multi-méthoxy. L'acide (E)-3,4,5-triméthoxycinnamique est un puissant agoniste des récepteurs GABAA/BZ actif par voie orale. Le (E)-3,4,5-triméthoxycinnamique présente une affinité de liaison favorable aux récepteurs 5-HT2C et 5-HT1A, avec des valeurs IC50 de 2,5 et 7,6 μM, respectivement. L'acide (E)-3,4,5-triméthoxycinnamique présente une activité anticonvulsivante et sédative. L'acide (E)-3,4,5-triméthoxycinnamique peut être utilisé pour la recherche de l'insomnie, des maux de tête et de l'épilepsie.
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.
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(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.)
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