| 产品描述 | (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]. (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. |
(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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