TCN 238 是一种可口服的代谢型谷氨酸受体 4 正变构调节剂，EC50值为 1 μM。

TCN 238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4with an EC50 of 1 μM).

TCN238 has a greater than 30-fold selectivity for mGluR4 over mGluR5 using human recombinant receptors in CHO-K1 cells[1].

TCN238 has no activity at the adenosine A2A, serotonin 5-HT1A, or α2A-adrenergic receptors at concentrations up to 10 μM.?In a haloperidol-induced catalepsy rat model of Parkinson's disease, it dose-dependently reduces catalepsy with an ED50 of approximately 1 mg/kg.?TCN 238 administration in rats leads to downregulation of the mGluR4 gene, GRM4, in the hippocampus and the gene for the GABAA receptor α subunit, GABRA1, in the frontal cortex without affecting hippocampal-dependent memory[1].

125404-04-8

C12H11N3

197.24

TCN 238;TCN238

DMSO:150 mg/mL (760.49 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years