| Description | TCN238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4with an EC50 of 1 μM). |
| In vitro | TCN238 has a greater than 30-fold selectivity for mGluR4 over mGluR5 using human recombinant receptors in CHO-K1 cells[1]. |
| In vivo | 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]. |
| Target activity | mGlu4 receptor:1 μM (EC50) |
| Synonyms | TCN 238 |
| molecular weight | 197.24 |
| Molecular formula | C12H11N3 |
| CAS | 125404-04-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 150 mg/mL (760.49 mM) |
| References | 1. Pershina E V , Arkhipov V I . Subacute activation of mGlu4 receptors causes the feedback inhibition of its gene expression in rat brain[J]. Life Sciences, 2016, 153:50-54. 2. East S P , Bamford S , Dietz M G A , et al. An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction[J]. Bioorganic & Medicinal Chemistry Letters, 2010, 20(16):4901-4905. |