TCN 238

TCN 238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4, EC50 = 1 µM). It has a greater than 30-fold selectivity for mGluR4 over mGluR5 using human recombinant receptors in CHO-K1 cells. It has no activity at the adenosine A2A, serotonin 5-HT1A, or alpha2A-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 alpha subunit, GABRA1, in the frontal cortex without affecting hippocampal-dependent memory.Formal Name: (E)-4-(2-phenylethenyl)-2-pyrimidinamine. CAS Number: 125404-04-8. Molecular Formula: C12H11N3. Formula Weight: 197.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 228, 295 nm. SMILES: NC1=NC=CC(/C=C/C2=CC=CC=C2)=N1. InChi Code: InChI=1S/C12H11N3/c13-12-14-9-8-11(15-12)7-6-10-4-2-1-3-5-10/h1-9H,(H2,13,14,15)/b7-6+. InChi Key: LNUXNUNUGIHCPA-VOTSOKGWSA-N.