Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: (E)-4-(2-phenylethenyl)-2-pyrimidinamine
Purity: ≥98%
Formula Markup: C12H11N3
Formula Weight: 197.2
CAS Number: 125404-04-8
Notes: TCN 238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4; EC50 = 1 µM).{40126} 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 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.{40127}
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