Cayman 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 A_2A, serotonin 5-HT_1A, or α_2A-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 GABA_A receptor α subunit, GABRA1, in the frontal cortex without affecting hippocampal-dependent memory.

WARNING This product is not for human or veterinary use.