TC-N 22A

TC-N 22A is a potent, selective, orally active and brain-permeable mGlu₄ PAM with an EC₅₀ of 9 nM in human mGlu₄-expressing BHK cells. TC-N 22A is less active (EC₅₀>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo^[1].
IC50 & Target: EC50: 9 nM (mGlu₄ receptor)
EC50: >10 μM (mGlu 1, 2, 3, 5, and 7 receptors)^[1] In Vitro: TC-N 22A is selected for mGlu₄ and has an EC₅₀ of 9 nM in human mGlu₄-expressing BHK cells. This compound is less active in agonist and PAM modelinactive (EC₅₀>10 μM), and is inactive in negative allosteric modulator (NAM) model at mGlu 1, 2, 3, 5, and 7 receptors (IC₅₀ >10 μM) and shows low potential for hERG channel inhibition^[1].
In Vivo: TC-N 22A (oral administration; 10 mg/kg) displays good plasma (259 ng/mL) and brain exposure levels (200 ng/mL) as well as good brain penetration (brain/plasma ratios of 0.8) after 1 h following a 10 mg/kg oral administration in SpragueDawley rats^[1].