TAK-653

TAK-653 is an AMPA receptor positive allosteric modulator (PAM).¹ It increases glutamate-induced calcium influx in CHO cells expressing human AMPA receptors (EC₅₀ = 3.3 µM). TAK-653 potentiates AMPA receptor-mediated currents in primary rat hippocampal neurons (EC₅₀ = 4.4 µM). In vivo, TAK-653 (0.1-10 mg/kg) ameliorates MK-801-induced working memory deficits in the radial arm maze task in rats. It increases accuracy in the delayed match-to-sample (DMTS) test in cynomolgus monkeys when administered at a dose of 0.06 mg/kg. TAK-653 reverses dominance between initially dominant and submissive rat pairs, a marker of antidepressant-like activity, in the rat reduction of submissive behavior model.²

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1. Suzuki, A., Kunugi, A., Tajima, Y., et al. Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement. Sci. Rep. 11(1), 14532 (2021).

2. Hara, H., Suzuki, A., Kunugi, A., et al. TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats. Pharmacol. Biochem. Behav. 211:173289, (2021).