A-841720

A-841720 is a noncompetitive antagonist of the group 1 metabotropic glutamate receptor mGluR1 with an IC₅₀ value of 10.7 nM for inhibition of L-glutamate-induced calcium release in 1321 N1 cells.¹ It is selective for mGluR1 over mGluR5 (IC₅₀ = 343 nM) as well as mGluR2, mGluR4, and mGluR7, where it does not inhibit agonist-induced calcium release in HEK293 cells. It is also selective for mGluR1 over a panel of other G-coupled protein receptors as well as ligand- and voltage-gated ion channels at a concentration of 10 µM. A-841720 dose-dependently inhibits complete Freund's adjuvant-induced inflammatory pain (ED₅₀ = 23 µmol/kg) and sciatic nerve injury-induced mechanical allodynia (ED₅₀ = 28 µmol/kg) in rats. It also enhances cocaine seeking in mice after a prolonged abstinence following a single conditioning session when administered at a dose of 10 mg/kg per day.²

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1. El-Kouhen, O., Lehto, S.G., Pan, J.B., et al. Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: Effects of A-841720, a novel non-competitive mGluR1 receptor antagonist. Br. J. Pharmacol. 149(6), 761-774 (2006).

2. Halbout, B., Bernardi, R.E., Hansson, A.C., et al. Incubation of cocaine seeking following brief cocaine experience in mice is enhanced by mGluR1 blockade. J. Neurosci. 34(5), 1781-1790 (2014).