ACPT-I

ACPT-I is an agonist of the group III metabotropic glutamate receptors (mGluRs) mGluR4a and mGluR8 (EC₅₀s = 7.2 and 8.2 µM, respectively) that has no effect on mGluR1a or mGluR2.¹ It has diverse biological activity, including neuroprotective, anticonvulsant, and anxiolytic-like effects.^2,3,4,5 ACPT-I (1-200 µM) reduces cell death following oxygen-glucose deprivation in primary neuronal cultures and in a rat model of middle cerebral artery occlusion when used at a dose of 30 mg/kg.² It is neuroprotective against excitotoxicity induced by kainite in vitro and in vivo and reduces the incidence of clonic seizures in various seizure models in mice and rats (ED₅₀s = 0.08-49.3 nM, i.c.v.).^3,4 ACPT-I also has anxiolytic-like effects in mice and rats, however, these effects can be blocked by WAY-100635 (Item No. 14599) and flumazenil (Item No. 14252), indicating the involvement of the serotonin (5-HT) receptor subtype 5-HT_1A and GABA_A receptor.⁵

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1. Acher, F.C., Tellier, F.J., Azerad, R., et al. Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: New tools to discriminate between metabotropic glutamate receptor subtypes. J. Med. Chem. 40, 3119-3129 (1997).

2. Domin, H., Przykaza, Ł., Jantas, D., et al. Neuroprotective potential of the group III mGlu receptor agonist ACPT-I in animal models of ischemic stroke: In vitro and in vivo studies. Neuropharmacology 102, 276-294 (2016).

3. Domin, H., Gołenbiowska, K., Jantas, D., et al. Group III mGlu receptor agonist, ACPT-I, exerts potential neuroprotective effects in vitro and in vivo. Neurotox. Res. 26(1), 99-113 (2014).

4. Chapman, A.G., Talebi, A., Yip, P.K., et al. Anticonvulsant activity of a mGlu4α receptor selective agonist, (1S,3R,4S)-1-aminocyclopentane-1,2,4-tricarboxylic acid. Eur. J. Pharmacol. 424(2), 107-113 (2001).

5. Stachowicz, K., Kłodzińska, A., Palucha-Poniewiera, A., et al. The group III mGlu receptor agonist ACPT-I exerts anxiolytic-like but not antidepressant-like effects, mediated by the serotonergic and GABA-ergic systems. Neuropharmacology 57(3), 227-234 (2009).