194918-76-8

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. It has diverse biological activity, including neuroprotective, anticonvulsant, and anxiolytic-like effects. 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. 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.). ACPT-I also has anxiolytic-like effects in mice and rats, however, these effects can be blocked by WAY-100635 and flumazenil , indicating the involvement of the serotonin (5-HT) receptor subtype 5-HT_1A and GABA_A receptor.

ACPT-I is a competitive antagonist for metabotropic receptors (mGluRs).

Agonist for group III mGlu receptors (EC 50 values are 7.2 and 8.2 μ M for mGlu 4a and mGlu 8 respectively). Anticonvulsant in mice.

Desiccate at -20°C

[1] FRANCINE C. ACHER. Synthesis and Pharmacological Characterization of Aminocyclopentanetricarboxylic Acids: New Tools to Discriminate between Metabotropic Glutamate Receptor Subtypes[J]. Journal of Medicinal Chemistry, 1997, 40 19: 3119-3129. DOI: 10.1021/jm970207b
[2] HELENA DOMIN . Neuroprotective potential of the group III mGlu receptor agonist ACPT-I in animal models of ischemic stroke: In vitro and in vivo studies[J]. Neuropharmacology, 2016, 102: Pages 276-294. DOI: 10.1016/j.neuropharm.2015.11.025
[3] HELENA DOMIN. Group III mGlu receptor agonist, ACPT-I, exerts potential neuroprotective effects in vitro and in vivo.[J]. Neurotoxicity Research, 2014, 26 1: 99-113. DOI: 10.1007/s12640-013-9455-7
[4] ASTRID G CHAPMAN. Anticonvulsant activity of a mGlu4α receptor selective agonist, (1S,3R,4S)-1-aminocyclopentane-1,2,4-tricarboxylic acid[J]. European journal of pharmacology, 2001, 424 2: Pages 107-113. DOI: 10.1016/s0014-2999(01)01013-5
[5] K. STACHOWICZ . The group III mGlu receptor agonist ACPT-I exerts anxiolytic-like but not antidepressant-like effects, mediated by the serotonergic and GABA-ergic systems[J]. Neuropharmacology, 2009, 57 3: Pages 227-234. DOI: 10.1016/j.neuropharm.2009.06.005