| Identification | Back Directory | [Name]
ACPT-I | [CAS]
194918-76-8 | [Synonyms]
ACPT-I
ACPT I,ACPTI
(1S,3R,4S)-1-AMINOCYCLOPENTANE-1,3,4-TRICARBOXYLIC ACID
4-AMINO-1BETA,2BETA,4BETA-CYCLOPENTANETRICARBOXYLIC ACID
1,2,4-Cyclopentanetricarboxylic acid, 4-amino-, (1α,2α,4β)- | [Molecular Formula]
C8H11NO6 | [MDL Number]
MFCD06795869 | [MOL File]
194918-76-8.mol | [Molecular Weight]
217.18 |
| Chemical Properties | Back Directory | [Boiling point ]
440.4±45.0 °C(Predicted) | [density ]
1.651±0.06 g/cm3(Predicted) | [storage temp. ]
Desiccate at -20°C | [solubility ]
Soluble to 10 mM in water and to 50 mM in 1.1eq. NaOH | [form ]
Powder | [pka]
1.85±0.60(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
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-HT1A and GABAA receptor. | [Uses]
ACPT-I is a competitive antagonist for metabotropic receptors (mGluRs). | [Biological Activity]
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. | [storage]
Desiccate at -20°C | [References]
[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 |
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