| Identification | Back Directory | [Name]
4H-Pyrrolo[3,4-c][1,6]naphthyridin-4-one, 2-(5-benzofuranylsulfonyl)-1,2,3,3a,5,9b-hexahydro-5-methyl-, (3aS,9bS)- | [CAS]
2079895-60-4 | [Synonyms]
4H-Pyrrolo[3,4-c][1,6]naphthyridin-4-one, 2-(5-benzofuranylsulfonyl)-1,2,3,3a,5,9b-hexahydro-5-methyl-, (3aS,9bS)- | [Molecular Formula]
C19H17N3O4S | [MOL File]
2079895-60-4.mol | [Molecular Weight]
383.42 |
| Hazard Information | Back Directory | [Description]
AM1488 is a Potent and Efficacious Potentiator of Glycine Receptor. | [Uses]
AM-1488 is a potent, orally active glycine receptor (GlyR) potentiator (hGlyRα3 EC50=0.45 μM)[1][2]. | [in vivo]
AM-1488 (oral gavage; 20 mg/kg; once) treatment significantly reverse mechanical allodynia induced by nerve injury in a mouse model of neuropathic pain, without being confounded by sedation or motor side effects[1]. | Animal Model: | Mouse model of spared nerve injury (SNI)[1] | | Dosage: | 20 mg/kg | | Administration: | Oral gavage; 20 mg/kg; once | | Result: | Produced a significant 94% reversal of tactile allodynia, and the unbound brain concentration was 2.8- and 1.6-fold higher than the mouse GlyRα1 and GlyRα3 EC50 values, respectively. |
| Animal Model: | Naive mice[1] | | Dosage: | 20 mg/kg | | Administration: | Oral gavage; 20 mg/kg; once | | Result: | Showed not significantly different from mice treated with vehicle. |
| [References]
[1] Xin Huang, et al. Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators. Nat Struct Mol Biol. 2017 Feb;24(2):108-113. DOI:10.1038/nsmb.3329
[2] Howard Bregman, et al. The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors. J Med Chem. 2017 Feb 9;60(3):1105-1125. DOI:10.1021/acs.jmedchem.6b01496 |
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