| Bioactivity | AM-1488 is a potent, orally active glycine receptor (GlyR) potentiator (hGlyRα3 EC50=0.45 μM)[1][2]. |
| Invitro | AM-1488 also potentiates native GlyRs in mouse spinal-cord neurons, which express mostly GlyRα1(β) and GlyRα3(β)[1]. Cell Viability Assay[1] Cell Line: |
| 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: |
| Name | AM-1488 |
| CAS | 2079895-60-4 |
| Formula | C19H17N3O4S |
| Molar Mass | 383.42 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. |