| Description | GYKI 53655 hydrochloride (LY300168 hydrochloride) is an antagonist of AMPA and is used in the study of neurological disorders. |
| In vitro | GYKI 53655 hydrochloride 分别在在 HEK293 细胞中表达的重组人 GluR1 受体和重组人 GluR4 受体中抑制AMPA（10microM）介导的反应，其近似 IC50 值分别为 6 μM 以及 5 μM[1]。 |
| In vivo | GYKI 53655 hydrochloride（2-8 mg/kg）能够在体内剂量依赖性抑制或完全消除 AMPA 反应[3]。 |
| Target activity | mGluR4:5 μM, mGluR1:6 μM |
| Synonyms | GYKI53655 hydrochloride, LY300168 hydrochloride |
| molecular weight | 388.85 |
| Molecular formula | C19H21ClN4O3 |
| CAS | 143692-48-2 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 120 mg/mL (308.60 mM), Sonication is recommended. H2O: 2 mg/mL (5.14 mM), Sonication is recommended. |
| References | 1. Bleakman D, et al. Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: stereospecificity and selectivity profiles. Neuropharmacology. 1996;35(12):1689-702. 2. Chizh BA, et al. A comparison of intravenous NBQX and GYKI 53655 as AMPA antagonists in the rat spinal cord. Br J Pharmacol. 1994 Jul;112(3):843-6. 3. Szabados T, et al. Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res Bull. 2001 Jun;55(3):387-91. |