| Description | CLP290 is an activator of the neuron-specific K+-Cl cotransporter KCC2 and displays potential for the treatment of a wide range of neurological and psychiatric indications. |
| In vivo | In vivo co-treatment with morphine and oral CLP290 prevented membrane KCC2 downregulation in SDH neurons.?Concurrently, co-treatment with CLP290 significantly mitigated MIH and acute administration of CLP257 in established MIH restored normal nociceptive behavior. |
| Animal experiments | Morphine sulfate (50 mg/ml) was diluted in saline sterile solution immediately before injection.?Morphine or saline were subcutaneously injected twice a day (10 mg/kg;?9 a.m. 6 p.m.) in na?ve adult rats.?The KCC2 enhancer CLP257 and its carbamate pro-drug CLP290 were freshly diluted in 20% 2-hydroxypropyl-β-cyclodextrin (HPCD) prior injection.?CLP257 or vehicle were delivered intraperitoneally after 7 8 days of morphine or saline, as described (100 mg/kg).?CLP290 or vehicle were delivered orally by gavage twice a day for the whole duration of the morphine/saline treatment (100 mg/kg). |
| Synonyms | CLP-290 |
| molecular weight | 404.46 |
| Molecular formula | C19H21FN4O3S |
| CAS | 1181083-81-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 12 mg/mL (29.67 mM) |
| References | 1. Ferrini F, et al. Enhancing KCC2 function counteracts morphine-induced hyperalgesia. Sci Rep. 2017 Jun 20;7(1):3870. |