156364-04-4
156364-04-4 性质
| 密度 | 1.37±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 10.68±0.40(Predicted) |
156364-04-4 用途与合成方法
IC50: 17 nM (BZ1 receptor)
SX-3228 is a selective ligand for the BZ1 receptor. Among the BZ-receptor subtypes, SX-3228 preferentially binds to the BZ1 receptor (IC 50 =17 nM). It has very weak affinity for the BZ2 receptor (spinal cord: IC 50 =127 nM), and virtually no affinity for the peripheral type BZ receptor (kidney: IC 50 >10000 nM). A compound with similar selectivity, SX-3228 has been shown to bind to BZ receptors, but not to dopamine (D 1 , D 2 ), serotonin (5-HT 1 , 5-HT 2 and 5-HT 3 subtypes), noradrenaline (α 1 , α 2 , β), GABA or acetylcholine (muscarinic) subtypes.
Administration of 0.5-2.5 mg/kg SX-3228 to rats during the light phase induces a significant reduction of rapid-eye-movement sleep (REMS) (P<0.05) during the third recording hour. Administration of SX-3228 (0.5-2.5 mg/kg) at the beginning of the dark period significantly and dose-dependently reduces waking (W) and increases slow wave sleep (SWS) during the 6-h recording period (P<0.05-0.01); however, significant changes during the last recording hour are restricted to the 2.5 mg/kg dose (P<0.01).
