| Bioactivity | SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC50 of 17 nM. |
| Target | IC50: 17 nM (BZ1 receptor) |
| Invitro | SX-3228 is a selective ligand for the BZ1 receptor. Among the BZ-receptor subtypes, SX-3228 preferentially binds to the BZ1 receptor (IC50=17 nM). It has very weak affinity for the BZ2 receptor (spinal cord: IC50=127 nM), and virtually no affinity for the peripheral type BZ receptor (kidney: IC50>10000 nM). A compound with similar selectivity, SX-3228 has been shown to bind to BZ receptors, but not to dopamine (D1, D2), serotonin (5-HT1, 5-HT2 and 5-HT3 subtypes), noradrenaline (α1, α2, β), GABA or acetylcholine (muscarinic) subtypes[1]. |
| In Vivo | 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)[1]. |
| Name | SX-3228 |
| CAS | 156364-04-4 |
| Formula | C18H18N4O3 |
| Molar Mass | 338.36 |
| 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]. Alvariño F, et al. Effect of SX-3228, a selective ligand for the BZ1 receptor, on sleep and waking during the light-dark cycle in the rat. Braz J Med Biol Res. 1999 Aug;32(8):1007-14. |