PeptideDB

SX-3228

CAS: 156364-04-4 F: C18H18N4O3 W: 338.36

SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC50 of 17 nM.
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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.