1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor


Cat. No.: HY-100291
Handling Instructions

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

For research use only. We do not sell to patients.

SX-3228 Chemical Structure

SX-3228 Chemical Structure

CAS No. : 156364-04-4

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


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

IC50 & Target

IC50: 17 nM (BZ1 receptor)[1]

In Vitro

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].

Animal Administration

Twelve male Wistar rats (350-380 g) are used. Subcutaneous (sc) injections are given in a final volume of 1.0 mL/kg. All rats are given the corresponding volume of control solution (saline+Tween-80) in the control sessions. Following sc injection, a 6-h sleep recording is started at approximately 8:00 a.m. At least 4 days are allowed to elapse between injections to avoid long-lasting and rebound effects on sleep. The effects of SX-3228 0.5-2.5 mg/kg are studied in one group of animals (N=6) during the light phase of the 12-h light:12-h dark cycle, starting 1 h after the beginning of the light period. Polysomnographic recordings are started immediately after control solution or drug administration. Each rat receives all four treatments (control, and 0.5, 1.0, 2.5 mg/kg SX-3228).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight









Please store the product under the recommended conditions in the Certificate of Analysis.


Room temperature in continental US; may vary elsewhere

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Cat. No.: HY-100291