1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. CX1763

CX1763 is an AMPAR allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of AMPAR containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression.

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CX1763

CX1763 Chemical Structure

CAS No. : 1086378-73-5

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Description

CX1763 is an AMPAR allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of AMPAR containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression[1].

IC50 & Target[1]

AMPA Receptor

 

In Vitro

CX1763 (100 μM) acts as a low-impact AMPA receptor positive allosteric modulator in rat brain membranes and neurons, increasing [3H]AMPA binding and peak glutamate-induced currents without intrinsic agonism up to 100 μM, and upregulating calcium-impermeable GluR2(R)-containing receptors[1].

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

In Vivo

CX1763 (10 mg/kg; intravenous injection; single administration) induces a significant and persistent enhancement of approximately 20% in hippocampal fEPSP amplitude in anesthetized rats[1].
CX1763 (1-5 mg/kg; i.p.; single administration) improves specific attention parameters (shortens response latency, reduces premature responses) in the 5CSRTT ADHD rat model at the 5 mg/kg i.p. dose, while increasing omission errors without altering the correct response rate[1].
CX1763 (1-18 mg/kg; i.p.; single administration) dose-dependently reduces amphetamine-induced hyperactivity in mice, with an AD50 of 2 mg/kg, and completely reverses this symptom at 18 mg/kg via intraperitoneal injection[1].

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

Animal Model: Long-Evans (male, 250-350 g)[1]
Dosage: 10 mg/kg
Administration: i.v.; single dose
Result: Significantly potentiated hippocampal fEPSP amplitude by ~20% at 15 minutes post-dose.
Peaked at ~15 minutes post-dose.
Declined to baseline by 100-120 minutes post-dose.
Animal Model: hooded Wistar (male, 250-310 g, 5-Choice Serial Reaction Time Task trained)[1]
Dosage: 1 mg/kg; 5 mg/kg
Administration: i.p.; single dose
Result: Did not significantly alter 5CSRTT parameters at 1 mg/kg.
Significantly decreased correct response latency at 5 mg/kg.
Significantly decreased the percentage of premature responses at 5 mg/kg.
Significantly increased omission errors at 5 mg/kg.
Did not significantly improve the percentage of correct responses at 5 mg/kg.
Animal Model: CD1[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 18 mg/kg
Administration: i.p.; single dose
Result: Dose-dependently reduced amphetamine-induced hyperactivity, with an AD50 of 2 mg/kg.
Significantly reduced hyperactivity at doses of 3-18 mg/kg.
Completely reversed amphetamine-induced hyperactivity to baseline levels at 18 mg/kg.
Molecular Weight

275.30

Formula

C14H17N3O3

CAS No.
SMILES

CN([C@H]1CC[C@@H](CC1)O)C(C2=CC3=NON=C3C=C2)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

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CX1763
Cat. No.:
HY-182631
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