2. Membrane Transporter/Ion Channel Neuronal Signaling
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  4. R-(+)-EU-1180-453

R-(+)-EU-1180-453 is a positive allosteric modulator targeting NMDA receptors containing GluN2C and GluN2D subunits, with a pEC50 value of 5.5 for both rat receptor subtypes, and it can cross the blood-brain barrier. R-(+)-EU-1180-453 increases the potency of glutamate, enhances receptor responses to maximally effective concentrations of agonists, and acts only on receptors bound to both co-agonists. R-(+)-EU-1180-453 is applicable to research related to Alzheimer's disease, Parkinson's disease, epilepsy, and neuropathic pain.

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R-(+)-EU-1180-453

R-(+)-EU-1180-453 Chemical Structure

CAS No. : 2488764-06-1

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R-(+)-EU-1180-453 Related Antibodies

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Description

R-(+)-EU-1180-453 is a positive allosteric modulator targeting NMDA receptors containing GluN2C and GluN2D subunits, with a pEC50 value of 5.5 for both rat receptor subtypes, and it can cross the blood-brain barrier. R-(+)-EU-1180-453 increases the potency of glutamate, enhances receptor responses to maximally effective concentrations of agonists, and acts only on receptors bound to both co-agonists. R-(+)-EU-1180-453 is applicable to research related to Alzheimer's disease, Parkinson's disease, epilepsy, and neuropathic pain[1].

In Vitro

R-(+)-EU-1180-453 (30 μM; concentrations for concentration−effect curves) potentiates GluN1/GluN2C and GluN1/GluN2D NMDA receptors expressed in Xenopus laevis oocytes with a pEC50 of 5.5, maximal potentiation of 410% and 390% respectively, and a p(doubling concentration) of 5.9 and 5.8 respectively[1].

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

R-(+)-EU-1180-453 Related Antibodies
In Vivo

EU-1180-453 (10 mg/kg; i.p.; single dose) is brain-penetrant in male C57BL/6 mice, achieving a brain:plasma AUC0-t ratio of 1.4 ± 0.5 after a single 10 mg/kg i.p. dose, with a plasma half-life of 1.07 ± 0.04 hours[1].

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

Animal Model: C57BL/6 (male, 6-8 weeks of age, fed)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
Result: Reached peak plasma concentration of 695 ng/mL (1.83 μM) at 0.25 hours post-dosing.
Reached peak brain concentration of 962 ng/mL (2.5 μM) at 0.25 hours post-dosing.
Achieved a brain:plasma AUC_LAST ratio of 1.4.
Exhibited a plasma half-life (t1/2) of 1.07 hours.
Showed plasma protein binding of 98.7% bound at 1 μM, with 1.3% free fraction.
Molecular Weight

380.42

Formula

C22H21FN2O3
CAS No.
SMILES

C(OC1=CC=C(OC)C=C1)[C@H]2C=3N(CC(=O)N2CC4=CC(F)=CC=C4)C=CC3
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Purity & Documentation
References
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R-(+)-EU-1180-453 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

R-(+)-EU-1180-4532488764-06-1iGluRIonotropic glutamate receptorsschizophreniaepilepsyhuntington’s choreaXenopus laevis oocytesmale C57BL/6 miceNMDA receptorsGluN2C-containing NMDA receptorsparkinson’s diseaseGluN2D-containing NMDA receptorsalzheimer’s diseaseInhibitorinhibitorinhibit

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