Blixeprodil hydrochloride
Based on 1 Customer Validation
Blixeprodil hydrochloride (GM-1020 hydrochloride) is an orally active, blood-brain barrier-penetrant NMDA receptor inhibitor with a Ki of 3.25 µM in rat cortical tissues. Blixeprodil hydrochloride binds to the MK-801 ion channel site and blocks NMDA receptor-mediated currents in hyperpolarized states in a voltage-dependent manner. Blixeprodil hydrochloride modulates the power of cortical EEG frequency bands, alters spontaneous motor activity, and induces ataxia at high doses. Blixeprodil hydrochloride can be used in the research of depression.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3048183-44-1
- Formule: C13H17ClFNO
- Masse moléculaire:257.73
-
Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform iGluR
More
Activité biologique
Blixeprodil (GM-1020) hydrochloride binds to NMDA receptors in rat brain homogenates with a Ki value of 3.25 µM[1].
Blixeprodil hydrochloride inhibits the functional activities of both NR1/NR2A and NR1/NR2B NMDA receptors in Xenopus laevis oocytes with similar potency, with IC50 values of 3.70 µM and 4.16 µM, respectively[1].
Blixeprodil hydrochloride inhibits NR1/2A NMDA receptor-mediated currents in HEK293 cells with an IC50 of 1.192 µM, and blocks the receptor in a voltage-dependent manner;
Blixeprodil hydrochloride binds to the human μ-opioid receptor in transfected HEK cells, with a Ki value of 19 µM[1].
Blixeprodil hydrochloride exhibits selective binding to NMDA receptors across a broad panel of off-targets, with weak binding affinity for the serotonin transporter (Ki = 6.2 µM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Blixeprodil (0.75-9 mg/kg; i.p.; weekly; 5 weeks) hydrochloride reverses CMS-induced depressive-like phenotypes in rats at doses ≥1.5 mg/kg i.p., with effects durable for up to 15 days after the final weekly dose[1].
Blixeprodil (1.5-9 mg/kg; i.p.; single dose; 1-10 mg/kg; p.o.; single dose) hydrochloride restores CMS-induced anhedonia in rats for up to 14 days post-dose[1].
Blixeprodil (1-32 mg/kg; s.c.; single dose) hydrochloride produces motor impairment in rats and mice only at doses ≥ 10 mg/kg s.c., with a 12-fold separation between efficacious plasma exposures for antidepressant-like effects and those causing ataxia in rats[1].
Blixeprodil (1-10 mg/kg; s.c.; single dose) hydrochloride produces dose-dependent changes in rat cortical EEG indicative of NMDA receptor target engagement[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 3048183-44-1
-
Appearance Solid
-
Masse moléculaire 257.73
-
Formule C13H17ClFNO
-
SMILES
CN[C@]1(C2=CC=C(C=C2)F)C(CCCC1)=O.Cl
-
Synonyms
GM-1020 hydrochloride
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Blixeprodil hydrochloride Related Classifications
HY-172419A Related Classifications
Powered by Bioz