5.04539

Eliprodil

• Synonyme(s) : Eliprodil, α-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperidineethanol, NMDA Antagonist IX
• Formule empirique (notation de Hill): C₂₀H₂₃ClFNO
• Numéro CAS: 119431-25-3
• Poids moléculaire : 347.85
• Numéro MDL: MFCD00866651
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥99% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 17 mg/mL
• Température de stockage: 2-8°C
• InChI: 1S/C20H23ClFNO/c21-18-5-3-17(4-6-18)20(24)14-23-11-9-16(10-12-23)13-15-1-7-19(22)8-2-15/h1-8,16,20,24H,9-14H2
• Clé InChI: GGUSQTSTQSHJAH-UHFFFAOYSA-N

Description

Description générale

A negative allosteric modulator selective for NR2B containing NMDA receptors (IC₅₀ = 1, >100, and >100 µM for NR2B, NR2A, and NR2C, respectively). Also a potent ligand for α1 receptor (K_i = 0.013 µM), one of the two types of unique non-opioid, non-phencyclidine brain α receptors. Blocks neuronal voltage-gated Ca2⁺

A negative allosteric modulator selective for NR2B containing NMDA receptors (IC₅₀ = 1, >100, and >100 µM for NR2B, NR2A, and NR2C, respectively). Also a potent ligand for ς1 receptor (K_i = 0.013 µM), one of the two types of unique non-opioid, non-phencyclidine brain ς receptors. Blocks neuronal voltage-gated Ca2+ channels and selectively inhibits the rapid component of the delayed rectifier K+ current (IKr). A neuroprotective agent in acute ischemic stroke. Prolongs the QT interval in EKG.

Actions biochimiques/physiologiques

Primary Target
NMDA receptors

Target IC₅₀: 1, >100, and >100 →M for NR2B, NR2A, and NR2C, respectively.

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Lengyel, C., et al. 2004. Br. J. Pharmacol.143, 152.

Nikam, S., et al. 2002. Curr Pharm Des.8, 845.Whittemore, E., et al. 1997. J. Pharmacol. Exp. Ther.282, 326.M
Bath, C., et al. 1996. Eur. J. Pharmacol.299, 103.
Carter, C., et al. 1994. Neuropsychopharmacol.11, 257.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable