5.04539

Eliprodil

• Synonym(e): Eliprodil, α-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperidineethanol, NMDA Antagonist IX
• Empirische Formel (Hill-System): C₂₀H₂₃ClFNO
• CAS-Nummer: 119431-25-3
• Molekulargewicht: 347.85
• MDL-Nummer: MFCD00866651
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥99% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white
• Löslichkeit: DMSO: 17 mg/mL
• Lagertemp.: 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
• InChIKey: GGUSQTSTQSHJAH-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Primary Target
NMDA receptors

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

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable