General description
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 (Ki = 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 (Ki = 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 Actions
Primary Target
NMDA receptors
Target IC50: 1, >100, and >100 →M for NR2B, NR2A, and NR2C, respectively.
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51131635
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5045390001
