CP-283097

CP-283097 is an orally active and conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors[1].

Product Specifications

CAS Number

[138047-56-0]

UNSPSC

12352005

Target

IGluR

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Smiles

O[C@@H]1[C@H](N2CCC(O)(CC2)CC3=CC=CC=C3)COC4=CC(O)=CC=C41

Molecular Formula

C21H25NO4

Molecular Weight

355.43

References & Citations

[1]Butler TW, et al. (3R,4S) -3-[4- (4-fluorophenyl) -4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S) -1- (4-hydroxyphenyl) -2- (4-hydroxy-4-phenylpiperidino) - 1-propanol. J Med Chem. 1998 Mar 26;41 (7) :1172-84.