10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine Property

Boiling point:

320.3±11.0 °C(Predicted)

Density 

1.144±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

insoluble in H2O; ≥10.45 mg/mL in DMSO; ≥102.6 mg/mL in EtOH

form 

oil

pka

7.96±0.40(Predicted)

color 

brown

Hazard and Precautionary Statements (GHS)

10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine Chemical Properties,Usage,Production

Biological Activity

(+)-mk 801 is a potent antagonist of nmda with ki value of 30.5nm [1].mk 801 is a potent anticonvulsant exhibits both anxiolytic and sympathomimetic properties. it is found to be a noncompetitive antagonist of nmda. mk 801 can penetrate into the central nervous system. in the in vitro assay, mk 801 binds to rat cerebral cortical membrane with high affinity in a saturable manner. this binding is reversible even when the concentration of mk 801 is up to 100μm. it is also found that the binding shows a regional specificity. most of these binding sites are located in the hippocampus. in rat cortical-slice preparations, mk 801 causes a potent blockade of depolarizing responses to nmda with a high selectivity. this effect is persistent. the blockade can also cause a suppression of the epileptiform activity induced by tetrodotoxin or other neurotoxin [1].

target

NMDA

References

[1] wong eh, kemp ja, priestley t, knight ar, woodruff gn, iversen ll . the anticonvulsant mk-801 is a potent n-methyl-d-aspartate antagonist. proc natl acad sci u s a. 1986 sep;83(18):7104-8.