10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine
10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine Basic information
- Product Name:
- 10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine
- Synonyms:
-
- 10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine
- 5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine
- 5-Methyl-5,11-epimino-10,11-dihydro-5H-dibenzo[a,d]cycloheptene
- 5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-
- (+)-MK 801
- 5-Methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene
- Dizocilpinum,Dizocilpina,10,11-dihydro-5-methyl-5H-dibenzocyclohepten-5,10-imine,DIZOCILPINE
- ">cyclohepten-5,10-imine,DIZOCILPINE
- CAS:
- 70449-94-4
- MF:
- C16H15N
- MW:
- 221.3
- EINECS:
- 274-609-7
- Mol File:
- 70449-94-4.mol
10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine Chemical Properties
- 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
- InChI
- InChI=1S/C16H15N/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16/h2-9,15,17H,10H2,1H3
- InChIKey
- LBOJYSIDWZQNJS-UHFFFAOYSA-N
- SMILES
- C12=CC=CC=C1C1(C)NC(C2)C2=CC=CC=C12
10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine Usage And Synthesis
Uses
(Rac)-Dizocilpine ((Rac)-MK-801) is the racemate of Dizocilpine (HY-15084B). Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist[1].
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.
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