10,11-Dihydro-5-methyl-5H-dibenzo(a,d)cyclohepten-5,10-imine → Dizocilpine

HRID 1646093Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1646093
[CH3:1][C:2]12[C:17]3[C:12](=[CH:13][CH:14]=[CH:15][CH:16]=3)[CH:10]([NH:11]1)[CH2:9][C:8]1[C:3]2=[CH:4][CH:5]=[CH:6][CH:7]=1.CCC(COC(C(N(CC[NH+](C)C)C)=O)(C1C=CC=CC=1)C1C=CC=CC=1)CC.[Cl-]>>[CH3:1][C@:2]12[C:17]3[CH:16]=[CH:15][CH:14]=[CH:13][C:12]=3[C@H:10]([NH:11]1)[CH2:9][C:8]1[CH:7]=[CH:6][CH:5]=[CH:4][C:3]2=1

Komponenten

3

Edukt 2

HCID 120710,11-Dihydro-5-methyl-5H-dibenzo(a,d)cyclohepten-5,10-imineHCID 19153X 100

Produkt 1

HCID 180081Dizocilpine

Versuchsvorschrift

[3H]MK-801 binding was performed using Triton X-100 washed synaptic plasma membranes (SPM) prepared from rat forebrain (30-45 day old, male Sprague-Dawley; Sasco, St. Charles, MO) as described previously [J. W. Thomas, W. F. Hood, J. B. Monahan, P. C. Contreras and T. L. O'Donohue, Brain Res., 442, 396-398 (1988)]. The assay was initiated by the addition of SPM (0.20-0.30 mg) to an incubation containing 2.0 nM [3H]MK-801 (15 Ci/mmole; New England Nuclear, Boston, MA) and various concentrations of the appropriate test compound in a total volume of 0.5 ml (all additions were made in 50mM Tris/acetate buffer, pH 7.4) and continued for 120 min at 25° C. The samples were then filtered through glass fiber filters (Schleicher and Schuell #32) which were pretreated with 0.05% (v/v) polyethylenimine. The filters were washed and the radioactivity quantitated by liquid scintillation spectrometry. Inhibition of [3H]MK-801 binding was measured as a decrease in specific basal binding (basal binding=2583 ±381 DPM) with nonspecific binding as the residual binding in the presence of 60 μM MK-801 (562 ±30 DPM). The IC50 values for the inhibition of [3H]MK-801 binding were determined using a logit-log analysis and are reported in Table III, below.

Aufarbeitung

  1. customprepared from rat forebrain (30-45 day old, male Sprague-Dawley; Sasco, St. Charles, MO)
  2. additionThe assay was initiated by the addition of SPM (0.20-0.30 mg) to an incubation
  3. additioncontaining
  4. concentration2.0 nM [3H]MK-801 (15 Ci/mmole; New England Nuclear, Boston, MA) and various concentrations of the appropriate test compound in a total volume of 0.5 ml (all additions were made in 50mM Tris/acetate buffer, pH 7.4)
  5. filtrationThe samples were then filtered through glass fiber filters (Schleicher and Schuell #32) which
  6. washThe filters were washed

Quellen und Nachweise

ORD-Eintrag
ord-ed5341fe21814547ba5b05068fec2fea
Quelldatensatz
uspto-grants-1993_01
Patentnummer
US05177240

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