2-(2-Furanyl)-7-(2-phenylethyl)-7H-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidin-5-amine → Adenosine

HRID 2219069

Reaktionsgleichung

Reaktionsgleichung von HRID 2219069
CCN[C:4]([C@H:6]1[O:10][C@@H:9]([N:11]2[C:15]3[N:16]=[CH:17][N:18]=[C:19]([NH2:20])[C:14]=3[N:13]=[CH:12]2)[C@H:8]([OH:21])[C@@H:7]1[OH:22])=[O:5].C1C=CC(CCN2N=CC3C4N(C(N)=NC2=3)N=C(C2OC=CC=2)N=4)=CC=1.[3H]CCC(N1C(=O)N(C(CC[3H])[3H])C(=O)C2NC(C3CCCC3)=NC1=2)[3H]>>[C@@H:9]1([N:11]2[C:15]3[N:16]=[CH:17][N:18]=[C:19]([NH2:20])[C:14]=3[N:13]=[CH:12]2)[O:10][C@H:6]([CH2:4][OH:5])[C@@H:7]([OH:22])[C@H:8]1[OH:21]

Komponenten

4

Edukt 3

HCID 1764082-(2-Furanyl)-7-(2-phenylethyl)-7H-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidin-5-amineHCID 448222Neca2×HCID 53319341[3H]Dpcpx

Produkt 1

HCID 60961Adenosine

Versuchsvorschrift

Perform assays in deep well 96 well plates. Total assay volume is 200 μl. Add 50 μl compound dilution buffer (total ligand binding) or 50 μl CGS 15923 working solution (A2a non-specific binding) or 50 μl NECA working solution (A1 non-specific binding) or 50 μl of drug working solution. Add 50 μl ligand stock ([3H]-SCH 58261 for A2a, [3H]-DPCPX for A1). Add 100 μl of diluted membranes containing the appropriate receptor. Mix. Incubate at room temperature for 90 minutes. Harvest using a Brandel cell harvester onto Packard GF/B filter plates. Add 45 μl Microscint 20 (Packard), and count using the Packard TopCount Microscintillation Counter. Determine IC50 values by fitting the displacement curves using an iterative curve fitting program (Excel). Determine Ki values using the Cheng-Prusoff equation.

Aufarbeitung

  1. additionAdd 100 μl of diluted membranes
  2. additioncontaining the appropriate receptor
  3. additionMix
  4. filtrationfilter plates
  5. additionAdd 45 μl Microscint 20 (Packard), and count

Quellen und Nachweise

ORD-Eintrag
ord-f5a84f56fd9649cc8aeb39eb4fb00ebd
Quelldatensatz
uspto-grants-2008_08
Patentnummer
US07414058B2

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