Tris(hydroxymethyl)aminomethane → 2,8-Di-benzylaminoadenosine

HRID 2216273

Reaktionsgleichung

Reaktionsgleichung von HRID 2216273
[3H]CCC(N1C(=O)N(C(CC[3H])[3H])C(=O)C2N[C:10]([CH:12]3[CH2:16][CH2:15][CH2:14][CH2:13]3)=[N:11]C1=2)[3H].P(O[CH2:40][C@H]1O[C@@H](N2C3N=C(N)NC(=O)C=3N=C2)[C@H](O)[C@@H]1O)(OP(OP(O)(O)=O)(O)=O)(=O)O.[C@@H:59]1([N:68]2[C:77]3[N:76]=[CH:75][N:74]=[C:72]([NH2:73])[C:71]=3[N:70]=[CH:69]2)[O:67][C@H:64]([CH2:65][OH:66])[C@@H:62]([OH:63])[C@H:60]1[OH:61].C(O)C(N)(CO)CO.CNC([C@H]1O[C@@H](N2C3N=CN=C([NH:104][CH2:105][C:106]4[CH:111]=[CH:110][C:109](N)=[C:108]([125I])[CH:107]=4)C=3N=C2)[C@H](O)[C@@H]1O)=O>>[CH2:105]([NH:104][C:75]1[N:74]=[C:72]([NH2:73])[C:71]2[N:70]=[C:69]([NH:11][CH2:10][C:12]3[CH:16]=[CH:15][CH:14]=[CH:13][CH:40]=3)[N:68]([C:77]=2[N:76]=1)[C@@H:59]1[O:67][C@H:64]([CH2:65][OH:66])[C@@H:62]([OH:63])[C@H:60]1[OH:61])[C:106]1[CH:111]=[CH:110][CH:109]=[CH:108][CH:107]=1

Komponenten

6

Edukt 5

HCID 6503Tris(hydroxymethyl)aminomethaneHCID 60961Adenosine2×HCID 53319341[3H]DpcpxHCID 73754993[125I]AB-MecaHCID 135398633Guanosine Triphosphate

Produkt 1

HCID 695382212,8-Di-benzylaminoadenosine

Versuchsvorschrift

Measurements with [3H]DPCPX in the absence of GTP were performed according to a protocol published previously.30 Adenosine A2A receptor affinities were determined according to Gao et al.31 Adenosine A3 receptor affinities were determined essentially as described.28,29 Briefly, assays were performed in 50/10/1 buffer (50 mM Tris/10 mM MgCl2/1 mM ethylenediaminetetra-acetic acid (EDTA) and 0.01% 3-([3-cholamidopropyl]-dimethylammonio)-1-propanesulfonate (CHAPS)) in glass tubes and contained 50 μl of a HEK 293 cell membrane suspension (10–30 μg), 25 μL [125I]AB MECA (final concentration 0.15 nM), and 25 μl of ligand. Incubations were carried out for 1 hr at 37° C. and were terminated by rapid filtration over Whatman GF/B filters, using a Brandell cell harvester (Brandell, Gaithersburg, Md.). Tubes were washed three times with 3 ml of buffer. Radioactivity was determined in a Beckman 5500B γ-counter. Nonspecific binding was determined in the presence of 10−5 M R-PIA.

Aufarbeitung

  1. customwere terminated by rapid filtration over Whatman GF/B filters
  2. washTubes were washed three times with 3 ml of buffer

Quellen und Nachweise

ORD-Eintrag
ord-8c6dd28e39854d4fa40e1af56d589cee
Quelldatensatz
uspto-grants-2006_09
Patentnummer
US07112574B2

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