Indomethacin → 1,8-Naphthyridin-2(1H)-one, 3-methyl-1-phenyl-

HRID 867506

Reaktionsgleichung

Reaktionsgleichung von HRID 867506
CC(NCC(O)COC1C=CC=[C:13]2[CH:18]=[CH:17][CH:16]=[CH:15][C:14]=12)C.CC1[N:29]([C:30]([C:32]2[CH:33]=CC(Cl)=C[CH:37]=2)=[O:31])[C:28]2[CH:27]=[CH:26][C:25](OC)=[CH:24]C=2C=1CC(O)=O.C[N:46](CCN(C1C=CC=CN=1)CC1C=CC(OC)=CC=1)C>>[CH3:33][C:32]1[C:30](=[O:31])[N:29]([C:13]2[CH:14]=[CH:15][CH:16]=[CH:17][CH:18]=2)[C:28]2[C:27]([CH:37]=1)=[CH:26][CH:25]=[CH:24][N:46]=2

Komponenten

4

Edukt 3

HCID 3715IndomethacinHCID 4946PropranololHCID 4992Pyrilamine

Produkt 1

HCID 30877611,8-Naphthyridin-2(1H)-one, 3-methyl-1-phenyl-

Versuchsvorschrift

The sensitized guinea pigs are injected i.v. with 1 mg/kg propranolol, 5 mg/kg indomethacin and 2 mg/kg mepyramine given together in a volume of 1 ml/kg. Fifteen minutes later the animals are challenged with nebulized ovalbumin. Test compounds are administered orally 2 hours before challenge with ovalbumin. Suppression of anaphylactic bronchospasm is expressed as a percent inhibition of the peak increase in intratracheal pressure by comparison to a vehicle-treated control group. In this procedure, 3-methyl-1-phenyl-1,8-naphthyridin-2(1H)-one (referred to as Compound A hereinafter) provided a 96% inhibition at a dose of 5 mg/kg p.o.

Aufarbeitung

  1. customFifteen minutes
  2. temperatureincrease in intratracheal pressure by comparison to a vehicle-treated control group

Quellen und Nachweise

ORD-Eintrag
ord-07f24219b0c44c7d96307fab4bd33719
Quelldatensatz
uspto-grants-1988_10
Patentnummer
US04775686

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