199. Inhibition of induced asthma by oral oxarbazole: Controlled dose-ranging data

Falliers, Constantine J.; Mingo, Thomas S.

doi:10.1016/0091-6749(78)90439-6

Cited by 3 publications

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“…Subsequently, the same spasmogen was injected 1, 30 and 60 min after the medication with isoproterenol hydrochloride (Winthrop Laboratories), or disodium cromoglycate (DSCG, Fisons), and 5, 30 min and 1, 2, 3, and 4 h after the medications with bitolterol mesylate (25), aminophylline (Baker), prednisone (Organon), oxarbazole (Sterling-Winthrop, an antagonist of SRS-A and bradykinin) (11,24), thenyldiamine HC1 (an antihista mine, Winthrop Laboratories), or atropine sulfate (Merck).…”

Section: Measurement O F Inhibition O F Bronchoconstriction By Drugsmentioning

confidence: 99%

The Effects of Antiasthmatic Drugs against Immune Complex-Induced Bronchoconstriction in Anesthetized Dogs

Mielens¹

1979

Pharmacology

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Bronchoconstriction was induced in nonsensitized dogs by intravenous injections of soluble immune complexes. Immune complex-induced bronchoconstriction was associated with a drop in blood pressure and a drop in the circulating complement levels. Different antiasthmatic agents were compared for their effects in dogs against bronchoconstriction induced by intravenous injections of immune complexes or histamine. Bronchodilators (isoproterenol, aminophylline, and bitolterol) inhibited both types of bronchoconstriction, whereas disodium cromoglycate, prednisone, and oxarbazole inhibited only bronchoconstriction induced by immune complexes. Thenyldiamine and atropine inhibited histamine- and carbachol-induced bronchoconstriction, respectively, but they were ineffective at the same doses against immune complex-induced bronchoconstriction.

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Section: Measurement O F Inhibition O F Bronchoconstriction By Drugsmentioning

confidence: 99%

The Effects of Antiasthmatic Drugs against Immune Complex-Induced Bronchoconstriction in Anesthetized Dogs

Mielens¹

1979

Pharmacology

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1 The Search for Antiallergic Drugs for the Treatment of Asthma - Problems in Finding a Successor to Sodium Cromoglycate

Suschitzky

Sheard

1985

Progress in Medicinal Chemistry

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Disposition of a Series of Tetrahydrocarbazoles

Edelson

Benziger

1980

Drug Metabolism Reviews

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Cyclindole was extensively metabolized and eliminated primarily via the kidneys from most laboratory animals and man. Only in the dog was cyclindole a major urinary component. Cyclindole was metabolized by N-demethylation and/or hydroxylation. In studies utilizing radiolabeled drug, the primary urinary component was polar material which probably resulted from conjugation of the hydroxylated products. When desmethylcyclindole was administered to rats and dogs, large amounts of unchanged drug were administered to rats and dogs, large amounts of unchanged drug were recovered in the urine; there was no 3-aminotetrahydrocarbazole present. Significant amounts of urinary radioactivity were thought to represent hydroxylated and/or conjugated products. When 7-hydroxycyclindole was administered to dogs, only free parent drug was recovered from the urine; there was no evidence for N-demethylation. Flucindole, the 6,8-difluoro analog of cyclindole was metabolized by dog and man via N-demethylation with the formyl derivative being a probable intermediate in this reaction; both products were found in the urine. No didesmethyl metabolite was detected. In contrast to cyclindole, the N-oxide of flucindole was found in urine from both species. The route of elimination of oxarbazole and its metabolites was species specific: urinary excretion was 96.5, 38.7, 24.5, and 2.0% for the guinea pig, monkey, rat, and dog, respectively. The major urinary metabolite was O-demethyl oxarbazole; this metabolite was conjugated in all species except the guinea pig. The dog and monkey excreted small quantities of conjugated N-debenzoylated oxarbazole in urine. The profound changes in pharmacological activity that result from relatively small chemical modifications of the tetrahydrocarbazole nucleus make it likely that many further investigations of this class of compounds will be undertaken in the future.

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199. Inhibition of induced asthma by oral oxarbazole: Controlled dose-ranging data

Cited by 3 publications

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The Effects of Antiasthmatic Drugs against Immune Complex-Induced Bronchoconstriction in Anesthetized Dogs

The Effects of Antiasthmatic Drugs against Immune Complex-Induced Bronchoconstriction in Anesthetized Dogs

1 The Search for Antiallergic Drugs for the Treatment of Asthma - Problems in Finding a Successor to Sodium Cromoglycate

Disposition of a Series of Tetrahydrocarbazoles

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