Genotoxicity of 4-(piperazin-1-yl)-8-(trifluoromethyl)pyrido[2,3-e][1,2,4] triazolo[4,3-a]pyrazine, a Potent H4 Receptor Antagonist for the Treatment of Allergy: Evidence of Glyoxal Intermediate Involvement.

Gunduz, Mithat; Cirello, Amanda L; Klimko, Peter; Dumouchel, Jennifer L; Argikar, Upendra A

Gunduz, Mithat; Cirello, Amanda L; Klimko, Peter; Dumouchel, Jennifer L; Argikar, Upendra A.

Affiliation

Gunduz M; PK Sciences, Global Biotransformation, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, United States.
Cirello AL; PK Sciences, Global Biotransformation, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, United States.
Klimko P; PK Sciences, Global Biotransformation, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, United States.
Dumouchel JL; PK Sciences, Global Biotransformation, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, United States.
Argikar UA; PK Sciences, Global Biotransformation, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, United States.

Drug Metab Lett ; 11(2): 144-148, 2017.

Article in En | MEDLINE | ID: mdl-29110630

Subject(s)

Glyoxal/metabolism; Histamine Antagonists/toxicity; Hypersensitivity/drug therapy; Piperazines/toxicity; Piperazines/therapeutic use; Pyrazines/toxicity; Pyrazines/therapeutic use; Pyridines/toxicity; Pyridines/therapeutic use; Receptors, Histamine H4/antagonists & inhibitors; Triazoles/toxicity; Triazoles/therapeutic use; Animals; Biological Assay; Biotransformation; Histamine Antagonists/chemistry; Histamine Antagonists/metabolism; Mutagenicity Tests; Mutagens/chemistry; Mutagens/metabolism; Mutagens/toxicity; Phenobarbital/pharmacology; Piperazines/chemistry; Piperazines/pharmacology; Pyrazines/chemistry; Pyrazines/pharmacology; Pyridines/chemistry; Pyridines/pharmacology; Rats; Rats, Sprague-Dawley; Triazoles/chemistry; Triazoles/pharmacology; beta-Naphthoflavone/pharmacology

Key words

H4 Receptor; Induced rat liver S9 fractions; genotoxicity; glyoxal; o-phenylenediamine; quinoxaline

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Piperazines / Pyrazines / Pyridines / Triazoles / Receptors, Histamine H4 / Glyoxal / Histamine Antagonists / Hypersensitivity Type of study: Prognostic_studies Limits: Animals Language: En Journal: Drug Metab Lett Journal subject: FARMACOLOGIA / METABOLISMO Year: 2017 Document type: Article Affiliation country: United States Country of publication: United Arab Emirates

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