Disposition and metabolism of NY-198 V. Metabolism of 14c-ny-198 in rats and dogs

Osamu Nagata; Takehisa Yamada; Toshiaki Yamaguchi; Hiromichi Hasegawa; Eiichi Okezaki; Tetsuya Terasaki; Akira Tsuji

doi:10.11250/chemotherapy1953.36.Supplement2-Base_174

Disposition and metabolism of NY-198 V. Metabolism of ¹⁴c-ny-198 in rats and dogs

Osamu Nagata, Takehisa Yamada, Toshiaki Yamaguchi, Hiromichi Hasegawa, Eiichi Okezaki, Tetsuya Terasaki, Akira Tsuji

PHA - Life and Pharmaceutical Science

Research output: Contribution to journal › Article › peer-review

16 Citations (Scopus)

Abstract

We studied metabolism of ¹⁴C-NY-198 in rats and dogs following oral administration of the drug. The metabolites of NY-198 in rat urine were identified as follows: M-I, unchanged NY-198; M-II, glucuronic acid conjugate of NY-198; M-IV and M-V, compounds cleaved at the piperazine ring; M-III and M-VI, compounds further metabolized through oxidative dealkylation of M-IV and M-V. In serum and urine of rats and dogs, mainly M-I was found, and amounted to more than 80% of the metabolites in these samples. The major metabolite in rat bile was M-II, followed by M-I. These results indicate that metabolism of NY-198 hardly occurs and that most of the drug remains unchanged in rats and dogs.

Original language	English
Pages (from-to)	174-187
Number of pages	14
Journal	Chemotherapy
Volume	36
DOIs	https://doi.org/10.11250/chemotherapy1953.36.Supplement2-Base_174
Publication status	Published - 1988

ASJC Scopus subject areas

Pharmacology (medical)
Infectious Diseases
Pharmacology
Drug Discovery
Oncology

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.11250/chemotherapy1953.36.Supplement2-Base_174

Cite this

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title = "Disposition and metabolism of NY-198 V. Metabolism of 14c-ny-198 in rats and dogs",

abstract = "We studied metabolism of 14C-NY-198 in rats and dogs following oral administration of the drug. The metabolites of NY-198 in rat urine were identified as follows: M-I, unchanged NY-198; M-II, glucuronic acid conjugate of NY-198; M-IV and M-V, compounds cleaved at the piperazine ring; M-III and M-VI, compounds further metabolized through oxidative dealkylation of M-IV and M-V. In serum and urine of rats and dogs, mainly M-I was found, and amounted to more than 80% of the metabolites in these samples. The major metabolite in rat bile was M-II, followed by M-I. These results indicate that metabolism of NY-198 hardly occurs and that most of the drug remains unchanged in rats and dogs.",

author = "Osamu Nagata and Takehisa Yamada and Toshiaki Yamaguchi and Hiromichi Hasegawa and Eiichi Okezaki and Tetsuya Terasaki and Akira Tsuji",

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T1 - Disposition and metabolism of NY-198 V. Metabolism of 14c-ny-198 in rats and dogs

AU - Nagata, Osamu

AU - Yamada, Takehisa

AU - Yamaguchi, Toshiaki

AU - Hasegawa, Hiromichi

AU - Okezaki, Eiichi

AU - Terasaki, Tetsuya

AU - Tsuji, Akira

PY - 1988

Y1 - 1988

N2 - We studied metabolism of 14C-NY-198 in rats and dogs following oral administration of the drug. The metabolites of NY-198 in rat urine were identified as follows: M-I, unchanged NY-198; M-II, glucuronic acid conjugate of NY-198; M-IV and M-V, compounds cleaved at the piperazine ring; M-III and M-VI, compounds further metabolized through oxidative dealkylation of M-IV and M-V. In serum and urine of rats and dogs, mainly M-I was found, and amounted to more than 80% of the metabolites in these samples. The major metabolite in rat bile was M-II, followed by M-I. These results indicate that metabolism of NY-198 hardly occurs and that most of the drug remains unchanged in rats and dogs.

AB - We studied metabolism of 14C-NY-198 in rats and dogs following oral administration of the drug. The metabolites of NY-198 in rat urine were identified as follows: M-I, unchanged NY-198; M-II, glucuronic acid conjugate of NY-198; M-IV and M-V, compounds cleaved at the piperazine ring; M-III and M-VI, compounds further metabolized through oxidative dealkylation of M-IV and M-V. In serum and urine of rats and dogs, mainly M-I was found, and amounted to more than 80% of the metabolites in these samples. The major metabolite in rat bile was M-II, followed by M-I. These results indicate that metabolism of NY-198 hardly occurs and that most of the drug remains unchanged in rats and dogs.

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