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Biomedical subjects

A Isimer

Publications and source records attributed to A Isimer.

23 records · Page 2Linked to original sources
PubMed1990

Sulphamethoxazole acetylation in fast and slow acetylators.

Acetylation of sulphamethoxazole was studied in 22 subjects previously phenotyped with sulphadimidine. Sulphamethoxazole and its acetylated metabolite were measured in 6 h plasma and 0-6 h urine samples. Percentage of plasma acetylated-sulphamethoxazole did not correlate with the percentage of urinary acetylated-sulphamethoxazole. There was also no correlation between the percentage of acetylated-sulphadimidine and percentage of acetylated-sulphamethoxazole in plasma. The finding suggest that the acetylation of sulphamethoxazole has no predictive value in determining acetylator status.

Acetylation↗
PubMedDate not supplied

Omission of the deconjugation step in urine analysis and the unaltered outcome of CYP2D6 phenotyping with dextromethorphan.

The present study was aimed at determining whether the deconjugation step in chemical analysis could be omitted without altering the outcome of phenotyping CYP2D6 with dextromethorphan. This drug and its metabolite, dextrorphan, were assayed by high-performance liquid chromatography (HPLC) in urine. Urinary levels of dextromethorphan and dextrorphan with and without enzymatic (beta-glucuronidase) treatment of urine and the metabolic ratios for dextromethorphan were determined in 45 subjects. Although the enzymatic treatment did not alter the urinary concentration of dextromethorphan in both phenotypes, it increased the urinary concentration of dextrorphan in both poor and extensive metabolizers by 3.7- and 12.8-fold, respectively. A urinary unconjugated dextromethorphan/unconjugated dextrorphan metabolic ratio of 2.00 and a total dextromethorphan/total dextrorphan metabolic ratio of 0.30, respectively, identified three poor metabolizers. Enzymatic treatment decreased the urinary antimode value. Moreover, the urinary metabolic ratio based on unconjugated dextrorphan and dextromethorphan correlated well with that based on assay of total dextrorphan and dextromethorphan (rs = 0.9458, P < 0.001). The results show that urinary analysis of dextrorphan and dextromethorphan omitting the enzymatic deconjugation step is a fast, reliable and sensitive method and could be used for studying CYP2D6 type genetic polymorphism in man.

Adolescent↗
PubMedDate not supplied

Synthesis and antinociceptive activity of some 3-substituted benzothiazolone derivatives.

Thirteen 3-substituted benzothiazolone derivatives have been synthesized. Their chemical structures have been elucidated by IR and NMR spectral data and by elemental analyses. Among these compounds, 1-¿3-[2(3H)-benzothiazolon-3-yl[propanoyl]morpholine (5b); 1-¿3-[2(3H)-benzothiazolon-3-yl[propanoyl]-4-benzylpiperidine++ + (5c); 1-¿3-[2(3H)-benzothiazolon-3-yl[-propanoyl]-4-phenylpiperazine (5d); 3-[3-(4-benzylpiperidine-1-yl)propyl]-2(3H)-benzothiazolone (5k); 3-[3-(4-benzylpiperazine-1-yl)propyl]-2(3H)-benzothiazolone (5I); 3-[3-(4-phenylpiperazine-1-yl)propyl]-2(3H)-benzothiazolone (5m) have been found to be significantly more active than the others.

Analgesics, Non-Narcotic↗