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Biomedical subjects

B Testa

Publications and source records attributed to B Testa.

At least 199 records · Page 11Linked to original sources

A reappraisal of the stereoselective metabolism of nicotine to nicotine-1'-N-oxide.

1. The cis and trans 1'-N-oxide metabolites of (2'R)-(+)-nicotine have the absolute configuration (1'S; 2'R) and (1'R; 2'R), respectively, and not the reverse as previously published. 2. Reinterpretation of metabolic data in the light of this reassignment reveals that N-oxidation of nicotine leads preferentially to the (1'R)-N-oxide, with little dependence on the configuration of the 2'-centre. 3. It is proposed that (2'S)-(-)-nicotine and (2'R)-(+)-nicotine bind to the same enzymic site by two distinct modes of binding; each of these modes involves the more basic centre (in this case the pyrrolidine ring) as the governing binding moiety.

Animals↗

Isomerisation and urinary excretion of proxibarbal and valofan in man; a preliminary study.

Proxibarbal and valofan are tautomeric drugs which interconvert rapidly in solution. In the present study, the urinary excretion of these two drugs was investigated in two subjects after separate oral administration. In both cases, only proxibarbal was found in urine, while the excretion of valofan was negligible or non-detectable. More than half of a dose remains unaccounted for after proxibarbal administration, and more than three quarters after valofan administration. A simple chemical equilibrium of tautomerism as found in vitro is insufficient to account for the excretion kinetics of the two drugs in humans.

Adult↗