1. 3-Mercaptopicolinic acid (SK&F 34288) inhibited gluconeogenesis in vitro, with lactate as substrate, in rat kidney-cortex and liver slices. 2. In perfused rat livers, gluconeogenesis was inhibited when lactate, pyruvate or alanine served as substrate, but not with fructose, suggesting pyruvate carboxylase or phosphoenolpyruvate carboxylase as the site of inhibition. No significant effects were evident in O2 consumption, hepatic glycogen, urea production, or [lactate]/[pyruvate] ratios. 3. A hypoglycaemic effect was evident in vivo in starved and alloxan-diabetic rats, starved guinea pigs and starved mice, but not in 4h-post-absorptive rats. 4. In the starved rat the hypoglycaemia was accompanied by an increase in blood lactate. 5. A trace dose of [14C]lactate in vivo was initially oxidized to a lesser extent in inhibitor-treated rats, but during 90min the total CO2 evolved was slightly greater. The total amount of the tracer oxidized was not significantly different from that in the controls.
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March 1974
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Research Article|
March 01 1974
3-Mercaptopicolinic acid, an inhibitor of gluconeogenesis
N. W. DiTullio;
N. W. DiTullio
1Research and Development Division, Smith Kline and French Laboratories, Philadelphia, Pa. 19101, U.S.A.
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C. E. Berkoff;
C. E. Berkoff
1Research and Development Division, Smith Kline and French Laboratories, Philadelphia, Pa. 19101, U.S.A.
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B. Blank;
B. Blank
1Research and Development Division, Smith Kline and French Laboratories, Philadelphia, Pa. 19101, U.S.A.
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V. Kostos;
V. Kostos
1Research and Development Division, Smith Kline and French Laboratories, Philadelphia, Pa. 19101, U.S.A.
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E. J. Stack;
E. J. Stack
1Research and Development Division, Smith Kline and French Laboratories, Philadelphia, Pa. 19101, U.S.A.
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H. L. Saunders
H. L. Saunders
*
1Research and Development Division, Smith Kline and French Laboratories, Philadelphia, Pa. 19101, U.S.A.
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Publisher: Portland Press Ltd
Online ISSN: 1470-8728
Print ISSN: 0264-6021
© 1974 London: The Biochemical Socity
1974
Biochem J (1974) 138 (3): 387–394.
Citation
N. W. DiTullio, C. E. Berkoff, B. Blank, V. Kostos, E. J. Stack, H. L. Saunders; 3-Mercaptopicolinic acid, an inhibitor of gluconeogenesis. Biochem J 1 March 1974; 138 (3): 387–394. doi: https://doi.org/10.1042/bj1380387
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