Inhibition of catechol-O-methyltransferase by n-butyl gallate

Dorris, Roy L.; Dill, Riva

doi:10.1016/0028-3908(77)90034-x

Cited by 6 publications

(2 citation statements)

References 5 publications

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“…These inhibitors include, e.g., pyrogallol and its derivatives, catechol, tropolones, and 3,4-dihydroxy-2-methylpropiophe none (U-0521). Although they appeared to be effec tive, they had poor bioavailability and were usually extremely short acting (Belleau and Burba, 1961;Dorris and Dill, 1977;Ross and Haljasmaa, 1964a). Gallates, catechols, tropolone and its derivatives, and pyrogallol were all tested in vitro and in vivo.…”

Section: First-generation Comt Inhibitorsmentioning

confidence: 99%

“…Catechol itself is highly toxic, inducing again convulsions in the rat after an oral dose of 100 mg/kg (Angel and Rodgers, 1968;Bakke, 1970). 1) are effective COMT inhibitors in vitro and in vivo but have an extremely short duration of action in the rat, only 15-30 min after an intraper itoneal injection (Dorris and Dill, 1977). 1) are effective COMT inhibitors in vitro and in vivo but have an extremely short duration of action in the rat, only 15-30 min after an intraper itoneal injection (Dorris and Dill, 1977).…”

Section: Safety Concerns Of First-generation Agentsmentioning

confidence: 99%

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Toxicology and Safety of Comt Inhibitors

Haasio

2010

International Review of Neurobiology

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Section: First-generation Comt Inhibitorsmentioning

confidence: 99%

Section: Safety Concerns Of First-generation Agentsmentioning

confidence: 99%

Toxicology and Safety of Comt Inhibitors

Haasio

2010

International Review of Neurobiology

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Molecular orbital studies on m- and p-methylation of substituted catechols by catechol O-methyltransferase

Shinagawa

2009

Int. J. Quantum Chem.

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The electronic structures of catechol derivatives, 3,4-dihydroxy-1 -substituted benzenes, including epinephrine and norepinephrine, were calculated by means of CNDO/2 and M IND0/3 methods. Correlation between the ratio (meta:para) of 0-methylated products of catechols catalyzed by catechol 0-methyltransferase and the reaction indices calculated from molecular orbital parameters was found. The regression analysis showed that the electron donative indices at C2 and para 0 position and the electron acceptable index at c 6 position in the catechols by CNDO/2 calculation represented the best correlation with the meta:pam ratio. The correlation coefficient between the mera:para ratio predicted by regression equation and the observed one was 0.900. By means of MIND0/3 calculations. the regression equation from the electron donative indices at Cz. Cq, and c 6 positions in catechols exhibited the correlation coefficient 0.798.

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