✦ LIBER ✦

Stereoselective inhibition by chloroquine of histamine N-methyltransferase in the human liver and brain

✍ Scribed by P. Donatelli; G. Marchi; G. M. Pacifici; L. Giuliani; L. L. Gustafsson

Publisher: Springer
Year: 1994
Tongue: English
Weight: 421 KB
Volume: 47
Category: Article
ISSN: 0031-6970
DOI: 10.1007/bf00191166

No coin nor oath required. For personal study only.

✦ Synopsis

This study was designed to determine whether both enantiomers of chloroquine inhibit histamine N-methyltransferase. The mean estimates of ICs0 for the d-and/-enantiomers of chloroquine were 4.9 and 17.8 ~tM (liver), respectively and 6.9 and 21.6 ~tM (brain), respectively. K i estimates were significantly lower with d-than with/-chloroquine; hence, d-chloroquine interacts with the enzyme more effectively than /-chloroquine. If the adverse effects of chloroquine are due to the inhibition of histamine N-methyltransferase, therapy with the/-enantiomer might have lower toxicity. The residual activity of histamine N-methyltransferase should reflect both the degree of inhibition by chloroquine and the level of enzyme expression. The rate of histamine methylation was measured in 100 human liver samples and its range and fold of variation were 29 % and threefold, respectively.

Susceptibility to chloroquine should be greater in subjects with limited expression of histamine N-methyltransferase.

📜 SIMILAR VOLUMES

In vitro inhibition of the activation of

In vitro inhibition of the activation of the human complement and coagulation systems by chloroquine

✍ V.D. Ramanathan; U. Sengupta 📂 Article 📅 1985 🏛 Elsevier Science 🌐 English ⚖ 359 KB

Inactivation of phosphatidylethanolamine

Inactivation of phosphatidylethanolamine N-methyltransferase-2 in aflatoxin-induced liver cancer and partial reversion of the neoplastic phenotype by PEMT transfection of hepatoma cells

✍ Luciana Tessitore; Eliana Sesca; Dennis E. Vance 📂 Article 📅 2000 🏛 John Wiley and Sons 🌐 French ⚖ 131 KB

Phosphatidylethanolamine N-methyltransferase(PEMT) is an enzyme in liver that catalyzes the stepwise methylation of phosphatidylethanolamine to phosphatidylcholine, in addition to the main pathway that synthesizes phosphatidylcholine directly from choline. We have reported that PEMT is permanently i

Measurement of N-acetylaspartylglutamate

Measurement of N-acetylaspartylglutamate in the human frontal brain by 1H-MRS at 7 T

✍ Changho Choi; Subroto Ghose; Jinsoo Uh; Aditya Patel; Ivan E. Dimitrov; Hanzhang 📂 Article 📅 2010 🏛 John Wiley and Sons 🌐 English ⚖ 262 KB

## Abstract __N__‐Acetylaspartylglutamate in human brain has been measured with difference editing at 7 T. The CH~2~ proton resonances (∼2.5 ppm) of the aspartyl groups of __N__‐acetylaspartylglutamate and __N__‐acetylaspartate were difference edited (MEGA) using 20‐msec gaussian radiofrequency pul

The fate of trace elements in the brain,

The fate of trace elements in the brain, muscles and liver, as shown by the results of sinusostomy and angiostomy during stimulation and inhibition of the central nervous system

✍ V. R. Soroka 📂 Article 📅 1959 🏛 Springer US 🌐 English ⚖ 465 KB

Regulation of liver and brain hexose mon

Regulation of liver and brain hexose monophosphate dehydrogenases by insulin and dietary intake in the female rat

✍ Ralph N. Martins; Gilbert B. Stokes; Colin L. Masters 📂 Article 📅 1986 🏛 Springer 🌐 English ⚖ 492 KB

Transcriptional inhibition of stromelysi

Transcriptional inhibition of stromelysin by interferon-γ in normal human fibroblasts is mediated by the AP-1 domain

✍ Martyn Lewis; Edward P. Amento; Elaine N. Unemori 📂 Article 📅 1999 🏛 John Wiley and Sons 🌐 English ⚖ 224 KB 👁 1 views

The expression of the major matrix-degrading metalloproteinase, stromelysin (SL), is modulated by a variety of cytokines and growth factors. Interferon-gamma (IFN-gamma) is a potent modulator of SL expression, either inhibiting or activating expression in a cell-specific manner. We have investigated