Histamine N-methyl transferase: inhibition by drugs.
Identifieur interne : 002E21 ( Main/Exploration ); précédent : 002E20; suivant : 002E22Histamine N-methyl transferase: inhibition by drugs.
Auteurs : G M Pacifici [Italie] ; P. Donatelli ; L. GiulianiSource :
- British journal of clinical pharmacology [ 0306-5251 ] ; 1992.
Descripteurs français
- KwdFr :
- MESH :
- analyse : Histamine N-methyltransferase.
- antagonistes et inhibiteurs : Histamine N-methyltransferase.
- Adulte, Adulte d'âge moyen, Femelle, Humains, Mâle, Répartition dans les tissus, Sujet âgé.
English descriptors
- KwdEn :
- MESH :
- chemical , analysis : Histamine N-Methyltransferase.
- chemical , antagonists & inhibitors : Histamine N-Methyltransferase.
- Adult, Aged, Female, Humans, Male, Middle Aged, Tissue Distribution.
Abstract
1. Histamine N-methyl transferase activity was measured in samples of human liver, brain, kidney, lung and intestinal mucosa. The mean (+/- s.d.) rate (nmol min-1 mg-1 protein) of histamine N-methylation was 1.78 +/- 0.59 (liver, n = 60), 1.15 +/- 0.38 (renal cortex, n = 8), 0.79 +/- 0.14 (renal medulla, n = 8), 0.35 +/- 0.08 (lung, n = 20), 0.47 +/- 0.18 (human intestine, n = 30) and 0.29 +/- 0.14 (brain, n = 13). 2. Inhibition of histamine N-methyl transferase by 15 drugs was investigated in human liver. The IC50 for the various drugs ranged over three orders of magnitude; chloroquine was the most potent inhibitor. 3. The average IC50 values for chloroquine were 12.6, 22.0, 19.0, 21.6 microM in liver, renal cortex, brain and colon, respectively. These values are lower than the Michaelis-Menten constant for histamine N-methyltransferase in liver (43.8 microM) and kidney (45.5 microM). Chloroquine carried a mixed non-competitive inhibition of hepatic histamine N-methyl transferase. Some side-effects of chloroquine may be explained by inhibition of histamine N-methyl transferase.
DOI: 10.1111/j.1365-2125.1992.tb05637.x
PubMed: 1457266
Affiliations:
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Le document en format XML
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Donatelli</name></author><author><name sortKey="Giuliani, L" sort="Giuliani, L" uniqKey="Giuliani L" first="L" last="Giuliani">L. Giuliani</name></author></analytic><series><title level="j">British journal of clinical pharmacology</title><idno type="ISSN">0306-5251</idno><imprint><date when="1992" type="published">1992</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Adult</term><term>Aged</term><term>Female</term><term>Histamine N-Methyltransferase (analysis)</term><term>Histamine N-Methyltransferase (antagonists & inhibitors)</term><term>Humans</term><term>Male</term><term>Middle Aged</term><term>Tissue Distribution</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Adulte</term><term>Adulte d'âge moyen</term><term>Femelle</term><term>Histamine N-methyltransferase (analyse)</term><term>Histamine N-methyltransferase (antagonistes et inhibiteurs)</term><term>Humains</term><term>Mâle</term><term>Répartition dans les tissus</term><term>Sujet âgé</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analysis" xml:lang="en"><term>Histamine N-Methyltransferase</term></keywords><keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Histamine N-Methyltransferase</term></keywords><keywords scheme="MESH" qualifier="analyse" xml:lang="fr"><term>Histamine N-methyltransferase</term></keywords><keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Histamine N-methyltransferase</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Adult</term><term>Aged</term><term>Female</term><term>Humans</term><term>Male</term><term>Middle Aged</term><term>Tissue Distribution</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Adulte</term><term>Adulte d'âge moyen</term><term>Femelle</term><term>Humains</term><term>Mâle</term><term>Répartition dans les tissus</term><term>Sujet âgé</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">1. Histamine N-methyl transferase activity was measured in samples of human liver, brain, kidney, lung and intestinal mucosa. The mean (+/- s.d.) rate (nmol min-1 mg-1 protein) of histamine N-methylation was 1.78 +/- 0.59 (liver, n = 60), 1.15 +/- 0.38 (renal cortex, n = 8), 0.79 +/- 0.14 (renal medulla, n = 8), 0.35 +/- 0.08 (lung, n = 20), 0.47 +/- 0.18 (human intestine, n = 30) and 0.29 +/- 0.14 (brain, n = 13). 2. Inhibition of histamine N-methyl transferase by 15 drugs was investigated in human liver. The IC50 for the various drugs ranged over three orders of magnitude; chloroquine was the most potent inhibitor. 3. The average IC50 values for chloroquine were 12.6, 22.0, 19.0, 21.6 microM in liver, renal cortex, brain and colon, respectively. These values are lower than the Michaelis-Menten constant for histamine N-methyltransferase in liver (43.8 microM) and kidney (45.5 microM). Chloroquine carried a mixed non-competitive inhibition of hepatic histamine N-methyl transferase. Some side-effects of chloroquine may be explained by inhibition of histamine N-methyl transferase.</div></front></TEI><affiliations><list><country><li>Italie</li></country><region><li>Toscane</li></region><settlement><li>Pise</li></settlement><orgName><li>Université de Pise</li></orgName></list><tree><noCountry><name sortKey="Donatelli, P" sort="Donatelli, P" uniqKey="Donatelli P" first="P" last="Donatelli">P. Donatelli</name><name sortKey="Giuliani, L" sort="Giuliani, L" uniqKey="Giuliani L" first="L" last="Giuliani">L. Giuliani</name></noCountry><country name="Italie"><region name="Toscane"><name sortKey="Pacifici, G M" sort="Pacifici, G M" uniqKey="Pacifici G" first="G M" last="Pacifici">G M Pacifici</name></region></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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