Inhibition of a type B monoamine oxidase inhibitor, (E)-2-(4-fluorophenethyl)-3-fluoroallylamine (MDL-72974A), on semicarbazide-sensitive amine oxidases isolated from vascular tissues and sera of different species
Identifieur interne : 004572 ( Main/Exploration ); précédent : 004571; suivant : 004573Inhibition of a type B monoamine oxidase inhibitor, (E)-2-(4-fluorophenethyl)-3-fluoroallylamine (MDL-72974A), on semicarbazide-sensitive amine oxidases isolated from vascular tissues and sera of different species
Auteurs : Peter H. Yu [Canada] ; Dong-Mei Zuo [Canada]Source :
- Biochemical Pharmacology [ 0006-2952 ] ; 1992.
English descriptors
Abstract
(E)-2-(4-Fluorophenethyl)-3-fluoroallylamine hydrochloride (MDL-72974A) has been discovered recently to be a very potent and highly selective type B monoamine oxidase inhibitor. We have found that this inhibitor is also capable of inhibiting semicarbazide-sensitive amine oxidases (SSAOs) obtained from vascular tissues and sera of different species. The inhibition of SSAO by MDL-72974A was irreversible and time dependent. It was competitive without preincubation of the enzyme with the inhibitor and demonstrated a mixed-type of inhibition when the enzyme was preincubated with the inhibitor. The ic50 values were estimated to be 2 × 10−9 M, 5 × 10−9 M, 8 × 10−8 M and 2 × 10−9 M for SSAO from dog aorta, rat aorta, bovine aorta and human umbilical artery, respectively. SSAO obtained from bovine serum was relatively insensitive to MDL-72974A (ic50 = 3 × 10−7M. Following intraperitoneal administration of MDL-72974A, rat brain MAO-B was inhibited with the ed50 value being about 0.2 mg/kg. Rat aorta SSAO was also inhibited and to a similar extent by the same dose. MDL-72974A is the most potent SSAO inhibitor that has been described thus far.
Url:
DOI: 10.1016/0006-2952(92)90293-R
Affiliations:
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Yu</name><affiliation wicri:level="1"><country xml:lang="fr">Canada</country><wicri:regionArea>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0</wicri:regionArea><wicri:noRegion>S7N 0W0</wicri:noRegion></affiliation></author><author><name sortKey="Zuo, Dong Mei" sort="Zuo, Dong Mei" uniqKey="Zuo D" first="Dong-Mei" last="Zuo">Dong-Mei Zuo</name><affiliation wicri:level="1"><country xml:lang="fr">Canada</country><wicri:regionArea>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0</wicri:regionArea><wicri:noRegion>S7N 0W0</wicri:noRegion></affiliation></author></analytic><monogr></monogr><series><title level="j">Biochemical Pharmacology</title><title level="j" type="abbrev">BCP</title><idno type="ISSN">0006-2952</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="1992">1992</date><biblScope unit="volume">43</biblScope><biblScope unit="issue">2</biblScope><biblScope unit="page" from="307">307</biblScope><biblScope unit="page" to="312">312</biblScope></imprint><idno type="ISSN">0006-2952</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0006-2952</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>BSAO</term><term>BZ</term><term>MAO</term><term>MDL-72974A</term><term>PLP</term><term>PQR</term><term>SSAO</term></keywords></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">(E)-2-(4-Fluorophenethyl)-3-fluoroallylamine hydrochloride (MDL-72974A) has been discovered recently to be a very potent and highly selective type B monoamine oxidase inhibitor. We have found that this inhibitor is also capable of inhibiting semicarbazide-sensitive amine oxidases (SSAOs) obtained from vascular tissues and sera of different species. The inhibition of SSAO by MDL-72974A was irreversible and time dependent. It was competitive without preincubation of the enzyme with the inhibitor and demonstrated a mixed-type of inhibition when the enzyme was preincubated with the inhibitor. The ic50 values were estimated to be 2 × 10−9 M, 5 × 10−9 M, 8 × 10−8 M and 2 × 10−9 M for SSAO from dog aorta, rat aorta, bovine aorta and human umbilical artery, respectively. SSAO obtained from bovine serum was relatively insensitive to MDL-72974A (ic50 = 3 × 10−7M. Following intraperitoneal administration of MDL-72974A, rat brain MAO-B was inhibited with the ed50 value being about 0.2 mg/kg. Rat aorta SSAO was also inhibited and to a similar extent by the same dose. MDL-72974A is the most potent SSAO inhibitor that has been described thus far.</div></front></TEI><affiliations><list><country><li>Canada</li></country></list><tree><country name="Canada"><noRegion><name sortKey="Yu, Peter H" sort="Yu, Peter H" uniqKey="Yu P" first="Peter H." last="Yu">Peter H. Yu</name></noRegion><name sortKey="Zuo, Dong Mei" sort="Zuo, Dong Mei" uniqKey="Zuo D" first="Dong-Mei" last="Zuo">Dong-Mei Zuo</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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