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 : 001616 ( Istex/Corpus ); précédent : 001615; suivant : 001617Inhibition 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 ; Dong-Mei ZuoSource :
- 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
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ISTEX:215D2145F1C4E19244E35F5F768993D2FE8843D0Le document en format XML
<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><title xml:lang="en">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</title><author><name sortKey="Yu, Peter H" sort="Yu, Peter H" uniqKey="Yu P" first="Peter H." last="Yu">Peter H. Yu</name><affiliation><mods:affiliation>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</mods:affiliation></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><mods:affiliation>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</mods:affiliation></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">ISTEX</idno><idno type="RBID">ISTEX:215D2145F1C4E19244E35F5F768993D2FE8843D0</idno><date when="1992" year="1992">1992</date><idno type="doi">10.1016/0006-2952(92)90293-R</idno><idno type="url">https://api-v5.istex.fr/document/215D2145F1C4E19244E35F5F768993D2FE8843D0/fulltext/pdf</idno><idno type="wicri:Area/Istex/Corpus">001616</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Corpus" wicri:corpus="ISTEX">001616</idno></publicationStmt><sourceDesc><biblStruct><analytic><title level="a" type="main" xml:lang="en">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</title><author><name sortKey="Yu, Peter H" sort="Yu, Peter H" uniqKey="Yu P" first="Peter H." last="Yu">Peter H. Yu</name><affiliation><mods:affiliation>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</mods:affiliation></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><mods:affiliation>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</mods:affiliation></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><istex><corpusName>elsevier</corpusName><author><json:item><name>Peter H. Yu</name><affiliations><json:string>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</json:string></affiliations></json:item><json:item><name>Dong-Mei Zuo</name><affiliations><json:string>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</json:string></affiliations></json:item></author><subject><json:item><lang><json:string>eng</json:string></lang><value>SSAO : semicarbazide-sensitive amine oxidase</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>MAO : monoamine oxidase</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>BSAO : bovine serum amine oxidase</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>MDL-72974A : (E)-2-(4-fluorophenethyl)-3-fluoroallylamine hydrochloride</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>PQR : pyrroloquinoline quinone</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>BZ : benzylamine</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>PLP : pyridoxyl phosphate</value></json:item></subject><articleId><json:string>9290293R</json:string></articleId><language><json:string>eng</json:string></language><originalGenre><json:string>Full-length article</json:string></originalGenre><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.</abstract><qualityIndicators><score>5.725</score><pdfWordCount>3577</pdfWordCount><pdfCharCount>23187</pdfCharCount><pdfVersion>1.2</pdfVersion><pdfPageCount>6</pdfPageCount><pdfPageSize>504 x 756 pts</pdfPageSize><refBibsNative>true</refBibsNative><abstractWordCount>179</abstractWordCount><abstractCharCount>1149</abstractCharCount><keywordCount>7</keywordCount></qualityIndicators><title>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</title><pii><json:string>0006-2952(92)90293-R</json:string></pii><genre><json:string>research-article</json:string></genre><serie><title>Neuromethods</title><language><json:string>unknown</json:string></language><volume>Vol. 5</volume><pages><first>235</first><last>272</last></pages></serie><host><title>Biochemical Pharmacology</title><language><json:string>unknown</json:string></language><publicationDate>1992</publicationDate><issn><json:string>0006-2952</json:string></issn><pii><json:string>S0006-2952(00)X0527-8</json:string></pii><volume>43</volume><issue>2</issue><pages><first>307</first><last>312</last></pages><genre><json:string>journal</json:string></genre></host><categories><wos><json:string>science</json:string><json:string>pharmacology & pharmacy</json:string></wos><scienceMetrix><json:string>health sciences</json:string><json:string>clinical medicine</json:string><json:string>pharmacology & pharmacy</json:string></scienceMetrix></categories><publicationDate>1992</publicationDate><copyrightDate>1992</copyrightDate><doi><json:string>10.1016/0006-2952(92)90293-R</json:string></doi><id>215D2145F1C4E19244E35F5F768993D2FE8843D0</id><fulltext><json:item><extension>pdf</extension><original>true</original><mimetype>application/pdf</mimetype><uri>https://api-v5.istex.fr/document/215D2145F1C4E19244E35F5F768993D2FE8843D0/fulltext/pdf</uri></json:item><json:item><extension>zip</extension><original>false</original><mimetype>application/zip</mimetype><uri>https://api-v5.istex.fr/document/215D2145F1C4E19244E35F5F768993D2FE8843D0/fulltext/zip</uri></json:item><istex:fulltextTEI uri="https://api-v5.istex.fr/document/215D2145F1C4E19244E35F5F768993D2FE8843D0/fulltext/tei"><teiHeader><fileDesc><titleStmt><title level="a" type="main" xml:lang="en">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</title></titleStmt><publicationStmt><authority>ISTEX</authority><publisher>ELSEVIER</publisher><availability><p>ELSEVIER</p></availability><date>1992</date></publicationStmt><sourceDesc><biblStruct type="inbook"><analytic><title level="a" type="main" xml:lang="en">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</title><author xml:id="author-0000"><persName><forename type="first">Peter H.</forename><surname>Yu</surname></persName><note type="correspondence"><p>Corresponding author: Dr. Peter H. Yu, Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada. Tel. (306) 966-8816; FAX (306) 966-8830.</p></note><affiliation>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</affiliation></author><author xml:id="author-0001"><persName><forename type="first">Dong-Mei</forename><surname>Zuo</surname></persName><affiliation>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</affiliation></author><idno type="istex">215D2145F1C4E19244E35F5F768993D2FE8843D0</idno><idno type="DOI">10.1016/0006-2952(92)90293-R</idno><idno type="PII">0006-2952(92)90293-R</idno><idno type="ArticleID">9290293R</idno></analytic><monogr><title level="j">Biochemical Pharmacology</title><title level="j" type="abbrev">BCP</title><idno type="pISSN">0006-2952</idno><idno type="PII">S0006-2952(00)X0527-8</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="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></monogr></biblStruct></sourceDesc></fileDesc><profileDesc><creation><date>1992</date></creation><langUsage><language ident="en">en</language></langUsage><abstract xml:lang="en"><p>(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.</p></abstract><textClass xml:lang="en"><keywords scheme="keyword"><list><head>Abbreviations</head><item><term>SSAO</term><term>semicarbazide-sensitive amine oxidase</term></item><item><term>MAO</term><term>monoamine oxidase</term></item><item><term>BSAO</term><term>bovine serum amine oxidase</term></item><item><term>MDL-72974A</term><term>(E)-2-(4-fluorophenethyl)-3-fluoroallylamine hydrochloride</term></item><item><term>PQR</term><term>pyrroloquinoline quinone</term></item><item><term>BZ</term><term>benzylamine</term></item><item><term>PLP</term><term>pyridoxyl phosphate</term></item></list></keywords></textClass></profileDesc><revisionDesc><change when="1992">Published</change></revisionDesc></teiHeader></istex:fulltextTEI><json:item><extension>txt</extension><original>false</original><mimetype>text/plain</mimetype><uri>https://api-v5.istex.fr/document/215D2145F1C4E19244E35F5F768993D2FE8843D0/fulltext/txt</uri></json:item></fulltext><metadata><istex:metadataXml wicri:clean="Elsevier, elements deleted: tail"><istex:xmlDeclaration>version="1.0" encoding="UTF-8"</istex:xmlDeclaration><istex:docType PUBLIC="-//ES//DTD journal article DTD version 4.5.2//EN//XML" URI="art452.dtd" name="istex:docType"></istex:docType><istex:document><converted-article version="4.5.2" docsubtype="fla" xml:lang="en"><item-info><jid>BCP</jid><aid>9290293R</aid><ce:pii>0006-2952(92)90293-R</ce:pii><ce:doi>10.1016/0006-2952(92)90293-R</ce:doi><ce:copyright type="unknown" year="1992"></ce:copyright></item-info><head><ce:title>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</ce:title><ce:author-group><ce:author><ce:given-name>Peter H.</ce:given-name><ce:surname>Yu</ce:surname><ce:cross-ref refid="COR1"><ce:sup loc="post">∗</ce:sup></ce:cross-ref></ce:author><ce:author><ce:given-name>Dong-Mei</ce:given-name><ce:surname>Zuo</ce:surname></ce:author><ce:affiliation><ce:textfn>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</ce:textfn></ce:affiliation><ce:correspondence id="COR1"><ce:label>∗</ce:label><ce:text>Corresponding author: Dr. Peter H. Yu, Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada. Tel. (306) 966-8816; FAX (306) 966-8830.</ce:text></ce:correspondence></ce:author-group><ce:date-received day="24" month="6" year="1991"></ce:date-received><ce:date-accepted day="5" month="9" year="1991"></ce:date-accepted><ce:abstract class="author"><ce:section-title>Abstract</ce:section-title><ce:abstract-sec><ce:simple-para view="all" id="simple-para.0010">(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 <ce:small-caps>ic</ce:small-caps><ce:inf loc="post">50</ce:inf> values were estimated to be 2 × 10<ce:sup loc="post">−9</ce:sup> M, 5 × 10<ce:sup loc="post">−9</ce:sup> M, 8 × 10<ce:sup loc="post">−8</ce:sup> M and 2 × 10<ce:sup loc="post">−9</ce:sup> 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 (<math altimg="si1.gif"><scp>ic</scp><inf loc="post">50</inf> = 3 × 10<sup loc="post">−7</sup><rm>M</rm></math>. Following intraperitoneal administration of MDL-72974A, rat brain MAO-B was inhibited with the <ce:small-caps>ed</ce:small-caps><ce:inf loc="post">50</ce:inf> 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.</ce:simple-para></ce:abstract-sec></ce:abstract><ce:keywords class="abr"><ce:section-title>Abbreviations</ce:section-title><ce:keyword><ce:text>SSAO</ce:text><ce:keyword><ce:text>semicarbazide-sensitive amine oxidase</ce:text></ce:keyword></ce:keyword><ce:keyword><ce:text>MAO</ce:text><ce:keyword><ce:text>monoamine oxidase</ce:text></ce:keyword></ce:keyword><ce:keyword><ce:text>BSAO</ce:text><ce:keyword><ce:text>bovine serum amine oxidase</ce:text></ce:keyword></ce:keyword><ce:keyword><ce:text>MDL-72974A</ce:text><ce:keyword><ce:text>(E)-2-(4-fluorophenethyl)-3-fluoroallylamine hydrochloride</ce:text></ce:keyword></ce:keyword><ce:keyword><ce:text>PQR</ce:text><ce:keyword><ce:text>pyrroloquinoline quinone</ce:text></ce:keyword></ce:keyword><ce:keyword><ce:text>BZ</ce:text><ce:keyword><ce:text>benzylamine</ce:text></ce:keyword></ce:keyword><ce:keyword><ce:text>PLP</ce:text><ce:keyword><ce:text>pyridoxyl phosphate</ce:text></ce:keyword></ce:keyword></ce:keywords></head></converted-article></istex:document></istex:metadataXml><mods version="3.6"><titleInfo lang="en"><title>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</title></titleInfo><titleInfo type="alternative" lang="en" contentType="CDATA"><title>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</title></titleInfo><name type="personal"><namePart type="given">Peter H.</namePart><namePart type="family">Yu</namePart><affiliation>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</affiliation><description>Corresponding author: Dr. Peter H. Yu, Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada. Tel. (306) 966-8816; FAX (306) 966-8830.</description><role><roleTerm type="text">author</roleTerm></role></name><name type="personal"><namePart type="given">Dong-Mei</namePart><namePart type="family">Zuo</namePart><affiliation>Neuropsychiatric Research Unit, Department of Psychiatry, University of Saskatchewan, Saskatoon, Saskatchewan, S7N 0W0, Canada</affiliation><role><roleTerm type="text">author</roleTerm></role></name><typeOfResource>text</typeOfResource><genre type="research-article" displayLabel="Full-length article"></genre><originInfo><publisher>ELSEVIER</publisher><dateIssued encoding="w3cdtf">1992</dateIssued><copyrightDate encoding="w3cdtf">1992</copyrightDate></originInfo><language><languageTerm type="code" authority="iso639-2b">eng</languageTerm><languageTerm type="code" authority="rfc3066">en</languageTerm></language><physicalDescription><internetMediaType>text/html</internetMediaType></physicalDescription><abstract 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.</abstract><subject lang="en"><genre>Abbreviations</genre><topic>SSAO : semicarbazide-sensitive amine oxidase</topic><topic>MAO : monoamine oxidase</topic><topic>BSAO : bovine serum amine oxidase</topic><topic>MDL-72974A : (E)-2-(4-fluorophenethyl)-3-fluoroallylamine hydrochloride</topic><topic>PQR : pyrroloquinoline quinone</topic><topic>BZ : benzylamine</topic><topic>PLP : pyridoxyl phosphate</topic></subject><relatedItem type="host"><titleInfo><title>Biochemical Pharmacology</title></titleInfo><titleInfo type="abbreviated"><title>BCP</title></titleInfo><genre type="journal">journal</genre><originInfo><dateIssued encoding="w3cdtf">19920122</dateIssued></originInfo><identifier type="ISSN">0006-2952</identifier><identifier type="PII">S0006-2952(00)X0527-8</identifier><part><date>19920122</date><detail type="volume"><number>43</number><caption>vol.</caption></detail><detail type="issue"><number>2</number><caption>no.</caption></detail><extent unit="issue pages"><start>119</start><end>391</end></extent><extent unit="pages"><start>307</start><end>312</end></extent></part></relatedItem><identifier type="istex">215D2145F1C4E19244E35F5F768993D2FE8843D0</identifier><identifier type="DOI">10.1016/0006-2952(92)90293-R</identifier><identifier type="PII">0006-2952(92)90293-R</identifier><identifier type="ArticleID">9290293R</identifier><recordInfo><recordContentSource>ELSEVIER</recordContentSource></recordInfo></mods></metadata></istex></record>Pour manipuler ce document sous Unix (Dilib)
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