High affinity binding of [ 3H]paroxetine and [ 3H]imipramine to human platelet membranes
Paroxetine, one of the most potent and specific serotonin uptake inhibitors, was tritiated and used for binding studies with human platelet membranes. Specific, high affinity binding was demonstrated. The binding was compared with [ 3H]imipramine binding; it was found that the maximal binding (B max...
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| Veröffentlicht in: | European journal of pharmacology 1983-12, Vol.96 (3), p.303-309 |
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| container_title | European journal of pharmacology |
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| creator | Mellerup, Erling T. Plenge, Per Engelstoft, Mogens |
| description | Paroxetine, one of the most potent and specific serotonin uptake inhibitors, was tritiated and used for binding studies with human platelet membranes. Specific, high affinity binding was demonstrated. The binding was compared with [
3H]imipramine binding; it was found that the maximal binding (B
max) was the same for [
3H]paroxetine and [
3H]imipramine, whereas the affinity was much higher for [
3H]paroxetine (K
D 0.08 nM and 0.56 nM for paroxetine and imipramine binding, respectively). IC
50 was calculated for the inhibition of [
3H]paroxetine and [
3H]imipramine binding by a number of antidepressants; the corresponding Hill coefficients were also calculated. |
| doi_str_mv | 10.1016/0014-2999(83)90321-7 |
| format | Article |
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3H]imipramine binding; it was found that the maximal binding (B
max) was the same for [
3H]paroxetine and [
3H]imipramine, whereas the affinity was much higher for [
3H]paroxetine (K
D 0.08 nM and 0.56 nM for paroxetine and imipramine binding, respectively). IC
50 was calculated for the inhibition of [
3H]paroxetine and [
3H]imipramine binding by a number of antidepressants; the corresponding Hill coefficients were also calculated.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(83)90321-7</identifier><identifier>PMID: 6233162</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>[ 3H]Imipramine ; [ 3H]Paroxetine ; Antidepressive Agents, Tricyclic - pharmacology ; Binding ; Biological and medical sciences ; Blood Platelets - metabolism ; Cell Membrane - metabolism ; Human platelets ; Humans ; Imipramine - blood ; Kinetics ; Medical sciences ; Neuropharmacology ; Paroxetine ; Pharmacology. Drug treatments ; Piperidines - blood ; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) ; Psychology. Psychoanalysis. Psychiatry ; Psychopharmacology ; Receptors, Serotonin - drug effects ; Serotonin Antagonists - blood ; Serotonin uptake</subject><ispartof>European journal of pharmacology, 1983-12, Vol.96 (3), p.303-309</ispartof><rights>1983</rights><rights>1985 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c367t-5b7a1ec1bc99384a2eccd76d2697cfcbc8b79c71fe6da68cb9d1211404c08e633</citedby><cites>FETCH-LOGICAL-c367t-5b7a1ec1bc99384a2eccd76d2697cfcbc8b79c71fe6da68cb9d1211404c08e633</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/0014299983903217$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8854988$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6233162$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Mellerup, Erling T.</creatorcontrib><creatorcontrib>Plenge, Per</creatorcontrib><creatorcontrib>Engelstoft, Mogens</creatorcontrib><title>High affinity binding of [ 3H]paroxetine and [ 3H]imipramine to human platelet membranes</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Paroxetine, one of the most potent and specific serotonin uptake inhibitors, was tritiated and used for binding studies with human platelet membranes. Specific, high affinity binding was demonstrated. The binding was compared with [
3H]imipramine binding; it was found that the maximal binding (B
max) was the same for [
3H]paroxetine and [
3H]imipramine, whereas the affinity was much higher for [
3H]paroxetine (K
D 0.08 nM and 0.56 nM for paroxetine and imipramine binding, respectively). IC
50 was calculated for the inhibition of [
3H]paroxetine and [
3H]imipramine binding by a number of antidepressants; the corresponding Hill coefficients were also calculated.</description><subject>[ 3H]Imipramine</subject><subject>[ 3H]Paroxetine</subject><subject>Antidepressive Agents, Tricyclic - pharmacology</subject><subject>Binding</subject><subject>Biological and medical sciences</subject><subject>Blood Platelets - metabolism</subject><subject>Cell Membrane - metabolism</subject><subject>Human platelets</subject><subject>Humans</subject><subject>Imipramine - blood</subject><subject>Kinetics</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Paroxetine</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperidines - blood</subject><subject>Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychopharmacology</subject><subject>Receptors, Serotonin - drug effects</subject><subject>Serotonin Antagonists - blood</subject><subject>Serotonin uptake</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1983</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1LHEEQhhtRzLrxHxjog4geJvbHbH9cAkHUDQi5KARCaHqqa7RlvuyeFf33zrrLHnMqeOupouoh5ISz75xxdckYLwthrT038sIyKXih98iMG20LprnYJ7Md8oUc5fzMGFtYsTgkh0pIyZWYkT_L-PhEfV3HLo7vtIpdiN0j7Wv6l8rlv8Gn_g3H2CH1XdhksY1D8u06G3v6tGp9R4fGj9jgSFtsq-Q7zF_JQe2bjMfbOicPN9f3V8vi7vftr6ufdwVIpcdiUWnPEXgF1kpTeoEAQasglNVQQwWm0hY0r1EFrwxUNnDBeclKYAaVlHNyttk7pP5lhXl0bcyATTMd0a-yM8xYq42awHIDQupzTli7IcXWp3fHmVsLdWtbbm3LGek-hTo9jX3b7l9VLYbd0Nbg1D_d9n0G39TT8xDzDjNmUVpjJuzHBsPJxWvE5DJE7ABDTAijC338_x0fHxuRsg</recordid><startdate>19831223</startdate><enddate>19831223</enddate><creator>Mellerup, Erling T.</creator><creator>Plenge, Per</creator><creator>Engelstoft, Mogens</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19831223</creationdate><title>High affinity binding of [ 3H]paroxetine and [ 3H]imipramine to human platelet membranes</title><author>Mellerup, Erling T. ; Plenge, Per ; Engelstoft, Mogens</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c367t-5b7a1ec1bc99384a2eccd76d2697cfcbc8b79c71fe6da68cb9d1211404c08e633</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1983</creationdate><topic>[ 3H]Imipramine</topic><topic>[ 3H]Paroxetine</topic><topic>Antidepressive Agents, Tricyclic - pharmacology</topic><topic>Binding</topic><topic>Biological and medical sciences</topic><topic>Blood Platelets - metabolism</topic><topic>Cell Membrane - metabolism</topic><topic>Human platelets</topic><topic>Humans</topic><topic>Imipramine - blood</topic><topic>Kinetics</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Paroxetine</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperidines - blood</topic><topic>Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychopharmacology</topic><topic>Receptors, Serotonin - drug effects</topic><topic>Serotonin Antagonists - blood</topic><topic>Serotonin uptake</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Mellerup, Erling T.</creatorcontrib><creatorcontrib>Plenge, Per</creatorcontrib><creatorcontrib>Engelstoft, Mogens</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Mellerup, Erling T.</au><au>Plenge, Per</au><au>Engelstoft, Mogens</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>High affinity binding of [ 3H]paroxetine and [ 3H]imipramine to human platelet membranes</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1983-12-23</date><risdate>1983</risdate><volume>96</volume><issue>3</issue><spage>303</spage><epage>309</epage><pages>303-309</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Paroxetine, one of the most potent and specific serotonin uptake inhibitors, was tritiated and used for binding studies with human platelet membranes. Specific, high affinity binding was demonstrated. The binding was compared with [
3H]imipramine binding; it was found that the maximal binding (B
max) was the same for [
3H]paroxetine and [
3H]imipramine, whereas the affinity was much higher for [
3H]paroxetine (K
D 0.08 nM and 0.56 nM for paroxetine and imipramine binding, respectively). IC
50 was calculated for the inhibition of [
3H]paroxetine and [
3H]imipramine binding by a number of antidepressants; the corresponding Hill coefficients were also calculated.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>6233162</pmid><doi>10.1016/0014-2999(83)90321-7</doi><tpages>7</tpages></addata></record> |
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| identifier | ISSN: 0014-2999 |
| ispartof | European journal of pharmacology, 1983-12, Vol.96 (3), p.303-309 |
| issn | 0014-2999 1879-0712 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | [ 3H]Imipramine [ 3H]Paroxetine Antidepressive Agents, Tricyclic - pharmacology Binding Biological and medical sciences Blood Platelets - metabolism Cell Membrane - metabolism Human platelets Humans Imipramine - blood Kinetics Medical sciences Neuropharmacology Paroxetine Pharmacology. Drug treatments Piperidines - blood Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Receptors, Serotonin - drug effects Serotonin Antagonists - blood Serotonin uptake |
| title | High affinity binding of [ 3H]paroxetine and [ 3H]imipramine to human platelet membranes |
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