Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1
6-Nitroquipazine has been known as one of the most potent and selective inhibitors of serotonin transporter in vitro and in vivo. Nine derivatives of 6-nitroquipazine were synthesized and tested for their potential abilities to displace [ 3H]citalopram binding to the rat cortical membranes.
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2000-07, Vol.10 (14), p.1559-1562 |
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container_title | Bioorganic & medicinal chemistry letters |
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creator | Lee, Byoung Se Chu, Soyoung Lee, Byung Chul Chi, Dae Yoon Choe, Yearn Seong Jeong, Kyung Ja Jin, Changbae |
description | 6-Nitroquipazine has been known as one of the most potent and selective inhibitors of serotonin transporter in vitro and in vivo. Nine derivatives of 6-nitroquipazine were synthesized and tested for their potential abilities to displace [
3H]citalopram binding to the rat cortical membranes. |
doi_str_mv | 10.1016/S0960-894X(00)00290-0 |
format | Article |
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Drug treatments</subject><subject>Quipazine - analogs & derivatives</subject><subject>Quipazine - chemical synthesis</subject><subject>Quipazine - chemistry</subject><subject>Quipazine - pharmacokinetics</subject><subject>Quipazine - pharmacology</subject><subject>Rats</subject><subject>Serotonin Plasma Membrane Transport Proteins</subject><subject>Serotonin Uptake Inhibitors - chemical synthesis</subject><subject>Serotonin Uptake Inhibitors - chemistry</subject><subject>Serotonin Uptake Inhibitors - pharmacokinetics</subject><subject>Serotoninergic system</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkF1LHDEUhoO06Fb7EyxzUaRejJ58zexclbK0KggKttC7mM2cbCOzyZpkhe2vN_uBeudNTsh5zsnLQ8gxhTMKtDm_g66BetyJv98ATgFYBzXskREVjai5APmBjF6QA_IppQcAKkCIfXJAoaMSJIzI_d3K53-YMFXa99XU-d75WaWtdd5lV56DrZq63GN4XLqF_u88FlQPYbYsXRtilTCGHLzzVY7ap0WIGeNZdatjrugR-Wj1kPDzrh6SP79-_p5c1tc3F1eTH9e14R3kelxOFAymQmswhiNazbjoaYst77Bj_Ris5NgKTg1izxm22FDGaGullcgPycl272IdFFNWc5cMDoP2GJZJtZRJBowVUG5BE0NKEa1aRDfXcaUoqLVatVGr1t4UgNqoVVDmvuw-WE7n2L-Z2roswNcdoJPRgy0ujEuvnKDAGlmw71sMi40nh1El49Ab7F1Ek1Uf3DtJngGtJpad</recordid><startdate>20000717</startdate><enddate>20000717</enddate><creator>Lee, Byoung Se</creator><creator>Chu, Soyoung</creator><creator>Lee, Byung Chul</creator><creator>Chi, Dae Yoon</creator><creator>Choe, Yearn Seong</creator><creator>Jeong, Kyung Ja</creator><creator>Jin, Changbae</creator><general>Elsevier Ltd</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>20000717</creationdate><title>Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1</title><author>Lee, Byoung Se ; Chu, Soyoung ; Lee, Byung Chul ; Chi, Dae Yoon ; Choe, Yearn Seong ; Jeong, Kyung Ja ; Jin, Changbae</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c390t-8390e420b4aa0cc3eefa234d17e739e92d80f53e7431ceed32e7e612217f5f5e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Animals</topic><topic>Binding, Competitive</topic><topic>Biological and medical sciences</topic><topic>Carrier Proteins - metabolism</topic><topic>Cell Membrane - metabolism</topic><topic>Cerebral Cortex - metabolism</topic><topic>Citalopram - pharmacokinetics</topic><topic>Drug Design</topic><topic>Indicators and Reagents</topic><topic>Kinetics</topic><topic>Medical sciences</topic><topic>Membrane Glycoproteins - metabolism</topic><topic>Membrane Transport Proteins</topic><topic>Models, Structural</topic><topic>Molecular Conformation</topic><topic>Nerve Tissue Proteins</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. 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subjects | Animals Binding, Competitive Biological and medical sciences Carrier Proteins - metabolism Cell Membrane - metabolism Cerebral Cortex - metabolism Citalopram - pharmacokinetics Drug Design Indicators and Reagents Kinetics Medical sciences Membrane Glycoproteins - metabolism Membrane Transport Proteins Models, Structural Molecular Conformation Nerve Tissue Proteins Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Quipazine - analogs & derivatives Quipazine - chemical synthesis Quipazine - chemistry Quipazine - pharmacokinetics Quipazine - pharmacology Rats Serotonin Plasma Membrane Transport Proteins Serotonin Uptake Inhibitors - chemical synthesis Serotonin Uptake Inhibitors - chemistry Serotonin Uptake Inhibitors - pharmacokinetics Serotoninergic system Structure-Activity Relationship |
title | Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1 |
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