Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands
Copyright © 2011 Elsevier Ltd. All rights reserved..
Novel arene- and quinolinesulfonamides were synthesized using different solutions and a solid-support methodology, and were evaluated for their affinity for 5-HT(1A), 5-HT(2A), 5-HT(6), and 5-HT(7) receptors. Compound 54 (N-Ethyl-N-[4-(1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinolin-2-yl)butyl]-8-quinolinesulfonamide) was identified as potent 5-HT(7) antagonist (K(i)=13 nM, K(B)=140 nM) with good selectivity over 5-HT(1A), 5-HT(2A), 5-HT(6) receptors. In the FST in mice, it reduced immobility in a manner similar to the selective 5-HT(7) antagonist SB-269970.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2011 |
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| Erschienen: |
2011 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:19 |
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| Enthalten in: |
Bioorganic & medicinal chemistry - 19(2011), 22 vom: 15. Nov., Seite 6750-9 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Zajdel, Paweł [VerfasserIn] |
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| Links: |
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| Themen: |
Antidepressive Agents |
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| Anmerkungen: |
Date Completed 22.05.2012 Date Revised 31.10.2011 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmc.2011.09.044 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM212250213 |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2011 Elsevier Ltd. All rights reserved. | ||
| 520 | |a Novel arene- and quinolinesulfonamides were synthesized using different solutions and a solid-support methodology, and were evaluated for their affinity for 5-HT(1A), 5-HT(2A), 5-HT(6), and 5-HT(7) receptors. Compound 54 (N-Ethyl-N-[4-(1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinolin-2-yl)butyl]-8-quinolinesulfonamide) was identified as potent 5-HT(7) antagonist (K(i)=13 nM, K(B)=140 nM) with good selectivity over 5-HT(1A), 5-HT(2A), 5-HT(6) receptors. In the FST in mice, it reduced immobility in a manner similar to the selective 5-HT(7) antagonist SB-269970 | ||
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| 650 | 7 | |a Ligands |2 NLM | |
| 650 | 7 | |a Quinolines |2 NLM | |
| 650 | 7 | |a Receptors, Serotonin |2 NLM | |
| 650 | 7 | |a Sulfonamides |2 NLM | |
| 650 | 7 | |a serotonin 7 receptor |2 NLM | |
| 700 | 1 | |a Marciniec, Krzysztof |e verfasserin |4 aut | |
| 700 | 1 | |a Maślankiewicz, Andrzej |e verfasserin |4 aut | |
| 700 | 1 | |a Paluchowska, Maria H |e verfasserin |4 aut | |
| 700 | 1 | |a Satała, Grzegorz |e verfasserin |4 aut | |
| 700 | 1 | |a Partyka, Anna |e verfasserin |4 aut | |
| 700 | 1 | |a Jastrzębska-Więsek, Magdalena |e verfasserin |4 aut | |
| 700 | 1 | |a Wróbel, Dagmara |e verfasserin |4 aut | |
| 700 | 1 | |a Wesołowska, Anna |e verfasserin |4 aut | |
| 700 | 1 | |a Duszyńska, Beata |e verfasserin |4 aut | |
| 700 | 1 | |a Bojarski, Andrzej J |e verfasserin |4 aut | |
| 700 | 1 | |a Pawłowski, Maciej |e verfasserin |4 aut | |
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