Effects of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook, a Constituent of Yokukansan, on Human Recombinant Serotonin7 Receptor
Effects of seven alkaloids, geissoschizine methyl ether (GM), hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine and isocorynoxeine, in Uncaria hook, a constituent of the kampo medicine yokukansan, on serotonin 7 (5-HT 7 ) receptor were investigated using Chinese hamster ovary (...
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| Veröffentlicht in: | Cellular and molecular neurobiology 2013, Vol.33 (1), p.129-135 |
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| container_title | Cellular and molecular neurobiology |
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| creator | Ueki, Toshiyuki Nishi, Akinori Imamura, Sachiko Kanno, Hitomi Mizoguchi, Kazushige Sekiguchi, Kyoji Ikarashi, Yasushi Kase, Yoshio |
| description | Effects of seven alkaloids, geissoschizine methyl ether (GM), hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine and isocorynoxeine, in Uncaria hook, a constituent of the kampo medicine yokukansan, on serotonin
7
(5-HT
7
) receptor were investigated using Chinese hamster ovary (CHO) cell membranes and human embryonic kidney 293 (HEK293) cells stably expressing the human recombinant 5-HT
7
receptor. A competitive binding assay using CHO membranes showed that GM (IC
50
= 0.034 μM) more strongly inhibited the binding of the radioligand [
3
H] LSD to 5-HT
7
receptor than the other alkaloids, suggesting that GM is bound to 5-HT
7
receptor. Agonistic/antagonistic effects of GM (1–50 μM) on the receptor were evaluated by measuring intracellular cAMP levels in HEK239 cells. GM (IC
50
= 6.0 μM) inhibited 5-HT-induced cAMP production in a concentration-dependent manner, as well as the specific 5-HT
7
receptor antagonist SB-269970 (0.1–1 μM). However, GM did not induce intracellular cAMP production as 5-HT did. These results suggest that GM has an antagonistic effect on 5-HT
7
receptor. |
| doi_str_mv | 10.1007/s10571-012-9878-3 |
| format | Article |
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7
(5-HT
7
) receptor were investigated using Chinese hamster ovary (CHO) cell membranes and human embryonic kidney 293 (HEK293) cells stably expressing the human recombinant 5-HT
7
receptor. A competitive binding assay using CHO membranes showed that GM (IC
50
= 0.034 μM) more strongly inhibited the binding of the radioligand [
3
H] LSD to 5-HT
7
receptor than the other alkaloids, suggesting that GM is bound to 5-HT
7
receptor. Agonistic/antagonistic effects of GM (1–50 μM) on the receptor were evaluated by measuring intracellular cAMP levels in HEK239 cells. GM (IC
50
= 6.0 μM) inhibited 5-HT-induced cAMP production in a concentration-dependent manner, as well as the specific 5-HT
7
receptor antagonist SB-269970 (0.1–1 μM). However, GM did not induce intracellular cAMP production as 5-HT did. These results suggest that GM has an antagonistic effect on 5-HT
7
receptor.</description><identifier>ISSN: 0272-4340</identifier><identifier>EISSN: 1573-6830</identifier><identifier>DOI: 10.1007/s10571-012-9878-3</identifier><language>eng</language><publisher>Boston: Springer US</publisher><subject>Alkaloids ; Biomedical and Life Sciences ; Biomedicine ; Cell Biology ; Neurobiology ; Neurosciences ; Original Research</subject><ispartof>Cellular and molecular neurobiology, 2013, Vol.33 (1), p.129-135</ispartof><rights>Springer Science+Business Media, LLC 2012</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3023-4477396d4d17e6071fb840702b7c55e007d7675c292e0a8fa7eeb2e037756c3</citedby><cites>FETCH-LOGICAL-c3023-4477396d4d17e6071fb840702b7c55e007d7675c292e0a8fa7eeb2e037756c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s10571-012-9878-3$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s10571-012-9878-3$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27923,27924,41487,42556,51318</link.rule.ids></links><search><creatorcontrib>Ueki, Toshiyuki</creatorcontrib><creatorcontrib>Nishi, Akinori</creatorcontrib><creatorcontrib>Imamura, Sachiko</creatorcontrib><creatorcontrib>Kanno, Hitomi</creatorcontrib><creatorcontrib>Mizoguchi, Kazushige</creatorcontrib><creatorcontrib>Sekiguchi, Kyoji</creatorcontrib><creatorcontrib>Ikarashi, Yasushi</creatorcontrib><creatorcontrib>Kase, Yoshio</creatorcontrib><title>Effects of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook, a Constituent of Yokukansan, on Human Recombinant Serotonin7 Receptor</title><title>Cellular and molecular neurobiology</title><addtitle>Cell Mol Neurobiol</addtitle><description>Effects of seven alkaloids, geissoschizine methyl ether (GM), hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine and isocorynoxeine, in Uncaria hook, a constituent of the kampo medicine yokukansan, on serotonin
7
(5-HT
7
) receptor were investigated using Chinese hamster ovary (CHO) cell membranes and human embryonic kidney 293 (HEK293) cells stably expressing the human recombinant 5-HT
7
receptor. A competitive binding assay using CHO membranes showed that GM (IC
50
= 0.034 μM) more strongly inhibited the binding of the radioligand [
3
H] LSD to 5-HT
7
receptor than the other alkaloids, suggesting that GM is bound to 5-HT
7
receptor. Agonistic/antagonistic effects of GM (1–50 μM) on the receptor were evaluated by measuring intracellular cAMP levels in HEK239 cells. GM (IC
50
= 6.0 μM) inhibited 5-HT-induced cAMP production in a concentration-dependent manner, as well as the specific 5-HT
7
receptor antagonist SB-269970 (0.1–1 μM). However, GM did not induce intracellular cAMP production as 5-HT did. These results suggest that GM has an antagonistic effect on 5-HT
7
receptor.</description><subject>Alkaloids</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Cell Biology</subject><subject>Neurobiology</subject><subject>Neurosciences</subject><subject>Original Research</subject><issn>0272-4340</issn><issn>1573-6830</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><recordid>eNp9kLFu2zAQhomiBeqmfYBuHDtE6ZGUdPIYGE4cIEWBJhkyETR1qhnLpENSQ_IWeeNQcOdOdzh8_w_cx9h3ARcCAH8mAQ2KCoSslh12lfrAFqJBVbWdgo9sARJlVasaPrMvKT0BwBKgWbC39TCQzYmHgV-TSykku3OvzhP_RXn3MvJ13lE858bzG9-HkfjluDdjcD13nj94a6IzfBPCvjB8FXzKLk_k89z4GPbT3vhk_DkPnm-mQ6n5QzYcts6bwtxRDDl453E-0zGH-JV9GsyY6Nu_ecburtb3q011-_v6ZnV5W1kFUlV1jaiWbV_3AqkFFMO2qwFBbtE2DRUnPbbYWLmUBKYbDBJty6oQm9aqM_bj1HqM4XmilPXBJUvjaDyFKWlRSyyOJKiCihNqY0gp0qCP0R1MfNEC9Cxfn-TrIl_P8vWckadMKqz_S1E_hSn68s9_Qu9fooeq</recordid><startdate>2013</startdate><enddate>2013</enddate><creator>Ueki, Toshiyuki</creator><creator>Nishi, Akinori</creator><creator>Imamura, Sachiko</creator><creator>Kanno, Hitomi</creator><creator>Mizoguchi, Kazushige</creator><creator>Sekiguchi, Kyoji</creator><creator>Ikarashi, Yasushi</creator><creator>Kase, Yoshio</creator><general>Springer US</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7TK</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>RC3</scope></search><sort><creationdate>2013</creationdate><title>Effects of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook, a Constituent of Yokukansan, on Human Recombinant Serotonin7 Receptor</title><author>Ueki, Toshiyuki ; Nishi, Akinori ; Imamura, Sachiko ; Kanno, Hitomi ; Mizoguchi, Kazushige ; Sekiguchi, Kyoji ; Ikarashi, Yasushi ; Kase, Yoshio</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3023-4477396d4d17e6071fb840702b7c55e007d7675c292e0a8fa7eeb2e037756c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>Alkaloids</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Cell Biology</topic><topic>Neurobiology</topic><topic>Neurosciences</topic><topic>Original Research</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ueki, Toshiyuki</creatorcontrib><creatorcontrib>Nishi, Akinori</creatorcontrib><creatorcontrib>Imamura, Sachiko</creatorcontrib><creatorcontrib>Kanno, Hitomi</creatorcontrib><creatorcontrib>Mizoguchi, Kazushige</creatorcontrib><creatorcontrib>Sekiguchi, Kyoji</creatorcontrib><creatorcontrib>Ikarashi, Yasushi</creatorcontrib><creatorcontrib>Kase, Yoshio</creatorcontrib><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Genetics Abstracts</collection><jtitle>Cellular and molecular neurobiology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ueki, Toshiyuki</au><au>Nishi, Akinori</au><au>Imamura, Sachiko</au><au>Kanno, Hitomi</au><au>Mizoguchi, Kazushige</au><au>Sekiguchi, Kyoji</au><au>Ikarashi, Yasushi</au><au>Kase, Yoshio</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effects of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook, a Constituent of Yokukansan, on Human Recombinant Serotonin7 Receptor</atitle><jtitle>Cellular and molecular neurobiology</jtitle><stitle>Cell Mol Neurobiol</stitle><date>2013</date><risdate>2013</risdate><volume>33</volume><issue>1</issue><spage>129</spage><epage>135</epage><pages>129-135</pages><issn>0272-4340</issn><eissn>1573-6830</eissn><abstract>Effects of seven alkaloids, geissoschizine methyl ether (GM), hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine and isocorynoxeine, in Uncaria hook, a constituent of the kampo medicine yokukansan, on serotonin
7
(5-HT
7
) receptor were investigated using Chinese hamster ovary (CHO) cell membranes and human embryonic kidney 293 (HEK293) cells stably expressing the human recombinant 5-HT
7
receptor. A competitive binding assay using CHO membranes showed that GM (IC
50
= 0.034 μM) more strongly inhibited the binding of the radioligand [
3
H] LSD to 5-HT
7
receptor than the other alkaloids, suggesting that GM is bound to 5-HT
7
receptor. Agonistic/antagonistic effects of GM (1–50 μM) on the receptor were evaluated by measuring intracellular cAMP levels in HEK239 cells. GM (IC
50
= 6.0 μM) inhibited 5-HT-induced cAMP production in a concentration-dependent manner, as well as the specific 5-HT
7
receptor antagonist SB-269970 (0.1–1 μM). However, GM did not induce intracellular cAMP production as 5-HT did. These results suggest that GM has an antagonistic effect on 5-HT
7
receptor.</abstract><cop>Boston</cop><pub>Springer US</pub><doi>10.1007/s10571-012-9878-3</doi><tpages>7</tpages></addata></record> |
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| subjects | Alkaloids Biomedical and Life Sciences Biomedicine Cell Biology Neurobiology Neurosciences Original Research |
| title | Effects of Geissoschizine Methyl Ether, an Indole Alkaloid in Uncaria Hook, a Constituent of Yokukansan, on Human Recombinant Serotonin7 Receptor |
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