1-(m-clorophenyl)-biguanide, a potent high affinity 5-HT3 receptor agonist
1-(m-Chlorophenyl)-biguanide (mCPBG) was examined and compared with three 5-HT3 receptor agonists in three 5-HT3 receptor models. mCPBG inhibited [3H]GR67330 binding to 5-HT3 receptors with high affinity (IC50 1.5 nM). mCPBG depolarized the rat vagus nerve with an EC50 one tenth of that for 5-HT (0....
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| Veröffentlicht in: | European journal of pharmacology 1990-06, Vol.182 (1), p.193-197 |
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| container_end_page | 197 |
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| container_title | European journal of pharmacology |
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| creator | KILPATRICK, G. J BUTLER, A BURRIDGE, J OXFORD, A. W |
| description | 1-(m-Chlorophenyl)-biguanide (mCPBG) was examined and compared with three 5-HT3 receptor agonists in three 5-HT3 receptor models. mCPBG inhibited [3H]GR67330 binding to 5-HT3 receptors with high affinity (IC50 1.5 nM). mCPBG depolarized the rat vagus nerve with an EC50 one tenth of that for 5-HT (0.05 vs. 0.46 microM); the maximum depolarization was approximately half that for 5-HT. The mCPBG depolarization was potently blocked by the selective 5-HT3 antagonist, ondansetron (pKB 8.6 +/- 0.1). In anaesthetised cats, mCPBG potently evoked the Bezold-Jarisch reflex which was blocked by low doses of ondansetron (10 micrograms/kg i.v.). It is concluded that mCPBG is a potent, high affinity 5-HT3 receptor agonist. |
| doi_str_mv | 10.1016/0014-2999(90)90513-6 |
| format | Article |
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J ; BUTLER, A ; BURRIDGE, J ; OXFORD, A. W</creator><creatorcontrib>KILPATRICK, G. J ; BUTLER, A ; BURRIDGE, J ; OXFORD, A. W</creatorcontrib><description>1-(m-Chlorophenyl)-biguanide (mCPBG) was examined and compared with three 5-HT3 receptor agonists in three 5-HT3 receptor models. mCPBG inhibited [3H]GR67330 binding to 5-HT3 receptors with high affinity (IC50 1.5 nM). mCPBG depolarized the rat vagus nerve with an EC50 one tenth of that for 5-HT (0.05 vs. 0.46 microM); the maximum depolarization was approximately half that for 5-HT. The mCPBG depolarization was potently blocked by the selective 5-HT3 antagonist, ondansetron (pKB 8.6 +/- 0.1). In anaesthetised cats, mCPBG potently evoked the Bezold-Jarisch reflex which was blocked by low doses of ondansetron (10 micrograms/kg i.v.). It is concluded that mCPBG is a potent, high affinity 5-HT3 receptor agonist.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(90)90513-6</identifier><identifier>PMID: 2144822</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier</publisher><subject>Anesthesia ; Animals ; Biguanides - pharmacology ; Binding, Competitive - drug effects ; Biological and medical sciences ; Cats ; Heart Rate - drug effects ; Imidazoles - pharmacology ; In Vitro Techniques ; Male ; Medical sciences ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Ondansetron ; Pharmacology. 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J</creatorcontrib><creatorcontrib>BUTLER, A</creatorcontrib><creatorcontrib>BURRIDGE, J</creatorcontrib><creatorcontrib>OXFORD, A. W</creatorcontrib><title>1-(m-clorophenyl)-biguanide, a potent high affinity 5-HT3 receptor agonist</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>1-(m-Chlorophenyl)-biguanide (mCPBG) was examined and compared with three 5-HT3 receptor agonists in three 5-HT3 receptor models. mCPBG inhibited [3H]GR67330 binding to 5-HT3 receptors with high affinity (IC50 1.5 nM). mCPBG depolarized the rat vagus nerve with an EC50 one tenth of that for 5-HT (0.05 vs. 0.46 microM); the maximum depolarization was approximately half that for 5-HT. The mCPBG depolarization was potently blocked by the selective 5-HT3 antagonist, ondansetron (pKB 8.6 +/- 0.1). In anaesthetised cats, mCPBG potently evoked the Bezold-Jarisch reflex which was blocked by low doses of ondansetron (10 micrograms/kg i.v.). It is concluded that mCPBG is a potent, high affinity 5-HT3 receptor agonist.</description><subject>Anesthesia</subject><subject>Animals</subject><subject>Biguanides - pharmacology</subject><subject>Binding, Competitive - drug effects</subject><subject>Biological and medical sciences</subject><subject>Cats</subject><subject>Heart Rate - drug effects</subject><subject>Imidazoles - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Ondansetron</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Receptors, Serotonin - drug effects</subject><subject>Reflex - drug effects</subject><subject>Serotoninergic system</subject><subject>Vagus Nerve - drug effects</subject><subject>Vagus Nerve - metabolism</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1990</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkD1PwzAURS0EKqXwD0DKAioSBj9_JPGIKqCgSixlthzHaY3SJNjJ0H9PQqMyveHec6V3ELoG8ggE4idCgGMqpZxLci-JAIbjEzSFNJGYJEBP0fRYOUcXIXwTQoSkYoImFDhPKZ2iD8DzHTZl7etma6t9eY8zt-l05XL7EOmoqVtbtdHWbbaRLgpXuXYfCbxcs8hbY5u29pHe1JUL7SU6K3QZ7NV4Z-jr9WW9WOLV59v74nmFDY15i4FxmtmUGsHiPAeigduCJJkQUuc8S7QwYGJZAAeRgGDGcsgZjTXjWuiCsBm6O-w2vv7pbGjVzgVjy1JXtu6CSvs3eQ_0RX4oGl-H4G2hGu922u8VEDUoVIMfNfhRkqg_hWrAbsb9LtvZ_AiNzvr8dsx1MLosvK6MC__bkkqepIL9AkEvdwY</recordid><startdate>19900621</startdate><enddate>19900621</enddate><creator>KILPATRICK, G. J</creator><creator>BUTLER, A</creator><creator>BURRIDGE, J</creator><creator>OXFORD, A. W</creator><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>19900621</creationdate><title>1-(m-clorophenyl)-biguanide, a potent high affinity 5-HT3 receptor agonist</title><author>KILPATRICK, G. J ; BUTLER, A ; BURRIDGE, J ; OXFORD, A. W</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c264t-1342be82c536dd10a14ef07b559ad4b7a5c1c69f14157153ce41d326a34a5af03</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1990</creationdate><topic>Anesthesia</topic><topic>Animals</topic><topic>Biguanides - pharmacology</topic><topic>Binding, Competitive - drug effects</topic><topic>Biological and medical sciences</topic><topic>Cats</topic><topic>Heart Rate - drug effects</topic><topic>Imidazoles - pharmacology</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Ondansetron</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Receptors, Serotonin - drug effects</topic><topic>Reflex - drug effects</topic><topic>Serotoninergic system</topic><topic>Vagus Nerve - drug effects</topic><topic>Vagus Nerve - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>KILPATRICK, G. J</creatorcontrib><creatorcontrib>BUTLER, A</creatorcontrib><creatorcontrib>BURRIDGE, J</creatorcontrib><creatorcontrib>OXFORD, A. W</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>KILPATRICK, G. J</au><au>BUTLER, A</au><au>BURRIDGE, J</au><au>OXFORD, A. W</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>1-(m-clorophenyl)-biguanide, a potent high affinity 5-HT3 receptor agonist</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1990-06-21</date><risdate>1990</risdate><volume>182</volume><issue>1</issue><spage>193</spage><epage>197</epage><pages>193-197</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>1-(m-Chlorophenyl)-biguanide (mCPBG) was examined and compared with three 5-HT3 receptor agonists in three 5-HT3 receptor models. mCPBG inhibited [3H]GR67330 binding to 5-HT3 receptors with high affinity (IC50 1.5 nM). mCPBG depolarized the rat vagus nerve with an EC50 one tenth of that for 5-HT (0.05 vs. 0.46 microM); the maximum depolarization was approximately half that for 5-HT. The mCPBG depolarization was potently blocked by the selective 5-HT3 antagonist, ondansetron (pKB 8.6 +/- 0.1). In anaesthetised cats, mCPBG potently evoked the Bezold-Jarisch reflex which was blocked by low doses of ondansetron (10 micrograms/kg i.v.). It is concluded that mCPBG is a potent, high affinity 5-HT3 receptor agonist.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>2144822</pmid><doi>10.1016/0014-2999(90)90513-6</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0014-2999 |
| ispartof | European journal of pharmacology, 1990-06, Vol.182 (1), p.193-197 |
| issn | 0014-2999 1879-0712 |
| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Anesthesia Animals Biguanides - pharmacology Binding, Competitive - drug effects Biological and medical sciences Cats Heart Rate - drug effects Imidazoles - pharmacology In Vitro Techniques Male Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Ondansetron Pharmacology. Drug treatments Rats Receptors, Serotonin - drug effects Reflex - drug effects Serotoninergic system Vagus Nerve - drug effects Vagus Nerve - metabolism |
| title | 1-(m-clorophenyl)-biguanide, a potent high affinity 5-HT3 receptor agonist |
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