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Characterization and distribution of putative 5‐ht7 receptors in guinea‐pig brain
1 In the presence of (−)−cyanopindolol (1.0 μM) and sumatriptan (1.0 μM), 0.5 nM [3H]‐carboxamidotryptamine ([3H]‐5‐CT) labelled a single population of receptors in guinea‐pig cerebral cortex membranes. 2 5‐HT‐displaceable binding was rapid, saturable and reversible. A high affinity binding site was...
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| Published in: | British journal of pharmacology 1995-05, Vol.115 (1), p.107-116 |
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| container_title | British journal of pharmacology |
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| creator | To, Z.P. Bonhaus, D.W. Eglen, R.M. Jakeman, L.B. |
| description | 1
In the presence of (−)−cyanopindolol (1.0 μM) and sumatriptan (1.0 μM), 0.5 nM [3H]‐carboxamidotryptamine ([3H]‐5‐CT) labelled a single population of receptors in guinea‐pig cerebral cortex membranes.
2
5‐HT‐displaceable binding was rapid, saturable and reversible. A high affinity binding site was characterized both by equilibrium saturation (Kd = 0.76 ± 0.28 nM; Bmax = 68.1 ± 26.7 fmol mg−1 protein) and kinetic (Kd = 0.18 ± 0.05 nM) analysis. The pharmacological profile of this site was similar to the profile obtained in transfected CHO‐K1 cells expressing guinea‐pig 5‐ht7 receptors.
3
Autoradiographic analysis revealed a discrete localization of binding sites in guinea‐pig brain, with the highest density of sites in the medial thalamic nuclei and related limbic and cortical regions. Moderate levels of binding were detected in sensory relay nuclei, substantia nigra, hypothalamus, central grey and dorsal raphe nuclei. This distribution corresponded to that observed using in situ hybridization with [35S]‐UTP labelled riboprobes complementary to mRNA encoding the guinea‐pig 5‐ht7 receptor.
4
In conclusion, under appropriate conditions, [3H]‐5‐CT labelled a single population of saturable binding sites that corresponded to an endogenous 5‐ht7 receptor in guinea‐pig brain. The distribution of 5‐ht7 receptors in thalamocortical and limbic brain regions suggests a role for these receptors in sensory and affective behaviours. |
| doi_str_mv | 10.1111/j.1476-5381.1995.tb16327.x |
| format | article |
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In the presence of (−)−cyanopindolol (1.0 μM) and sumatriptan (1.0 μM), 0.5 nM [3H]‐carboxamidotryptamine ([3H]‐5‐CT) labelled a single population of receptors in guinea‐pig cerebral cortex membranes.
2
5‐HT‐displaceable binding was rapid, saturable and reversible. A high affinity binding site was characterized both by equilibrium saturation (Kd = 0.76 ± 0.28 nM; Bmax = 68.1 ± 26.7 fmol mg−1 protein) and kinetic (Kd = 0.18 ± 0.05 nM) analysis. The pharmacological profile of this site was similar to the profile obtained in transfected CHO‐K1 cells expressing guinea‐pig 5‐ht7 receptors.
3
Autoradiographic analysis revealed a discrete localization of binding sites in guinea‐pig brain, with the highest density of sites in the medial thalamic nuclei and related limbic and cortical regions. Moderate levels of binding were detected in sensory relay nuclei, substantia nigra, hypothalamus, central grey and dorsal raphe nuclei. This distribution corresponded to that observed using in situ hybridization with [35S]‐UTP labelled riboprobes complementary to mRNA encoding the guinea‐pig 5‐ht7 receptor.
4
In conclusion, under appropriate conditions, [3H]‐5‐CT labelled a single population of saturable binding sites that corresponded to an endogenous 5‐ht7 receptor in guinea‐pig brain. The distribution of 5‐ht7 receptors in thalamocortical and limbic brain regions suggests a role for these receptors in sensory and affective behaviours.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1995.tb16327.x</identifier><identifier>PMID: 7647964</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>5‐Carboxamidotryptamine ; 5‐HT receptors ; 5‐ht7 ; 5‐hydroxytryptamine ; Animals ; autoradiography ; Biological and medical sciences ; Brain - metabolism ; Central nervous system ; Central neurotransmission. Neuromudulation. Pathways and receptors ; CHO Cells ; Cloning, Molecular ; Cricetinae ; Fundamental and applied biological sciences. Psychology ; Guinea Pigs ; guinea‐pig limbic system ; guinea‐pig thalamus ; in situ hybridization ; Ligands ; Male ; Radioligand Assay ; Receptors, Serotonin - genetics ; Receptors, Serotonin - metabolism ; Recombinant Proteins - metabolism ; RNA, Messenger - metabolism ; Serotonin - analogs & derivatives ; Serotonin - metabolism ; Serotonin Receptor Agonists - metabolism ; Vertebrates: nervous system and sense organs</subject><ispartof>British journal of pharmacology, 1995-05, Vol.115 (1), p.107-116</ispartof><rights>1995 British Pharmacological Society</rights><rights>1995 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1908750/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1908750/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,27924,27925,53791,53793</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3565966$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7647964$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>To, Z.P.</creatorcontrib><creatorcontrib>Bonhaus, D.W.</creatorcontrib><creatorcontrib>Eglen, R.M.</creatorcontrib><creatorcontrib>Jakeman, L.B.</creatorcontrib><title>Characterization and distribution of putative 5‐ht7 receptors in guinea‐pig brain</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>1
In the presence of (−)−cyanopindolol (1.0 μM) and sumatriptan (1.0 μM), 0.5 nM [3H]‐carboxamidotryptamine ([3H]‐5‐CT) labelled a single population of receptors in guinea‐pig cerebral cortex membranes.
2
5‐HT‐displaceable binding was rapid, saturable and reversible. A high affinity binding site was characterized both by equilibrium saturation (Kd = 0.76 ± 0.28 nM; Bmax = 68.1 ± 26.7 fmol mg−1 protein) and kinetic (Kd = 0.18 ± 0.05 nM) analysis. The pharmacological profile of this site was similar to the profile obtained in transfected CHO‐K1 cells expressing guinea‐pig 5‐ht7 receptors.
3
Autoradiographic analysis revealed a discrete localization of binding sites in guinea‐pig brain, with the highest density of sites in the medial thalamic nuclei and related limbic and cortical regions. Moderate levels of binding were detected in sensory relay nuclei, substantia nigra, hypothalamus, central grey and dorsal raphe nuclei. This distribution corresponded to that observed using in situ hybridization with [35S]‐UTP labelled riboprobes complementary to mRNA encoding the guinea‐pig 5‐ht7 receptor.
4
In conclusion, under appropriate conditions, [3H]‐5‐CT labelled a single population of saturable binding sites that corresponded to an endogenous 5‐ht7 receptor in guinea‐pig brain. The distribution of 5‐ht7 receptors in thalamocortical and limbic brain regions suggests a role for these receptors in sensory and affective behaviours.</description><subject>5‐Carboxamidotryptamine</subject><subject>5‐HT receptors</subject><subject>5‐ht7</subject><subject>5‐hydroxytryptamine</subject><subject>Animals</subject><subject>autoradiography</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Central nervous system</subject><subject>Central neurotransmission. Neuromudulation. Pathways and receptors</subject><subject>CHO Cells</subject><subject>Cloning, Molecular</subject><subject>Cricetinae</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Guinea Pigs</subject><subject>guinea‐pig limbic system</subject><subject>guinea‐pig thalamus</subject><subject>in situ hybridization</subject><subject>Ligands</subject><subject>Male</subject><subject>Radioligand Assay</subject><subject>Receptors, Serotonin - genetics</subject><subject>Receptors, Serotonin - metabolism</subject><subject>Recombinant Proteins - metabolism</subject><subject>RNA, Messenger - metabolism</subject><subject>Serotonin - analogs & derivatives</subject><subject>Serotonin - metabolism</subject><subject>Serotonin Receptor Agonists - metabolism</subject><subject>Vertebrates: nervous system and sense organs</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><recordid>eNpVkc1u1DAURi0EKkPhEZAihNgl2PH_BgEjaCtVggVdWzeOM-NRJgm2U1pWPALPyJPgaaNR640tn0_ftXwQekNwRfJ6v6sIk6LkVJGKaM2r1BBBa1ndPEGrI3qKVhhjWRKi1HP0IsYdxhlKfoJOpGBSC7ZCV-stBLDJBf8bkh-HAoa2aH1MwTfz3cXYFdOcMrx2Bf_35-82ySI466Y0hlj4odjMfnCQyeQ3RRPADy_Rsw766F4t-ym6-vrlx_q8vPx2drH-dFlONL-kdExITDpJdCMEqamiNTDrGsZUh61gANZZ4TqppMDcaQZUa1krSltVi1bRU_Thvneam71rrRtSgN5Mwe8h3JoRvHlMBr81m_HaEI2V5DgXvFsKwvhzdjGZvY_W9T0MbpyjkZJxrWueg68fTjqOWD4y87cLh2ih7wIM1sdjjHLBtRA59vE-9sv37vaICTYHsWZnDvbMwZ45iDWLWHNjPn8_vzvS_-fkmvI</recordid><startdate>199505</startdate><enddate>199505</enddate><creator>To, Z.P.</creator><creator>Bonhaus, D.W.</creator><creator>Eglen, R.M.</creator><creator>Jakeman, L.B.</creator><general>Blackwell Publishing Ltd</general><general>Nature Publishing</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>199505</creationdate><title>Characterization and distribution of putative 5‐ht7 receptors in guinea‐pig brain</title><author>To, Z.P. ; Bonhaus, D.W. ; Eglen, R.M. ; Jakeman, L.B.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p3147-e46701f719b66123832a4ceb448f0c64aacec6ef787605e94a39972833d826d83</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1995</creationdate><topic>5‐Carboxamidotryptamine</topic><topic>5‐HT receptors</topic><topic>5‐ht7</topic><topic>5‐hydroxytryptamine</topic><topic>Animals</topic><topic>autoradiography</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Central nervous system</topic><topic>Central neurotransmission. Neuromudulation. Pathways and receptors</topic><topic>CHO Cells</topic><topic>Cloning, Molecular</topic><topic>Cricetinae</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Guinea Pigs</topic><topic>guinea‐pig limbic system</topic><topic>guinea‐pig thalamus</topic><topic>in situ hybridization</topic><topic>Ligands</topic><topic>Male</topic><topic>Radioligand Assay</topic><topic>Receptors, Serotonin - genetics</topic><topic>Receptors, Serotonin - metabolism</topic><topic>Recombinant Proteins - metabolism</topic><topic>RNA, Messenger - metabolism</topic><topic>Serotonin - analogs & derivatives</topic><topic>Serotonin - metabolism</topic><topic>Serotonin Receptor Agonists - metabolism</topic><topic>Vertebrates: nervous system and sense organs</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>To, Z.P.</creatorcontrib><creatorcontrib>Bonhaus, D.W.</creatorcontrib><creatorcontrib>Eglen, R.M.</creatorcontrib><creatorcontrib>Jakeman, L.B.</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>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>To, Z.P.</au><au>Bonhaus, D.W.</au><au>Eglen, R.M.</au><au>Jakeman, L.B.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Characterization and distribution of putative 5‐ht7 receptors in guinea‐pig brain</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1995-05</date><risdate>1995</risdate><volume>115</volume><issue>1</issue><spage>107</spage><epage>116</epage><pages>107-116</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>1
In the presence of (−)−cyanopindolol (1.0 μM) and sumatriptan (1.0 μM), 0.5 nM [3H]‐carboxamidotryptamine ([3H]‐5‐CT) labelled a single population of receptors in guinea‐pig cerebral cortex membranes.
2
5‐HT‐displaceable binding was rapid, saturable and reversible. A high affinity binding site was characterized both by equilibrium saturation (Kd = 0.76 ± 0.28 nM; Bmax = 68.1 ± 26.7 fmol mg−1 protein) and kinetic (Kd = 0.18 ± 0.05 nM) analysis. The pharmacological profile of this site was similar to the profile obtained in transfected CHO‐K1 cells expressing guinea‐pig 5‐ht7 receptors.
3
Autoradiographic analysis revealed a discrete localization of binding sites in guinea‐pig brain, with the highest density of sites in the medial thalamic nuclei and related limbic and cortical regions. Moderate levels of binding were detected in sensory relay nuclei, substantia nigra, hypothalamus, central grey and dorsal raphe nuclei. This distribution corresponded to that observed using in situ hybridization with [35S]‐UTP labelled riboprobes complementary to mRNA encoding the guinea‐pig 5‐ht7 receptor.
4
In conclusion, under appropriate conditions, [3H]‐5‐CT labelled a single population of saturable binding sites that corresponded to an endogenous 5‐ht7 receptor in guinea‐pig brain. The distribution of 5‐ht7 receptors in thalamocortical and limbic brain regions suggests a role for these receptors in sensory and affective behaviours.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>7647964</pmid><doi>10.1111/j.1476-5381.1995.tb16327.x</doi><tpages>10</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | 5‐Carboxamidotryptamine 5‐HT receptors 5‐ht7 5‐hydroxytryptamine Animals autoradiography Biological and medical sciences Brain - metabolism Central nervous system Central neurotransmission. Neuromudulation. Pathways and receptors CHO Cells Cloning, Molecular Cricetinae Fundamental and applied biological sciences. Psychology Guinea Pigs guinea‐pig limbic system guinea‐pig thalamus in situ hybridization Ligands Male Radioligand Assay Receptors, Serotonin - genetics Receptors, Serotonin - metabolism Recombinant Proteins - metabolism RNA, Messenger - metabolism Serotonin - analogs & derivatives Serotonin - metabolism Serotonin Receptor Agonists - metabolism Vertebrates: nervous system and sense organs |
| title | Characterization and distribution of putative 5‐ht7 receptors in guinea‐pig brain |
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