Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex
Although the H 2 subclass of histamine receptor has been revealed by classical pharmacological approaches 1,2 , the direct identification of this adenylate cyclase-linked receptor has, despite much effort, remained elusive. Initial studies using 3 H-metiamide and 3 H-histamine 3,4 and, subsequently,...
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| Veröffentlicht in: | Nature (London) 1983-07, Vol.304 (5921), p.65-67 |
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| container_issue | 5921 |
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| container_title | Nature (London) |
| container_volume | 304 |
| creator | Gajtkowski, Gillian A. Norris, D. B. Rising, T. J. Wood, T. P. |
| description | Although the H
2
subclass of histamine receptor has been revealed by classical pharmacological approaches
1,2
, the direct identification of this adenylate cyclase-linked receptor has, despite much effort, remained elusive. Initial studies using
3
H-metiamide and
3
H-histamine
3,4
and, subsequently, work from our own laboratory and others using
3
H-cimetidine
5–8
and
3
H-ranitidine
9
in various tissues, has shown the unsuitability of these ligands for labelling the H
2
receptor. We report here our results using
3
H-tiotidine, a more potent H
2
-antagonist than either cimetidine or ranitidine
10
, and show that this ligand meets the criteria for labelling the H
2
receptor in guinea pig cerebral cortex membranes. |
| doi_str_mv | 10.1038/304065a0 |
| format | Article |
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2
subclass of histamine receptor has been revealed by classical pharmacological approaches
1,2
, the direct identification of this adenylate cyclase-linked receptor has, despite much effort, remained elusive. Initial studies using
3
H-metiamide and
3
H-histamine
3,4
and, subsequently, work from our own laboratory and others using
3
H-cimetidine
5–8
and
3
H-ranitidine
9
in various tissues, has shown the unsuitability of these ligands for labelling the H
2
receptor. We report here our results using
3
H-tiotidine, a more potent H
2
-antagonist than either cimetidine or ranitidine
10
, and show that this ligand meets the criteria for labelling the H
2
receptor in guinea pig cerebral cortex membranes.</description><identifier>ISSN: 0028-0836</identifier><identifier>EISSN: 1476-4687</identifier><identifier>DOI: 10.1038/304065a0</identifier><identifier>PMID: 6135157</identifier><language>eng</language><publisher>London: Nature Publishing Group UK</publisher><subject>Animals ; Binding, Competitive ; Cerebral Cortex - metabolism ; Cimetidine - analogs & derivatives ; Guanidines - metabolism ; Guinea Pigs ; Histamine H2 Antagonists - metabolism ; Humanities and Social Sciences ; Kinetics ; letter ; multidisciplinary ; Receptors, Histamine - metabolism ; Receptors, Histamine H2 - metabolism ; Science ; Structure-Activity Relationship ; Thiazoles - metabolism</subject><ispartof>Nature (London), 1983-07, Vol.304 (5921), p.65-67</ispartof><rights>Springer Nature Limited 1983</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c2250-5b4a356868af76b4e897dad5b1b9d44ea470f0ae3a384b9689c3b168d3ee05d63</citedby><cites>FETCH-LOGICAL-c2250-5b4a356868af76b4e897dad5b1b9d44ea470f0ae3a384b9689c3b168d3ee05d63</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1038/304065a0$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1038/304065a0$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,776,780,27901,27902,41464,42533,51294</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6135157$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Gajtkowski, Gillian A.</creatorcontrib><creatorcontrib>Norris, D. B.</creatorcontrib><creatorcontrib>Rising, T. J.</creatorcontrib><creatorcontrib>Wood, T. P.</creatorcontrib><title>Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex</title><title>Nature (London)</title><addtitle>Nature</addtitle><addtitle>Nature</addtitle><description>Although the H
2
subclass of histamine receptor has been revealed by classical pharmacological approaches
1,2
, the direct identification of this adenylate cyclase-linked receptor has, despite much effort, remained elusive. Initial studies using
3
H-metiamide and
3
H-histamine
3,4
and, subsequently, work from our own laboratory and others using
3
H-cimetidine
5–8
and
3
H-ranitidine
9
in various tissues, has shown the unsuitability of these ligands for labelling the H
2
receptor. We report here our results using
3
H-tiotidine, a more potent H
2
-antagonist than either cimetidine or ranitidine
10
, and show that this ligand meets the criteria for labelling the H
2
receptor in guinea pig cerebral cortex membranes.</description><subject>Animals</subject><subject>Binding, Competitive</subject><subject>Cerebral Cortex - metabolism</subject><subject>Cimetidine - analogs & derivatives</subject><subject>Guanidines - metabolism</subject><subject>Guinea Pigs</subject><subject>Histamine H2 Antagonists - metabolism</subject><subject>Humanities and Social Sciences</subject><subject>Kinetics</subject><subject>letter</subject><subject>multidisciplinary</subject><subject>Receptors, Histamine - metabolism</subject><subject>Receptors, Histamine H2 - metabolism</subject><subject>Science</subject><subject>Structure-Activity Relationship</subject><subject>Thiazoles - metabolism</subject><issn>0028-0836</issn><issn>1476-4687</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1983</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNplkE9LAzEUxIMotVbBLyDkJHpYfWn-bPYoRa1Q8KCCtyXJvq0p7WZNdkG_vVtavXh6zJsfAzOEnDO4YcD1LQcBSho4IGMmcpUJpfNDMgaY6gw0V8fkJKUVAEiWixEZKcYlk_mYvL-06HztHbW-qXyzpKGmfJ51PnR-0Ei7QD986sxmK-ZTGtFh24WYqG_osh--hrZ-SR1GtNGsqQuxw69TclSbdcKz_Z2Qt4f719k8Wzw_Ps3uFpmbTiVk0grDpdJKmzpXVqAu8spU0jJbVEKgETnUYJAbroUtlC4ct0zpiiOCrBSfkMtdbhvDZ4-pKzc-OVyvTYOhT6UGKYRkxQBe7UAXQ0oR67KNfmPid8mg3I5Y_o44oBf7zN5usPoD96sN_vXOT4PTLDGWq9DHZqj5P-sH1rJ4iQ</recordid><startdate>19830701</startdate><enddate>19830701</enddate><creator>Gajtkowski, Gillian A.</creator><creator>Norris, D. B.</creator><creator>Rising, T. J.</creator><creator>Wood, T. P.</creator><general>Nature Publishing Group UK</general><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>19830701</creationdate><title>Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex</title><author>Gajtkowski, Gillian A. ; Norris, D. B. ; Rising, T. J. ; Wood, T. P.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c2250-5b4a356868af76b4e897dad5b1b9d44ea470f0ae3a384b9689c3b168d3ee05d63</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1983</creationdate><topic>Animals</topic><topic>Binding, Competitive</topic><topic>Cerebral Cortex - metabolism</topic><topic>Cimetidine - analogs & derivatives</topic><topic>Guanidines - metabolism</topic><topic>Guinea Pigs</topic><topic>Histamine H2 Antagonists - metabolism</topic><topic>Humanities and Social Sciences</topic><topic>Kinetics</topic><topic>letter</topic><topic>multidisciplinary</topic><topic>Receptors, Histamine - metabolism</topic><topic>Receptors, Histamine H2 - metabolism</topic><topic>Science</topic><topic>Structure-Activity Relationship</topic><topic>Thiazoles - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Gajtkowski, Gillian A.</creatorcontrib><creatorcontrib>Norris, D. B.</creatorcontrib><creatorcontrib>Rising, T. J.</creatorcontrib><creatorcontrib>Wood, T. P.</creatorcontrib><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>Nature (London)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Gajtkowski, Gillian A.</au><au>Norris, D. B.</au><au>Rising, T. J.</au><au>Wood, T. P.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex</atitle><jtitle>Nature (London)</jtitle><stitle>Nature</stitle><addtitle>Nature</addtitle><date>1983-07-01</date><risdate>1983</risdate><volume>304</volume><issue>5921</issue><spage>65</spage><epage>67</epage><pages>65-67</pages><issn>0028-0836</issn><eissn>1476-4687</eissn><abstract>Although the H
2
subclass of histamine receptor has been revealed by classical pharmacological approaches
1,2
, the direct identification of this adenylate cyclase-linked receptor has, despite much effort, remained elusive. Initial studies using
3
H-metiamide and
3
H-histamine
3,4
and, subsequently, work from our own laboratory and others using
3
H-cimetidine
5–8
and
3
H-ranitidine
9
in various tissues, has shown the unsuitability of these ligands for labelling the H
2
receptor. We report here our results using
3
H-tiotidine, a more potent H
2
-antagonist than either cimetidine or ranitidine
10
, and show that this ligand meets the criteria for labelling the H
2
receptor in guinea pig cerebral cortex membranes.</abstract><cop>London</cop><pub>Nature Publishing Group UK</pub><pmid>6135157</pmid><doi>10.1038/304065a0</doi><tpages>3</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0028-0836 |
| ispartof | Nature (London), 1983-07, Vol.304 (5921), p.65-67 |
| issn | 0028-0836 1476-4687 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_80544519 |
| source | MEDLINE; Springer Nature - Complete Springer Journals; Nature Journals Online |
| subjects | Animals Binding, Competitive Cerebral Cortex - metabolism Cimetidine - analogs & derivatives Guanidines - metabolism Guinea Pigs Histamine H2 Antagonists - metabolism Humanities and Social Sciences Kinetics letter multidisciplinary Receptors, Histamine - metabolism Receptors, Histamine H2 - metabolism Science Structure-Activity Relationship Thiazoles - metabolism |
| title | Specific binding of 3H-tiotidine to histamine H2 receptors in guinea pig cerebral cortex |
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