Pharmacological Differences Between Rat and Human Endothelin B Receptors
Cloned rat and human endothelin-B receptors (ETBR) were utilized to determine if there are significant pharmacological differences between highly homologous ETBR from different species. Recombinant rat and human ETBR were expressed in CHO-K1 cells, and radioligand binding studies were carried out wi...
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| Veröffentlicht in: | Biochemical and biophysical research communications 1995-04, Vol.209 (2), p.506-512 |
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| container_title | Biochemical and biophysical research communications |
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| creator | Reynolds, E.E. Hwang, O. Flynn, M.A. Welch, K.M. Cody, W.L. Steinbaugh, B. He, J.X. Chung, F.Z. Doherty, A.M. |
| description | Cloned rat and human endothelin-B receptors (ETBR) were utilized to determine if there are significant pharmacological differences between highly homologous ETBR from different species. Recombinant rat and human ETBR were expressed in CHO-K1 cells, and radioligand binding studies were carried out with [125I]-ET-3 to determine the affinities of various ET receptor agonists and antagonists for rat and human ETBR. These receptors had similar affinities for a number of ETBR agonists (ET-1, ET-3, S6C, BQ 3020) and antagonists (Ro 47-0203, PD 142893). However, several peptide (PD 147452, PD 151583, BQ 788) and non-peptide (PD 156707, SE 209670) antagonists had different affinities for rat and human ETBR, with differences in Ki values between species ranging from 4.1- to 53.4-fold. The ETBR-selective agonist IRL 1620 also had a 5.7-fold higher affinity for rat ETBR than human ETBR. Thus despite their high degree of homology, rat and human ETBR show significant pharmacological differences with respect to both antagonist and agonist binding. |
| doi_str_mv | 10.1006/bbrc.1995.1530 |
| format | Article |
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Recombinant rat and human ETBR were expressed in CHO-K1 cells, and radioligand binding studies were carried out with [125I]-ET-3 to determine the affinities of various ET receptor agonists and antagonists for rat and human ETBR. These receptors had similar affinities for a number of ETBR agonists (ET-1, ET-3, S6C, BQ 3020) and antagonists (Ro 47-0203, PD 142893). However, several peptide (PD 147452, PD 151583, BQ 788) and non-peptide (PD 156707, SE 209670) antagonists had different affinities for rat and human ETBR, with differences in Ki values between species ranging from 4.1- to 53.4-fold. The ETBR-selective agonist IRL 1620 also had a 5.7-fold higher affinity for rat ETBR than human ETBR. Thus despite their high degree of homology, rat and human ETBR show significant pharmacological differences with respect to both antagonist and agonist binding.</description><identifier>ISSN: 0006-291X</identifier><identifier>EISSN: 1090-2104</identifier><identifier>DOI: 10.1006/bbrc.1995.1530</identifier><identifier>PMID: 7733918</identifier><language>eng</language><publisher>United States: Elsevier Inc</publisher><subject>Amino Acid Sequence ; Animals ; Binding, Competitive ; Endothelin Receptor Antagonists ; Endothelins - metabolism ; Humans ; Molecular Sequence Data ; Radioligand Assay ; Rats ; Receptor, Endothelin B ; Receptors, Endothelin - agonists ; Receptors, Endothelin - metabolism ; Recombinant Proteins ; Species Specificity</subject><ispartof>Biochemical and biophysical research communications, 1995-04, Vol.209 (2), p.506-512</ispartof><rights>1995 Academic Press</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c339t-d6f1a9284be26c4faef56c17a6ceb10b2baaa3109c0d1e94a2ed3f307ba593553</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1006/bbrc.1995.1530$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,777,781,3537,27905,27906,45976</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7733918$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Reynolds, E.E.</creatorcontrib><creatorcontrib>Hwang, O.</creatorcontrib><creatorcontrib>Flynn, M.A.</creatorcontrib><creatorcontrib>Welch, K.M.</creatorcontrib><creatorcontrib>Cody, W.L.</creatorcontrib><creatorcontrib>Steinbaugh, B.</creatorcontrib><creatorcontrib>He, J.X.</creatorcontrib><creatorcontrib>Chung, F.Z.</creatorcontrib><creatorcontrib>Doherty, A.M.</creatorcontrib><title>Pharmacological Differences Between Rat and Human Endothelin B Receptors</title><title>Biochemical and biophysical research communications</title><addtitle>Biochem Biophys Res Commun</addtitle><description>Cloned rat and human endothelin-B receptors (ETBR) were utilized to determine if there are significant pharmacological differences between highly homologous ETBR from different species. Recombinant rat and human ETBR were expressed in CHO-K1 cells, and radioligand binding studies were carried out with [125I]-ET-3 to determine the affinities of various ET receptor agonists and antagonists for rat and human ETBR. These receptors had similar affinities for a number of ETBR agonists (ET-1, ET-3, S6C, BQ 3020) and antagonists (Ro 47-0203, PD 142893). However, several peptide (PD 147452, PD 151583, BQ 788) and non-peptide (PD 156707, SE 209670) antagonists had different affinities for rat and human ETBR, with differences in Ki values between species ranging from 4.1- to 53.4-fold. The ETBR-selective agonist IRL 1620 also had a 5.7-fold higher affinity for rat ETBR than human ETBR. Thus despite their high degree of homology, rat and human ETBR show significant pharmacological differences with respect to both antagonist and agonist binding.</description><subject>Amino Acid Sequence</subject><subject>Animals</subject><subject>Binding, Competitive</subject><subject>Endothelin Receptor Antagonists</subject><subject>Endothelins - metabolism</subject><subject>Humans</subject><subject>Molecular Sequence Data</subject><subject>Radioligand Assay</subject><subject>Rats</subject><subject>Receptor, Endothelin B</subject><subject>Receptors, Endothelin - agonists</subject><subject>Receptors, Endothelin - metabolism</subject><subject>Recombinant Proteins</subject><subject>Species Specificity</subject><issn>0006-291X</issn><issn>1090-2104</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kL1PwzAQxS0EKqWwsiFlYkuw43x5pKVQpEqgCiQ26-xcqFESFzsB8d-TqBUbt9zw3r3T-xFyyWjEKM1ulHI6YkKkEUs5PSJTRgUNY0aTYzKlgyOMBXs7JWfef1DKWJKJCZnkOeeCFVOyet6Ca0Db2r4bDXVwZ6oKHbYafTDH7huxDTbQBdCWwapvoA2WbWm7LdamDebBBjXuOuv8OTmpoPZ4cdgz8nq_fFmswvXTw-Pidh3q4WMXllnFQMRFojDOdFIBVmmmWQ6ZRsWoihUA8KGDpiVDkUCMJa84zRWkgqcpn5Hrfe7O2c8efScb4zXWNbRoey_zPE4KPsyMRHujdtZ7h5XcOdOA-5GMyhGdHNHJEZ0c0Q0HV4fkXjVY_tkPrAa92Os41Psy6KTXZgRVGoe6k6U1_0X_AoaPfZE</recordid><startdate>19950417</startdate><enddate>19950417</enddate><creator>Reynolds, E.E.</creator><creator>Hwang, O.</creator><creator>Flynn, M.A.</creator><creator>Welch, K.M.</creator><creator>Cody, W.L.</creator><creator>Steinbaugh, B.</creator><creator>He, J.X.</creator><creator>Chung, F.Z.</creator><creator>Doherty, A.M.</creator><general>Elsevier Inc</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>19950417</creationdate><title>Pharmacological Differences Between Rat and Human Endothelin B Receptors</title><author>Reynolds, E.E. ; Hwang, O. ; Flynn, M.A. ; Welch, K.M. ; Cody, W.L. ; Steinbaugh, B. ; He, J.X. ; Chung, F.Z. ; Doherty, A.M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c339t-d6f1a9284be26c4faef56c17a6ceb10b2baaa3109c0d1e94a2ed3f307ba593553</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1995</creationdate><topic>Amino Acid Sequence</topic><topic>Animals</topic><topic>Binding, Competitive</topic><topic>Endothelin Receptor Antagonists</topic><topic>Endothelins - metabolism</topic><topic>Humans</topic><topic>Molecular Sequence Data</topic><topic>Radioligand Assay</topic><topic>Rats</topic><topic>Receptor, Endothelin B</topic><topic>Receptors, Endothelin - agonists</topic><topic>Receptors, Endothelin - metabolism</topic><topic>Recombinant Proteins</topic><topic>Species Specificity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Reynolds, E.E.</creatorcontrib><creatorcontrib>Hwang, O.</creatorcontrib><creatorcontrib>Flynn, M.A.</creatorcontrib><creatorcontrib>Welch, K.M.</creatorcontrib><creatorcontrib>Cody, W.L.</creatorcontrib><creatorcontrib>Steinbaugh, B.</creatorcontrib><creatorcontrib>He, J.X.</creatorcontrib><creatorcontrib>Chung, F.Z.</creatorcontrib><creatorcontrib>Doherty, A.M.</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>Biochemical and biophysical research communications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Reynolds, E.E.</au><au>Hwang, O.</au><au>Flynn, M.A.</au><au>Welch, K.M.</au><au>Cody, W.L.</au><au>Steinbaugh, B.</au><au>He, J.X.</au><au>Chung, F.Z.</au><au>Doherty, A.M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacological Differences Between Rat and Human Endothelin B Receptors</atitle><jtitle>Biochemical and biophysical research communications</jtitle><addtitle>Biochem Biophys Res Commun</addtitle><date>1995-04-17</date><risdate>1995</risdate><volume>209</volume><issue>2</issue><spage>506</spage><epage>512</epage><pages>506-512</pages><issn>0006-291X</issn><eissn>1090-2104</eissn><abstract>Cloned rat and human endothelin-B receptors (ETBR) were utilized to determine if there are significant pharmacological differences between highly homologous ETBR from different species. Recombinant rat and human ETBR were expressed in CHO-K1 cells, and radioligand binding studies were carried out with [125I]-ET-3 to determine the affinities of various ET receptor agonists and antagonists for rat and human ETBR. These receptors had similar affinities for a number of ETBR agonists (ET-1, ET-3, S6C, BQ 3020) and antagonists (Ro 47-0203, PD 142893). However, several peptide (PD 147452, PD 151583, BQ 788) and non-peptide (PD 156707, SE 209670) antagonists had different affinities for rat and human ETBR, with differences in Ki values between species ranging from 4.1- to 53.4-fold. The ETBR-selective agonist IRL 1620 also had a 5.7-fold higher affinity for rat ETBR than human ETBR. Thus despite their high degree of homology, rat and human ETBR show significant pharmacological differences with respect to both antagonist and agonist binding.</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>7733918</pmid><doi>10.1006/bbrc.1995.1530</doi><tpages>7</tpages></addata></record> |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Amino Acid Sequence Animals Binding, Competitive Endothelin Receptor Antagonists Endothelins - metabolism Humans Molecular Sequence Data Radioligand Assay Rats Receptor, Endothelin B Receptors, Endothelin - agonists Receptors, Endothelin - metabolism Recombinant Proteins Species Specificity |
| title | Pharmacological Differences Between Rat and Human Endothelin B Receptors |
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