Evidence for a M1 muscarinic receptor on the endothelium of human pulmonary veins
To characterize the muscarinic receptors on human pulmonary veins associated with the acetylcholine (ACh)‐induced relaxation, isolated venous and arterial preparations were pre‐contracted with noradrenaline (10 μM) and were subsequently challenged with ACh in the absence or presence of selective mus...
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| description | To characterize the muscarinic receptors on human pulmonary veins associated with the acetylcholine (ACh)‐induced relaxation, isolated venous and arterial preparations were pre‐contracted with noradrenaline (10 μM) and were subsequently challenged with ACh in the absence or presence of selective muscarinic antagonists.
ACh relaxed venous preparations derived from human lung with a pD2 value of 5.82±0.09 (n=16). In venous preparations where the endothelium had been removed, the ACh relaxations were abolished (n=4). ACh relaxed arterial preparations with a pD2 value of 7.06±0.14 (n=5).
Atropine (1 μM), the non selective antagonist for muscarinic receptors, inhibited ACh‐induced relaxations in human pulmonary veins. The affinity value (pKB value) for atropine was: 8.64±0.10 (n=5). The selective muscarinic antagonists (darifenacin (M3), himbacine (M2,M4), methoctramine (M2) and pFHHSiD (M1,M3)) also inhibited ACh‐induced relaxations in venous preparations. The pKB values obtained for these antagonists were not those predicted for the involvement of M2–5 receptors in the ACh‐induced relaxation in human pulmonary veins.
The pKB value for darifenacin (1 μM) was significantly greater in human pulmonary arterial (8.63±0.14) than in venous (7.41±0.20) preparations derived from three lung samples.
In human pulmonary veins, the pKB values for pirenzepine (0.5 and 1 μM), a selective antagonist for M1 receptors, were: 7.89±0.24 (n=7) and 8.18±0.22 (n=5), respectively. In the venous preparations, the pKB values derived from the functional studies with all the different muscarinic antagonists used were correlated (r=0.89; P=0.04; slope=0.78) with the affinity values (pKi values) previously published for human cloned m1 receptors in CHO cells.
These results suggest that the relaxations induced by ACh are due to the activation of M1 receptors on endothelial cells in isolated human pulmonary veins.
British Journal of Pharmacology (2000) 130, 73–78; doi:10.1038/sj.bjp.0703301 |
| doi_str_mv | 10.1038/sj.bjp.0703301 |
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ACh relaxed venous preparations derived from human lung with a pD2 value of 5.82±0.09 (n=16). In venous preparations where the endothelium had been removed, the ACh relaxations were abolished (n=4). ACh relaxed arterial preparations with a pD2 value of 7.06±0.14 (n=5).
Atropine (1 μM), the non selective antagonist for muscarinic receptors, inhibited ACh‐induced relaxations in human pulmonary veins. The affinity value (pKB value) for atropine was: 8.64±0.10 (n=5). The selective muscarinic antagonists (darifenacin (M3), himbacine (M2,M4), methoctramine (M2) and pFHHSiD (M1,M3)) also inhibited ACh‐induced relaxations in venous preparations. The pKB values obtained for these antagonists were not those predicted for the involvement of M2–5 receptors in the ACh‐induced relaxation in human pulmonary veins.
The pKB value for darifenacin (1 μM) was significantly greater in human pulmonary arterial (8.63±0.14) than in venous (7.41±0.20) preparations derived from three lung samples.
In human pulmonary veins, the pKB values for pirenzepine (0.5 and 1 μM), a selective antagonist for M1 receptors, were: 7.89±0.24 (n=7) and 8.18±0.22 (n=5), respectively. In the venous preparations, the pKB values derived from the functional studies with all the different muscarinic antagonists used were correlated (r=0.89; P=0.04; slope=0.78) with the affinity values (pKi values) previously published for human cloned m1 receptors in CHO cells.
These results suggest that the relaxations induced by ACh are due to the activation of M1 receptors on endothelial cells in isolated human pulmonary veins.
British Journal of Pharmacology (2000) 130, 73–78; doi:10.1038/sj.bjp.0703301</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1038/sj.bjp.0703301</identifier><identifier>PMID: 10781000</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Acetylcholine ; Biological and medical sciences ; Blood vessels and receptors ; Cell receptors ; Cell structures and functions ; darifenacin ; endothelium ; Fundamental and applied biological sciences. Psychology ; himbacine ; human pulmonary artery ; human pulmonary vein ; methoctramine ; Molecular and cellular biology ; Monoamines receptors (catecholamine, serotonine, histamine, acetylcholine) ; muscarinic receptor ; pFHHSiD ; pirenzepine ; Vertebrates: cardiovascular system</subject><ispartof>British journal of pharmacology, 2000-05, Vol.130 (1), p.73-78</ispartof><rights>2000 Nature Publishing Group</rights><rights>2000 INIST-CNRS</rights><rights>Copyright Nature Publishing Group May 2000</rights><rights>Copyright 2000, Nature Publishing Group 2000 Nature Publishing Group</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/PMC1572048/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1572048/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,1417,1433,27923,27924,45573,45574,46408,46832,53790,53792</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1358017$$DView record in Pascal Francis$$Hfree_for_read</backlink></links><search><creatorcontrib>Walch, Laurence</creatorcontrib><creatorcontrib>Gascard, Jean‐Pierre</creatorcontrib><creatorcontrib>Dulmet, Elisabeth</creatorcontrib><creatorcontrib>Brink, Charles</creatorcontrib><creatorcontrib>Norel, Xavier</creatorcontrib><title>Evidence for a M1 muscarinic receptor on the endothelium of human pulmonary veins</title><title>British journal of pharmacology</title><description>To characterize the muscarinic receptors on human pulmonary veins associated with the acetylcholine (ACh)‐induced relaxation, isolated venous and arterial preparations were pre‐contracted with noradrenaline (10 μM) and were subsequently challenged with ACh in the absence or presence of selective muscarinic antagonists.
ACh relaxed venous preparations derived from human lung with a pD2 value of 5.82±0.09 (n=16). In venous preparations where the endothelium had been removed, the ACh relaxations were abolished (n=4). ACh relaxed arterial preparations with a pD2 value of 7.06±0.14 (n=5).
Atropine (1 μM), the non selective antagonist for muscarinic receptors, inhibited ACh‐induced relaxations in human pulmonary veins. The affinity value (pKB value) for atropine was: 8.64±0.10 (n=5). The selective muscarinic antagonists (darifenacin (M3), himbacine (M2,M4), methoctramine (M2) and pFHHSiD (M1,M3)) also inhibited ACh‐induced relaxations in venous preparations. The pKB values obtained for these antagonists were not those predicted for the involvement of M2–5 receptors in the ACh‐induced relaxation in human pulmonary veins.
The pKB value for darifenacin (1 μM) was significantly greater in human pulmonary arterial (8.63±0.14) than in venous (7.41±0.20) preparations derived from three lung samples.
In human pulmonary veins, the pKB values for pirenzepine (0.5 and 1 μM), a selective antagonist for M1 receptors, were: 7.89±0.24 (n=7) and 8.18±0.22 (n=5), respectively. In the venous preparations, the pKB values derived from the functional studies with all the different muscarinic antagonists used were correlated (r=0.89; P=0.04; slope=0.78) with the affinity values (pKi values) previously published for human cloned m1 receptors in CHO cells.
These results suggest that the relaxations induced by ACh are due to the activation of M1 receptors on endothelial cells in isolated human pulmonary veins.
British Journal of Pharmacology (2000) 130, 73–78; doi:10.1038/sj.bjp.0703301</description><subject>Acetylcholine</subject><subject>Biological and medical sciences</subject><subject>Blood vessels and receptors</subject><subject>Cell receptors</subject><subject>Cell structures and functions</subject><subject>darifenacin</subject><subject>endothelium</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>himbacine</subject><subject>human pulmonary artery</subject><subject>human pulmonary vein</subject><subject>methoctramine</subject><subject>Molecular and cellular biology</subject><subject>Monoamines receptors (catecholamine, serotonine, histamine, acetylcholine)</subject><subject>muscarinic receptor</subject><subject>pFHHSiD</subject><subject>pirenzepine</subject><subject>Vertebrates: cardiovascular system</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNpVkUFr3DAUhEVJaTbbXnsWJVdv37MsS74E0iVNCglNoDkLrS1lZWzJldYb9t9HJUtKTu_wDTPDG0K-IqwQmPye-tWmn1YggDHAD2SBlagLziSekAUAiAJRylNyllIPkKHgn8gpgpCY6YI8XO1dZ3xrqA2RanqHdJxTq6PzrqXRtGbaZRA83W0NNb4L-Q5uHmmwdDuP2tNpHsbgdTzQvXE-fSYfrR6S-XK8S_L48-rP-qa4_X39a315W_SsbJqi4rpEYTtpm5pLtuFYw6a1VaNL6EorBVZlTq87a7BtGqw1cqnLLOaW29KwJbl49Z3mzWi61vhd1IOaohtzFxW0U--Jd1v1FPYKuSihktng29Eghr-zSTvVhzn63FnlZiiB8TqLzo8inb8y2Kh969JbCjIuAUWWsVfZsxvM4T8G9W8llXqVV1LHldSP-xtkdcNeADCdhrk</recordid><startdate>200005</startdate><enddate>200005</enddate><creator>Walch, Laurence</creator><creator>Gascard, Jean‐Pierre</creator><creator>Dulmet, Elisabeth</creator><creator>Brink, Charles</creator><creator>Norel, Xavier</creator><general>Blackwell Publishing Ltd</general><general>Nature Publishing</general><scope>IQODW</scope><scope>3V.</scope><scope>7QP</scope><scope>7RV</scope><scope>7TK</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M7P</scope><scope>NAPCQ</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>5PM</scope></search><sort><creationdate>200005</creationdate><title>Evidence for a M1 muscarinic receptor on the endothelium of human pulmonary veins</title><author>Walch, Laurence ; Gascard, Jean‐Pierre ; Dulmet, Elisabeth ; Brink, Charles ; Norel, Xavier</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-j3299-45a217fd8f96583b5160bcf49a20d2f87142ece6dfe1c9916a158a29655f5f2e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Acetylcholine</topic><topic>Biological and medical sciences</topic><topic>Blood vessels and receptors</topic><topic>Cell receptors</topic><topic>Cell structures and functions</topic><topic>darifenacin</topic><topic>endothelium</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>himbacine</topic><topic>human pulmonary artery</topic><topic>human pulmonary vein</topic><topic>methoctramine</topic><topic>Molecular and cellular biology</topic><topic>Monoamines receptors (catecholamine, serotonine, histamine, acetylcholine)</topic><topic>muscarinic receptor</topic><topic>pFHHSiD</topic><topic>pirenzepine</topic><topic>Vertebrates: cardiovascular system</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Walch, Laurence</creatorcontrib><creatorcontrib>Gascard, Jean‐Pierre</creatorcontrib><creatorcontrib>Dulmet, Elisabeth</creatorcontrib><creatorcontrib>Brink, Charles</creatorcontrib><creatorcontrib>Norel, Xavier</creatorcontrib><collection>Pascal-Francis</collection><collection>ProQuest Central (Corporate)</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Nursing & Allied Health Database</collection><collection>Neurosciences Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Natural Science Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Biological Science Database</collection><collection>Nursing & Allied Health Premium</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</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>Walch, Laurence</au><au>Gascard, Jean‐Pierre</au><au>Dulmet, Elisabeth</au><au>Brink, Charles</au><au>Norel, Xavier</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evidence for a M1 muscarinic receptor on the endothelium of human pulmonary veins</atitle><jtitle>British journal of pharmacology</jtitle><date>2000-05</date><risdate>2000</risdate><volume>130</volume><issue>1</issue><spage>73</spage><epage>78</epage><pages>73-78</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>To characterize the muscarinic receptors on human pulmonary veins associated with the acetylcholine (ACh)‐induced relaxation, isolated venous and arterial preparations were pre‐contracted with noradrenaline (10 μM) and were subsequently challenged with ACh in the absence or presence of selective muscarinic antagonists.
ACh relaxed venous preparations derived from human lung with a pD2 value of 5.82±0.09 (n=16). In venous preparations where the endothelium had been removed, the ACh relaxations were abolished (n=4). ACh relaxed arterial preparations with a pD2 value of 7.06±0.14 (n=5).
Atropine (1 μM), the non selective antagonist for muscarinic receptors, inhibited ACh‐induced relaxations in human pulmonary veins. The affinity value (pKB value) for atropine was: 8.64±0.10 (n=5). The selective muscarinic antagonists (darifenacin (M3), himbacine (M2,M4), methoctramine (M2) and pFHHSiD (M1,M3)) also inhibited ACh‐induced relaxations in venous preparations. The pKB values obtained for these antagonists were not those predicted for the involvement of M2–5 receptors in the ACh‐induced relaxation in human pulmonary veins.
The pKB value for darifenacin (1 μM) was significantly greater in human pulmonary arterial (8.63±0.14) than in venous (7.41±0.20) preparations derived from three lung samples.
In human pulmonary veins, the pKB values for pirenzepine (0.5 and 1 μM), a selective antagonist for M1 receptors, were: 7.89±0.24 (n=7) and 8.18±0.22 (n=5), respectively. In the venous preparations, the pKB values derived from the functional studies with all the different muscarinic antagonists used were correlated (r=0.89; P=0.04; slope=0.78) with the affinity values (pKi values) previously published for human cloned m1 receptors in CHO cells.
These results suggest that the relaxations induced by ACh are due to the activation of M1 receptors on endothelial cells in isolated human pulmonary veins.
British Journal of Pharmacology (2000) 130, 73–78; doi:10.1038/sj.bjp.0703301</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>10781000</pmid><doi>10.1038/sj.bjp.0703301</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Acetylcholine Biological and medical sciences Blood vessels and receptors Cell receptors Cell structures and functions darifenacin endothelium Fundamental and applied biological sciences. Psychology himbacine human pulmonary artery human pulmonary vein methoctramine Molecular and cellular biology Monoamines receptors (catecholamine, serotonine, histamine, acetylcholine) muscarinic receptor pFHHSiD pirenzepine Vertebrates: cardiovascular system |
| title | Evidence for a M1 muscarinic receptor on the endothelium of human pulmonary veins |
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