Histamine receptor subtypes mediating hyperpolarization in the isolated, perfused rat mesenteric pre-arteriolar bed
Histamine is a general dilator of rat blood vessels. We investigated the relative contribution of receptor subtypes to the rat mesenteric dilator responses initiated by histamine and related agonists. Histamine initiated dose, and endothelium-dependent, dilation of constricted mesenteric beds with a...
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| Veröffentlicht in: | European journal of pharmacology 1998-04, Vol.347 (2), p.237-244 |
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| description | Histamine is a general dilator of rat blood vessels. We investigated the relative contribution of receptor subtypes to the rat mesenteric dilator responses initiated by histamine and related agonists. Histamine initiated dose, and endothelium-dependent, dilation of constricted mesenteric beds with an ED
50 of 0.4±0.1 nmol. The ED
50 was increased 10-fold by 0.1
μM chlorpheniramine (a histamine H
1-receptor selective antagonist). Histamine H
2 receptor blockade with tiotidine (0.1
μM) slightly decreased, while thioperamide (1
μM), a selective histamine H
3 receptor antagonist, did not block histamine-induced dilation. Mesenteric bed dilation initiated by histamine H
2 receptor selective agonists, amthamine and dimaprit, were antagonized markedly by tiotidine. However, the dilation initiated by the putative histamine H
3 receptor selective agonists,
R(−)- or
S(+)-
α-methylhistamine and imetit were not affected by thioperamide (1
μM). Histamine H
2- and H
3-receptor mediated dilator effects were endothelium-independent and were blocked by either excess (80 mM) extracellular K
+, or 1 mM tetrabutylammonium (a non-selective K
+ channel blocker), as well as by 1
μM dequalinium, a non-peptide blocker of the small conductance Ca
2+-activated (SK
Ca) K
+ channels. We conclude that (i) histamine H
1 receptor subtype predominantly mediates endothelium-dependent dilator effect of histamine, and (ii) vascular hyperpolarization through opening of K
+ channels (SK
Ca) mediate the dilator responses to histamine H
2 receptor (amthamine and dimaprit) and the putative histamine H
3 receptor (
R(−)-
α-methylhistamine and imetit) agonists. |
| doi_str_mv | 10.1016/S0014-2999(98)00119-8 |
| format | Article |
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50 of 0.4±0.1 nmol. The ED
50 was increased 10-fold by 0.1
μM chlorpheniramine (a histamine H
1-receptor selective antagonist). Histamine H
2 receptor blockade with tiotidine (0.1
μM) slightly decreased, while thioperamide (1
μM), a selective histamine H
3 receptor antagonist, did not block histamine-induced dilation. Mesenteric bed dilation initiated by histamine H
2 receptor selective agonists, amthamine and dimaprit, were antagonized markedly by tiotidine. However, the dilation initiated by the putative histamine H
3 receptor selective agonists,
R(−)- or
S(+)-
α-methylhistamine and imetit were not affected by thioperamide (1
μM). Histamine H
2- and H
3-receptor mediated dilator effects were endothelium-independent and were blocked by either excess (80 mM) extracellular K
+, or 1 mM tetrabutylammonium (a non-selective K
+ channel blocker), as well as by 1
μM dequalinium, a non-peptide blocker of the small conductance Ca
2+-activated (SK
Ca) K
+ channels. We conclude that (i) histamine H
1 receptor subtype predominantly mediates endothelium-dependent dilator effect of histamine, and (ii) vascular hyperpolarization through opening of K
+ channels (SK
Ca) mediate the dilator responses to histamine H
2 receptor (amthamine and dimaprit) and the putative histamine H
3 receptor (
R(−)-
α-methylhistamine and imetit) agonists.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/S0014-2999(98)00119-8</identifier><identifier>PMID: 9653888</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Animals ; Arterioles - drug effects ; Arterioles - physiology ; Biological and medical sciences ; Dose-Response Relationship, Drug ; Electrophysiology ; Histamine - pharmacology ; Histamine Agonists - pharmacology ; Histamine and antagonists. Allergy ; Histamine Antagonists - pharmacology ; Histamine receptor subtype ; Male ; Medical sciences ; Perfused mesenteric bed ; Perfusion ; Pharmacology. Drug treatments ; Potassium - metabolism ; Potassium Channel Blockers ; Potassium Channels - metabolism ; Rats ; Rats, Sprague-Dawley ; Receptors, Histamine - physiology ; Splanchnic Circulation - drug effects ; Splanchnic Circulation - physiology ; Vascular hyperpolarization ; Vasodilation - drug effects ; Vasodilation - physiology</subject><ispartof>European journal of pharmacology, 1998-04, Vol.347 (2), p.237-244</ispartof><rights>1998 Elsevier Science B.V.</rights><rights>1998 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c455t-ec263af8079f6ae6b7a152199b0c201fc055ad14c74d9a0040145e321cf8ecf73</citedby><cites>FETCH-LOGICAL-c455t-ec263af8079f6ae6b7a152199b0c201fc055ad14c74d9a0040145e321cf8ecf73</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0014-2999(98)00119-8$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2304856$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9653888$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Adeagbo, Ayotunde S.O</creatorcontrib><creatorcontrib>Oriowo, Mabayoje A</creatorcontrib><title>Histamine receptor subtypes mediating hyperpolarization in the isolated, perfused rat mesenteric pre-arteriolar bed</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Histamine is a general dilator of rat blood vessels. We investigated the relative contribution of receptor subtypes to the rat mesenteric dilator responses initiated by histamine and related agonists. Histamine initiated dose, and endothelium-dependent, dilation of constricted mesenteric beds with an ED
50 of 0.4±0.1 nmol. The ED
50 was increased 10-fold by 0.1
μM chlorpheniramine (a histamine H
1-receptor selective antagonist). Histamine H
2 receptor blockade with tiotidine (0.1
μM) slightly decreased, while thioperamide (1
μM), a selective histamine H
3 receptor antagonist, did not block histamine-induced dilation. Mesenteric bed dilation initiated by histamine H
2 receptor selective agonists, amthamine and dimaprit, were antagonized markedly by tiotidine. However, the dilation initiated by the putative histamine H
3 receptor selective agonists,
R(−)- or
S(+)-
α-methylhistamine and imetit were not affected by thioperamide (1
μM). Histamine H
2- and H
3-receptor mediated dilator effects were endothelium-independent and were blocked by either excess (80 mM) extracellular K
+, or 1 mM tetrabutylammonium (a non-selective K
+ channel blocker), as well as by 1
μM dequalinium, a non-peptide blocker of the small conductance Ca
2+-activated (SK
Ca) K
+ channels. We conclude that (i) histamine H
1 receptor subtype predominantly mediates endothelium-dependent dilator effect of histamine, and (ii) vascular hyperpolarization through opening of K
+ channels (SK
Ca) mediate the dilator responses to histamine H
2 receptor (amthamine and dimaprit) and the putative histamine H
3 receptor (
R(−)-
α-methylhistamine and imetit) agonists.</description><subject>Animals</subject><subject>Arterioles - drug effects</subject><subject>Arterioles - physiology</subject><subject>Biological and medical sciences</subject><subject>Dose-Response Relationship, Drug</subject><subject>Electrophysiology</subject><subject>Histamine - pharmacology</subject><subject>Histamine Agonists - pharmacology</subject><subject>Histamine and antagonists. Allergy</subject><subject>Histamine Antagonists - pharmacology</subject><subject>Histamine receptor subtype</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Perfused mesenteric bed</subject><subject>Perfusion</subject><subject>Pharmacology. Drug treatments</subject><subject>Potassium - metabolism</subject><subject>Potassium Channel Blockers</subject><subject>Potassium Channels - metabolism</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptors, Histamine - physiology</subject><subject>Splanchnic Circulation - drug effects</subject><subject>Splanchnic Circulation - physiology</subject><subject>Vascular hyperpolarization</subject><subject>Vasodilation - drug effects</subject><subject>Vasodilation - physiology</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1v1DAQhi0EKtvCT6jkA0JUImXsxIl9qlAFtFKlHoCz5ThjapRNgsdBKr8eb3e1155szzyvPx4zdi7gUoBoP30HEE0ljTEfjL4oC2Eq_YJthO5MBZ2QL9nmiLxmp0S_AUAZqU7YiWlVrbXeMLqJlN02TsgTelzynDitfX5ckPgWh-hynH7xh7JOyzy6FP-VyjzxOPH8gDxSKWYcPvIChJVw4MnlkiScMqbo-ZKwcmk338V5j8Mb9iq4kfDtYTxjP79--XF9U93df7u9_nxX-UapXKGXbe2Chs6E1mHbd04oKYzpwUsQwYNSbhCN75rBOICmPFZhLYUPGn3o6jP2fr_vkuY_K1K220gex9FNOK9kO2O01AIKqPagTzNRwmCXFLcuPVoBdifbPsm2O5PWaPsk2-qSOz8csPbF1TF1sFv67w59R96NIbnJRzpisoZGq7ZgV3sMi4y_EZMlH3HyxX75k2yHOT5zkf93C54g</recordid><startdate>19980424</startdate><enddate>19980424</enddate><creator>Adeagbo, Ayotunde S.O</creator><creator>Oriowo, Mabayoje A</creator><general>Elsevier B.V</general><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>19980424</creationdate><title>Histamine receptor subtypes mediating hyperpolarization in the isolated, perfused rat mesenteric pre-arteriolar bed</title><author>Adeagbo, Ayotunde S.O ; Oriowo, Mabayoje A</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c455t-ec263af8079f6ae6b7a152199b0c201fc055ad14c74d9a0040145e321cf8ecf73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Animals</topic><topic>Arterioles - drug effects</topic><topic>Arterioles - physiology</topic><topic>Biological and medical sciences</topic><topic>Dose-Response Relationship, Drug</topic><topic>Electrophysiology</topic><topic>Histamine - pharmacology</topic><topic>Histamine Agonists - pharmacology</topic><topic>Histamine and antagonists. Allergy</topic><topic>Histamine Antagonists - pharmacology</topic><topic>Histamine receptor subtype</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Perfused mesenteric bed</topic><topic>Perfusion</topic><topic>Pharmacology. Drug treatments</topic><topic>Potassium - metabolism</topic><topic>Potassium Channel Blockers</topic><topic>Potassium Channels - metabolism</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptors, Histamine - physiology</topic><topic>Splanchnic Circulation - drug effects</topic><topic>Splanchnic Circulation - physiology</topic><topic>Vascular hyperpolarization</topic><topic>Vasodilation - drug effects</topic><topic>Vasodilation - physiology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Adeagbo, Ayotunde S.O</creatorcontrib><creatorcontrib>Oriowo, Mabayoje A</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>Adeagbo, Ayotunde S.O</au><au>Oriowo, Mabayoje A</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Histamine receptor subtypes mediating hyperpolarization in the isolated, perfused rat mesenteric pre-arteriolar bed</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1998-04-24</date><risdate>1998</risdate><volume>347</volume><issue>2</issue><spage>237</spage><epage>244</epage><pages>237-244</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Histamine is a general dilator of rat blood vessels. We investigated the relative contribution of receptor subtypes to the rat mesenteric dilator responses initiated by histamine and related agonists. Histamine initiated dose, and endothelium-dependent, dilation of constricted mesenteric beds with an ED
50 of 0.4±0.1 nmol. The ED
50 was increased 10-fold by 0.1
μM chlorpheniramine (a histamine H
1-receptor selective antagonist). Histamine H
2 receptor blockade with tiotidine (0.1
μM) slightly decreased, while thioperamide (1
μM), a selective histamine H
3 receptor antagonist, did not block histamine-induced dilation. Mesenteric bed dilation initiated by histamine H
2 receptor selective agonists, amthamine and dimaprit, were antagonized markedly by tiotidine. However, the dilation initiated by the putative histamine H
3 receptor selective agonists,
R(−)- or
S(+)-
α-methylhistamine and imetit were not affected by thioperamide (1
μM). Histamine H
2- and H
3-receptor mediated dilator effects were endothelium-independent and were blocked by either excess (80 mM) extracellular K
+, or 1 mM tetrabutylammonium (a non-selective K
+ channel blocker), as well as by 1
μM dequalinium, a non-peptide blocker of the small conductance Ca
2+-activated (SK
Ca) K
+ channels. We conclude that (i) histamine H
1 receptor subtype predominantly mediates endothelium-dependent dilator effect of histamine, and (ii) vascular hyperpolarization through opening of K
+ channels (SK
Ca) mediate the dilator responses to histamine H
2 receptor (amthamine and dimaprit) and the putative histamine H
3 receptor (
R(−)-
α-methylhistamine and imetit) agonists.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>9653888</pmid><doi>10.1016/S0014-2999(98)00119-8</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0014-2999 |
| ispartof | European journal of pharmacology, 1998-04, Vol.347 (2), p.237-244 |
| issn | 0014-2999 1879-0712 |
| language | eng |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Animals Arterioles - drug effects Arterioles - physiology Biological and medical sciences Dose-Response Relationship, Drug Electrophysiology Histamine - pharmacology Histamine Agonists - pharmacology Histamine and antagonists. Allergy Histamine Antagonists - pharmacology Histamine receptor subtype Male Medical sciences Perfused mesenteric bed Perfusion Pharmacology. Drug treatments Potassium - metabolism Potassium Channel Blockers Potassium Channels - metabolism Rats Rats, Sprague-Dawley Receptors, Histamine - physiology Splanchnic Circulation - drug effects Splanchnic Circulation - physiology Vascular hyperpolarization Vasodilation - drug effects Vasodilation - physiology |
| title | Histamine receptor subtypes mediating hyperpolarization in the isolated, perfused rat mesenteric pre-arteriolar bed |
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