Evidence that an atypical β‐adrenoceptor mediates the inhibition of spontaneous rhythmical contractions of rabbit isolated jejunum induced by ritodrine and salbutamol

1 The nature of the adrenoceptors mediating the inhibitory action of noradrenaline, ritodrine and salbutamol on the spontaneous activity of longitudinal muscle of the rabbit jejunum in vitro was investigated by use of a range of adrenoceptor antagonists. 2 The actions of ritodrine and salbutamol wer...

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Veröffentlicht in:British journal of pharmacology 1990-09, Vol.101 (1), p.27-30
Hauptverfasser: Norman, Bernard J., Leathard, Helen L.
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description 1 The nature of the adrenoceptors mediating the inhibitory action of noradrenaline, ritodrine and salbutamol on the spontaneous activity of longitudinal muscle of the rabbit jejunum in vitro was investigated by use of a range of adrenoceptor antagonists. 2 The actions of ritodrine and salbutamol were antagonized competitively by propranolol. The pA2 values of 6.4 and 6.6 respectively were smaller than those found elsewhere for β1‐ and β2‐adrenoceptors. 3 In contrast, the responses to ritodrine and salbutamol were antagonized only by high concentrations (>2.7 μm) of phentolamine and were unaffected by yohimbine (2.6 μm), mepyramine (2.5 μm) or cimetidine (4.0 μm). 4 Ritodrine which is less potent than salbutamol in tissues with typical β2‐adrenoceptors was found to be 8 times more potent than salbutamol in the rabbit jejunum. 5 It is suggested that in the rabbit jejunum ritodrine and salbutamol may act at an atypical β‐adrenoceptor, at which propranolol is a competitive but not very potent antagonist.
doi_str_mv 10.1111/j.1476-5381.1990.tb12083.x
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The pA2 values of 6.4 and 6.6 respectively were smaller than those found elsewhere for β1‐ and β2‐adrenoceptors. 3 In contrast, the responses to ritodrine and salbutamol were antagonized only by high concentrations (&gt;2.7 μm) of phentolamine and were unaffected by yohimbine (2.6 μm), mepyramine (2.5 μm) or cimetidine (4.0 μm). 4 Ritodrine which is less potent than salbutamol in tissues with typical β2‐adrenoceptors was found to be 8 times more potent than salbutamol in the rabbit jejunum. 5 It is suggested that in the rabbit jejunum ritodrine and salbutamol may act at an atypical β‐adrenoceptor, at which propranolol is a competitive but not very potent antagonist.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1990.tb12083.x</identifier><identifier>PMID: 2178019</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Albuterol - pharmacology ; Animals ; Biological and medical sciences ; Cimetidine - pharmacology ; Female ; In Vitro Techniques ; Jejunum - drug effects ; Male ; Medical sciences ; Muscle ; Muscle Contraction - drug effects ; Muscle, Smooth - drug effects ; Muscle, Smooth - physiology ; Norepinephrine - pharmacology ; Pharmacology. 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The pA2 values of 6.4 and 6.6 respectively were smaller than those found elsewhere for β1‐ and β2‐adrenoceptors. 3 In contrast, the responses to ritodrine and salbutamol were antagonized only by high concentrations (&gt;2.7 μm) of phentolamine and were unaffected by yohimbine (2.6 μm), mepyramine (2.5 μm) or cimetidine (4.0 μm). 4 Ritodrine which is less potent than salbutamol in tissues with typical β2‐adrenoceptors was found to be 8 times more potent than salbutamol in the rabbit jejunum. 5 It is suggested that in the rabbit jejunum ritodrine and salbutamol may act at an atypical β‐adrenoceptor, at which propranolol is a competitive but not very potent antagonist.</description><subject>Albuterol - pharmacology</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cimetidine - pharmacology</subject><subject>Female</subject><subject>In Vitro Techniques</subject><subject>Jejunum - drug effects</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Muscle</subject><subject>Muscle Contraction - drug effects</subject><subject>Muscle, Smooth - drug effects</subject><subject>Muscle, Smooth - physiology</subject><subject>Norepinephrine - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyrilamine - pharmacology</subject><subject>Rabbits</subject><subject>Receptors, Adrenergic, beta - drug effects</subject><subject>Receptors, Adrenergic, beta - metabolism</subject><subject>Ritodrine - pharmacology</subject><subject>Yohimbine - pharmacology</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1990</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVUUuO1DAUjBBoaAaOgGQhwS7Bz7E7CQsEjAYGaSRYwNqyHYc4SuzGdobJjiNwDbYchENwEpzpVgNLvLGfq169T2XZI8AFpPN0KIBW25yVNRTQNLiIEgiuy-L6VrY5QrezDca4ygHq-m52L4QB4wRW7CQ7IVDVGJpN9v38yrTaKo1iLyISFom47IwSI_r549fXb6L12jqld9F5NOnWiKhD4mpkbG-kicZZ5DoUds5GYbWbA_L9EvvpRkOlXy_UygorzQuZcpAJbkxCLRr0MNt5SmLtrFIsF-RNdK03VqdmWhTEKOcoJjfez-50Ygz6weE-zT6-Pv9wdpFfvnvz9uzlZa5YWkEOHZOYtV1LpCy3RDasBKIpSCrpljFaEdJJwkilGNS0krqRQFtZNYwyDKUqT7Pne93dLNPASq8TjHznzST8wp0w_F_Emp5_clccGqi2QJPAk4OAd59nHSKfTFB6HPfr4TUmtKbAEvHZnqi8C8Hr7lgEMF-N5gNf3eSrm3w1mh-M5tcp-eHfbR5TD84m_PEBFyE50XlhlQl_KjSkKuuaJN6LPe-LGfXyHx3wV-8vbp7lb0mhzUs</recordid><startdate>199009</startdate><enddate>199009</enddate><creator>Norman, Bernard J.</creator><creator>Leathard, Helen L.</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>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>199009</creationdate><title>Evidence that an atypical β‐adrenoceptor mediates the inhibition of spontaneous rhythmical contractions of rabbit isolated jejunum induced by ritodrine and salbutamol</title><author>Norman, Bernard J. ; Leathard, Helen L.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5083-1f5b05dfd2bb362b95312e41b4b46554722fb2527c51847be9b14db79545013c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1990</creationdate><topic>Albuterol - pharmacology</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cimetidine - pharmacology</topic><topic>Female</topic><topic>In Vitro Techniques</topic><topic>Jejunum - drug effects</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Muscle</topic><topic>Muscle Contraction - drug effects</topic><topic>Muscle, Smooth - drug effects</topic><topic>Muscle, Smooth - physiology</topic><topic>Norepinephrine - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Pyrilamine - pharmacology</topic><topic>Rabbits</topic><topic>Receptors, Adrenergic, beta - drug effects</topic><topic>Receptors, Adrenergic, beta - metabolism</topic><topic>Ritodrine - pharmacology</topic><topic>Yohimbine - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Norman, Bernard J.</creatorcontrib><creatorcontrib>Leathard, Helen L.</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><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>Norman, Bernard J.</au><au>Leathard, Helen L.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evidence that an atypical β‐adrenoceptor mediates the inhibition of spontaneous rhythmical contractions of rabbit isolated jejunum induced by ritodrine and salbutamol</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1990-09</date><risdate>1990</risdate><volume>101</volume><issue>1</issue><spage>27</spage><epage>30</epage><pages>27-30</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>1 The nature of the adrenoceptors mediating the inhibitory action of noradrenaline, ritodrine and salbutamol on the spontaneous activity of longitudinal muscle of the rabbit jejunum in vitro was investigated by use of a range of adrenoceptor antagonists. 2 The actions of ritodrine and salbutamol were antagonized competitively by propranolol. The pA2 values of 6.4 and 6.6 respectively were smaller than those found elsewhere for β1‐ and β2‐adrenoceptors. 3 In contrast, the responses to ritodrine and salbutamol were antagonized only by high concentrations (&gt;2.7 μm) of phentolamine and were unaffected by yohimbine (2.6 μm), mepyramine (2.5 μm) or cimetidine (4.0 μm). 4 Ritodrine which is less potent than salbutamol in tissues with typical β2‐adrenoceptors was found to be 8 times more potent than salbutamol in the rabbit jejunum. 5 It is suggested that in the rabbit jejunum ritodrine and salbutamol may act at an atypical β‐adrenoceptor, at which propranolol is a competitive but not very potent antagonist.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>2178019</pmid><doi>10.1111/j.1476-5381.1990.tb12083.x</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record>
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subjects Albuterol - pharmacology
Animals
Biological and medical sciences
Cimetidine - pharmacology
Female
In Vitro Techniques
Jejunum - drug effects
Male
Medical sciences
Muscle
Muscle Contraction - drug effects
Muscle, Smooth - drug effects
Muscle, Smooth - physiology
Norepinephrine - pharmacology
Pharmacology. Drug treatments
Pyrilamine - pharmacology
Rabbits
Receptors, Adrenergic, beta - drug effects
Receptors, Adrenergic, beta - metabolism
Ritodrine - pharmacology
Yohimbine - pharmacology
title Evidence that an atypical β‐adrenoceptor mediates the inhibition of spontaneous rhythmical contractions of rabbit isolated jejunum induced by ritodrine and salbutamol
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