Nebivolol is devoid of intrinsic sympathomimetic activity
Nebivolol is a chemically novel, potent and selective β 1-adrenoceptor-blocking agent that acutely lowers arterial blood pressure in hypertensive patients and rats without depressing, or even enhancing, left ventricular function. These properties could be compatible with a partial agonistic effect o...
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| Veröffentlicht in: | European journal of pharmacology 1989-01, Vol.159 (1), p.89-95 |
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| container_title | European journal of pharmacology |
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| creator | Janssens, W.J. Van de Water, A. Xhonneux, R. Reneman, R.S. Van Nueten, J.M. Janssen, P.A.J. |
| description | Nebivolol is a chemically novel, potent and selective
β
1-adrenoceptor-blocking agent that acutely lowers arterial blood pressure in hypertensive patients and rats without depressing, or even enhancing, left ventricular function. These properties could be compatible with a partial agonistic effect of β-adrenoceptor-blocking agents. It was the aim of the present study to investigate whether nebivolol has intrinsic sympathomimetic properties. The study was performed on reserpinized dogs and spontaneously hypertensive rats, and on various isolated tissues from various species. Unlike pindolol and practolol, nebivolol did not exert a stimulating effect on the heart rate and left ventricular function in reserpinized animals and/or in isolated atria of reserpinized rats at doses that are clinically active. Nebivolol did not induce relaxation of isolated coronary arteries and saphenous veins at concentrations that block β-adrenoceptors. These findings indicate that nebivolol is devoid of intrinsic sympathomimetic activity at clinically relevant doeses. |
| doi_str_mv | 10.1016/0014-2999(89)90047-2 |
| format | Article |
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β
1-adrenoceptor-blocking agent that acutely lowers arterial blood pressure in hypertensive patients and rats without depressing, or even enhancing, left ventricular function. These properties could be compatible with a partial agonistic effect of β-adrenoceptor-blocking agents. It was the aim of the present study to investigate whether nebivolol has intrinsic sympathomimetic properties. The study was performed on reserpinized dogs and spontaneously hypertensive rats, and on various isolated tissues from various species. Unlike pindolol and practolol, nebivolol did not exert a stimulating effect on the heart rate and left ventricular function in reserpinized animals and/or in isolated atria of reserpinized rats at doses that are clinically active. Nebivolol did not induce relaxation of isolated coronary arteries and saphenous veins at concentrations that block β-adrenoceptors. These findings indicate that nebivolol is devoid of intrinsic sympathomimetic activity at clinically relevant doeses.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(89)90047-2</identifier><identifier>PMID: 2565239</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Adrenergic beta-Antagonists - pharmacology ; Animals ; Antihypertensive agents ; Atria (isolated) ; Benzopyrans - pharmacology ; Biological and medical sciences ; Blood Pressure - drug effects ; Blood vessels (isolated) ; Cardiovascular system ; Dogs ; Electrocardiography ; Ethanolamines - pharmacology ; Female ; gb1-Adrenoceptor blockade ; Guinea Pigs ; Heart Rate - drug effects ; Hemodynamics - drug effects ; In Vitro Techniques ; Intrinsic sympathomimetic activity ; Isometric Contraction - drug effects ; Male ; Medical sciences ; Muscle, Smooth, Vascular - drug effects ; Nebivolol ; Pharmacology. Drug treatments ; Pindolol ; Practolol ; Rats ; Rats, Inbred SHR ; Rats, Inbred Strains ; Reserpine - pharmacology ; Reserpinized animals ; Sympathomimetics</subject><ispartof>European journal of pharmacology, 1989-01, Vol.159 (1), p.89-95</ispartof><rights>1989</rights><rights>1989 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c417t-e5ca239f84b6e4ab5219f90286b6cd0e613483a591a147f2cddbd6c733fb17413</citedby><cites>FETCH-LOGICAL-c417t-e5ca239f84b6e4ab5219f90286b6cd0e613483a591a147f2cddbd6c733fb17413</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/0014299989900472$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65534</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7336915$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2565239$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Janssens, W.J.</creatorcontrib><creatorcontrib>Van de Water, A.</creatorcontrib><creatorcontrib>Xhonneux, R.</creatorcontrib><creatorcontrib>Reneman, R.S.</creatorcontrib><creatorcontrib>Van Nueten, J.M.</creatorcontrib><creatorcontrib>Janssen, P.A.J.</creatorcontrib><title>Nebivolol is devoid of intrinsic sympathomimetic activity</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Nebivolol is a chemically novel, potent and selective
β
1-adrenoceptor-blocking agent that acutely lowers arterial blood pressure in hypertensive patients and rats without depressing, or even enhancing, left ventricular function. These properties could be compatible with a partial agonistic effect of β-adrenoceptor-blocking agents. It was the aim of the present study to investigate whether nebivolol has intrinsic sympathomimetic properties. The study was performed on reserpinized dogs and spontaneously hypertensive rats, and on various isolated tissues from various species. Unlike pindolol and practolol, nebivolol did not exert a stimulating effect on the heart rate and left ventricular function in reserpinized animals and/or in isolated atria of reserpinized rats at doses that are clinically active. Nebivolol did not induce relaxation of isolated coronary arteries and saphenous veins at concentrations that block β-adrenoceptors. These findings indicate that nebivolol is devoid of intrinsic sympathomimetic activity at clinically relevant doeses.</description><subject>Adrenergic beta-Antagonists - pharmacology</subject><subject>Animals</subject><subject>Antihypertensive agents</subject><subject>Atria (isolated)</subject><subject>Benzopyrans - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Blood Pressure - drug effects</subject><subject>Blood vessels (isolated)</subject><subject>Cardiovascular system</subject><subject>Dogs</subject><subject>Electrocardiography</subject><subject>Ethanolamines - pharmacology</subject><subject>Female</subject><subject>gb1-Adrenoceptor blockade</subject><subject>Guinea Pigs</subject><subject>Heart Rate - drug effects</subject><subject>Hemodynamics - drug effects</subject><subject>In Vitro Techniques</subject><subject>Intrinsic sympathomimetic activity</subject><subject>Isometric Contraction - drug effects</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Muscle, Smooth, Vascular - drug effects</subject><subject>Nebivolol</subject><subject>Pharmacology. Drug treatments</subject><subject>Pindolol</subject><subject>Practolol</subject><subject>Rats</subject><subject>Rats, Inbred SHR</subject><subject>Rats, Inbred Strains</subject><subject>Reserpine - pharmacology</subject><subject>Reserpinized animals</subject><subject>Sympathomimetics</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1989</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1LxDAQhoMoun78A4UeRPRQzaRJm1wEWfwC0YueQ5pMMdI2a9Jd2H9v1132qKchzDPvTB5CToFeA4XyhlLgOVNKXUp1pSjlVc52yARkpXJaAdslky1yQA5T-qKUCsXEPtlnohSsUBOiXrH2i9CGNvMpc7gI3mWhyXw_RN8nb7O07GZm-Ayd73AY38YOfuGH5THZa0yb8GRTj8jHw_379Cl_eXt8nt695JZDNeQorBk3NZLXJXJTCwaqUZTJsi6to1hCwWVhhAIDvGqYda52pa2Koqmh4lAckYt17iyG7zmmQXc-WWxb02OYJ11JBZxJ-S8IAgpVwCqRr0EbQ0oRGz2LvjNxqYHqlVq98qZX3rRU-letZuPY2SZ_XnfotkMbl2P_fNM3yZq2iaa3Pm2x8UelAjFit2sMR2kLj1En67G36HxEO2gX_N93_AC9lZQs</recordid><startdate>19890102</startdate><enddate>19890102</enddate><creator>Janssens, W.J.</creator><creator>Van de Water, A.</creator><creator>Xhonneux, R.</creator><creator>Reneman, R.S.</creator><creator>Van Nueten, J.M.</creator><creator>Janssen, P.A.J.</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>7TK</scope><scope>7X8</scope></search><sort><creationdate>19890102</creationdate><title>Nebivolol is devoid of intrinsic sympathomimetic activity</title><author>Janssens, W.J. ; Van de Water, A. ; Xhonneux, R. ; Reneman, R.S. ; Van Nueten, J.M. ; Janssen, P.A.J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c417t-e5ca239f84b6e4ab5219f90286b6cd0e613483a591a147f2cddbd6c733fb17413</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1989</creationdate><topic>Adrenergic beta-Antagonists - pharmacology</topic><topic>Animals</topic><topic>Antihypertensive agents</topic><topic>Atria (isolated)</topic><topic>Benzopyrans - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Blood Pressure - drug effects</topic><topic>Blood vessels (isolated)</topic><topic>Cardiovascular system</topic><topic>Dogs</topic><topic>Electrocardiography</topic><topic>Ethanolamines - pharmacology</topic><topic>Female</topic><topic>gb1-Adrenoceptor blockade</topic><topic>Guinea Pigs</topic><topic>Heart Rate - drug effects</topic><topic>Hemodynamics - drug effects</topic><topic>In Vitro Techniques</topic><topic>Intrinsic sympathomimetic activity</topic><topic>Isometric Contraction - drug effects</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Muscle, Smooth, Vascular - drug effects</topic><topic>Nebivolol</topic><topic>Pharmacology. Drug treatments</topic><topic>Pindolol</topic><topic>Practolol</topic><topic>Rats</topic><topic>Rats, Inbred SHR</topic><topic>Rats, Inbred Strains</topic><topic>Reserpine - pharmacology</topic><topic>Reserpinized animals</topic><topic>Sympathomimetics</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Janssens, W.J.</creatorcontrib><creatorcontrib>Van de Water, A.</creatorcontrib><creatorcontrib>Xhonneux, R.</creatorcontrib><creatorcontrib>Reneman, R.S.</creatorcontrib><creatorcontrib>Van Nueten, J.M.</creatorcontrib><creatorcontrib>Janssen, P.A.J.</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>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Janssens, W.J.</au><au>Van de Water, A.</au><au>Xhonneux, R.</au><au>Reneman, R.S.</au><au>Van Nueten, J.M.</au><au>Janssen, P.A.J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Nebivolol is devoid of intrinsic sympathomimetic activity</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1989-01-02</date><risdate>1989</risdate><volume>159</volume><issue>1</issue><spage>89</spage><epage>95</epage><pages>89-95</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Nebivolol is a chemically novel, potent and selective
β
1-adrenoceptor-blocking agent that acutely lowers arterial blood pressure in hypertensive patients and rats without depressing, or even enhancing, left ventricular function. These properties could be compatible with a partial agonistic effect of β-adrenoceptor-blocking agents. It was the aim of the present study to investigate whether nebivolol has intrinsic sympathomimetic properties. The study was performed on reserpinized dogs and spontaneously hypertensive rats, and on various isolated tissues from various species. Unlike pindolol and practolol, nebivolol did not exert a stimulating effect on the heart rate and left ventricular function in reserpinized animals and/or in isolated atria of reserpinized rats at doses that are clinically active. Nebivolol did not induce relaxation of isolated coronary arteries and saphenous veins at concentrations that block β-adrenoceptors. These findings indicate that nebivolol is devoid of intrinsic sympathomimetic activity at clinically relevant doeses.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>2565239</pmid><doi>10.1016/0014-2999(89)90047-2</doi><tpages>7</tpages></addata></record> |
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| subjects | Adrenergic beta-Antagonists - pharmacology Animals Antihypertensive agents Atria (isolated) Benzopyrans - pharmacology Biological and medical sciences Blood Pressure - drug effects Blood vessels (isolated) Cardiovascular system Dogs Electrocardiography Ethanolamines - pharmacology Female gb1-Adrenoceptor blockade Guinea Pigs Heart Rate - drug effects Hemodynamics - drug effects In Vitro Techniques Intrinsic sympathomimetic activity Isometric Contraction - drug effects Male Medical sciences Muscle, Smooth, Vascular - drug effects Nebivolol Pharmacology. Drug treatments Pindolol Practolol Rats Rats, Inbred SHR Rats, Inbred Strains Reserpine - pharmacology Reserpinized animals Sympathomimetics |
| title | Nebivolol is devoid of intrinsic sympathomimetic activity |
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