The pharmacology of a beta 2-selective adrenoceptor antagonist (ICI 118,551)

Journal of Cardiovascular Pharmacology
A J BilskiJ L Wale

Abstract

While specific antagonists of the beta 1-adrenoceptor, such as atenolol and betaxolol, are widely available, a potent specific antagonist selective for the beta 2-adrenoceptor has yet to be described. Previously described beta 2-selective antagonists such as butoxamine, H 35/25, and IPS 339 are lacking in potency, specificity, or appropriate beta 2-selectivity. ICI 118,551 [erythro-dl-1-(7-methylindan-4-yloxy)-3-isopropylaminobutan-2-ol] possesses a high degree of selectivity and specificity for the beta 2-adrenoceptor. The affinity of propranolol and ICI 118,551 for beta-adrenoceptors has been determined by comparing their antagonist potencies, expressed as pA2 values, against the actions of isoproterenol on the guinea pig atrium and uterus. ICI 118,551 had a higher affinity for the uterine beta 2-receptor than did propranolol (pA2 9.26 and 8.64, respectively) but a lower affinity for the atrial beta 1-receptor (pA2 7.17 and 8.30, respectively). Thus, the beta 2/ beta 1-selectivity ratios, in vitro, were 123 for ICI 118,551 and 2.2 for propranolol. The potency and selectivity of ICI 118,551 and atenolol on the chronotropic and vasodilator actions of isoproterenol were compared in anaesthetised dogs. The apparent K' B values at...Continue Reading

Citations

May 1, 1993·Naunyn-Schmiedeberg's Archives of Pharmacology·L HesseH H Wellhöner
Jul 1, 1992·Naunyn-Schmiedeberg's Archives of Pharmacology·S DheinW Klaus
May 1, 1994·Naunyn-Schmiedeberg's Archives of Pharmacology·F D RussellR J Summers
Aug 1, 1993·Pflügers Archiv : European journal of physiology·P MansierB Swynghedauw
Jul 1, 1984·Naunyn-Schmiedeberg's Archives of Pharmacology·R R RuffoloJ S Horng
Oct 1, 1986·Naunyn-Schmiedeberg's Archives of Pharmacology·K SonoM Fujiwara
Jan 1, 1985·Naunyn-Schmiedeberg's Archives of Pharmacology·G EngelB P Richardson
Jan 1, 1987·Graefe's Archive for Clinical and Experimental Ophthalmology = Albrecht Von Graefes Archiv Für Klinische Und Experimentelle Ophthalmologie·P Gautheron, M F Sugrue
Oct 1, 1992·Canadian Journal of Anaesthesia = Journal Canadien D'anesthésie·Y HayashiI Yoshiya
Jun 1, 1991·Cardiovascular Drugs and Therapy·A J Kaumann
Jun 1, 1992·Molecular and Chemical Neuropathology·G R Post, G Dawson
Dec 4, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Anna KlukovitsRóbert Gáspár
Oct 30, 1984·European Journal of Pharmacology·R A LefebvreM G Bogaert
Oct 22, 1985·European Journal of Pharmacology·B CostallC C Tan
Sep 23, 1986·European Journal of Pharmacology·S Hjorth, A Carlsson
Aug 29, 1989·European Journal of Pharmacology·F De PaermentierR W Horton
Feb 13, 1990·European Journal of Pharmacology·T SharpD G Grahame-Smith
Mar 17, 1992·European Journal of Pharmacology·M A MianM J Rand
Sep 1, 1993·European Journal of Obstetrics, Gynecology, and Reproductive Biology·B J JanssenJ F Smits
Mar 1, 1995·Obstetrics and Gynecology·Y R SmithW W Hurd
Jan 1, 1989·Pharmacology, Biochemistry, and Behavior·D C Davies, J M Payne
Aug 1, 1990·Pharmacology, Biochemistry, and Behavior·X M Yang, A J Dunn
Jan 1, 1989·Pharmacology & Therapeutics·M F Sugrue
Jan 1, 1990·Pharmacology & Therapeutics·T H Pringle, J G Riddell
Oct 1, 1988·Journal of the Autonomic Nervous System·Sheila M Gardiner, Terence Bennett
Mar 1, 1989·Journal of the Autonomic Nervous System·C DahlstrandH Ahlman
Jul 1, 1990·Journal of the Autonomic Nervous System·I MasiniA Mugelli
Aug 1, 1995·International Journal of Immunopharmacology·D T Lysle, M E Coussons-Read
Oct 17, 1989·European Journal of Pharmacology·P VanscheeuwijckN Fraeyman
Mar 13, 1990·European Journal of Pharmacology·P VanscheeuwijckN Fraeyman
Jan 1, 1994·Journal of Physiology, Paris·P PierretJ C Orsini
Jan 1, 1993·The Journal of Steroid Biochemistry and Molecular Biology·L EikvarV Hansson
Dec 9, 2003·European Journal of Pharmacology·Mayumi MatsushitaKatsuo Koike
May 7, 2003·Biochemical Pharmacology·Rangaswamy NagmaniDennis R Feller
Dec 25, 2002·European Journal of Pharmacology·Thekla WangemannOtto Erich Brodde
May 7, 1998·European Journal of Pharmacology·Aren van WaardeW Vaalburg
Aug 26, 1998·European Journal of Pharmacology·Y TomiyamaT Kurita
Feb 1, 1997·Physiology & Behavior·Y F DuanN Schneiderman
Aug 28, 1999·Journal of Pharmacological and Toxicological Methods·R CarcanoC Beretta
Oct 1, 2003·Clinical Positron Imaging : Official Journal of the Institute for Clinical P.E.T·Philip H. ElsingaWillem Vaalburg
Mar 21, 1998·British Journal of Pharmacology·D SarseroA J Kaumann
Aug 5, 1999·British Journal of Pharmacology·D R VarmaS Mulay
Jun 24, 2000·British Journal of Pharmacology·Sheila M GardinerTerence Bennett
Apr 18, 2002·British Journal of Pharmacology·Sheila M GardinerTerence Bennett
Nov 1, 1985·Proceedings of the National Academy of Sciences of the United States of America·J B FlexnerD J Brunswick
Apr 27, 2004·Immunopharmacology and Immunotoxicology·Shung-Te KaoJaung-Geng Lin
Apr 10, 2002·Critical Care Medicine·Thomas W L ScheerenArtur Fournell
Dec 24, 2005·Critical Care Medicine·Julien PottecherJacques Duranteau
Jul 13, 2005·Wound Repair and Regeneration : Official Publication of the Wound Healing Society [and] the European Tissue Repair Society·Christine E Pullar, R Rivkah Isseroff
Aug 1, 1994·British Journal of Clinical Pharmacology·N M WheeldonB J Lipworth
Jun 1, 1987·Clinical and Experimental Pharmacology & Physiology·P S MacdonaldG J Dusting
Jul 23, 1998·Clinical and Experimental Pharmacology & Physiology·Y HuangZ Y Chen
Jan 1, 1991·Fundamental & Clinical Pharmacology·K Vidal-Beretervide
Jun 1, 1990·Journal of Autonomic Pharmacology·D W WilliamsR J Summers
Dec 1, 1994·Journal of Autonomic Pharmacology·Sheila A Doggrell, A J Surman
Mar 1, 1992·British Journal of Pharmacology·N J BrownN W Read
Apr 1, 1992·British Journal of Pharmacology·Sheila M GardinerB Hughes
Oct 1, 1992·British Journal of Pharmacology·I P HallK Daykin
Mar 1, 1993·British Journal of Pharmacology·G P LuscombeD J Heal
Aug 1, 1996·British Journal of Pharmacology·A J Kaumann, P Molenaar
Apr 1, 1992·The Journal of Pharmacy and Pharmacology·R A Lefebvre
Feb 27, 2007·Head & Face Medicine·Giorgio IannettiCarlo Cavallotti
Dec 20, 2008·Anesthesia and Analgesia·Ru-Quan HanRona G Giffard
Jul 12, 2005·Journal of Smooth Muscle Research = Nihon Heikatsukin Gakkai Kikanshi·Yoshio TanakaKatsuo Koike
Jun 5, 2012·Biomedical Papers of the Medical Faculty of the University Palacký, Olomouc, Czechoslovakia·Lauro Figueroa-ValverdeMaria Lopez-Ramos
Jun 30, 2005·Reproduction : the Official Journal of the Society for the Study of Fertility·Róbert GáspárGeorge Falkay
May 31, 2014·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·Eric CarbonnelleCatherine Ghezzi
Nov 5, 2014·Proceedings of the National Academy of Sciences of the United States of America·Ivana Y KuoBarbara E Ehrlich
Aug 1, 1993·Journal of the Autonomic Nervous System·L Benbachir-LamriniR J Favier
Aug 1, 1986·Naunyn-Schmiedeberg's Archives of Pharmacology·C DahlöfV Nerme
May 6, 2008·European Journal of Pharmacology·Khaled Al ZubairJames R Docherty
Dec 9, 2010·British Journal of Pharmacology·Stephanie L CatusDana S Hutchinson
Apr 25, 1986·The American Journal of Cardiology·M R Bristow, R Ginsburg
May 18, 2004·European Journal of Pharmacology·Katsuo KoikeYoshio Tanaka
Sep 1, 1989·The Journal of Pharmacy and Pharmacology·S KarhuvaaraR Huupponen
Jan 1, 1989·British Journal of Clinical Pharmacology·S E HadfieldH M Snow
Jul 1, 1985·British Journal of Pharmacology·R A BrownG W Smith
Feb 1, 1986·British Journal of Pharmacology·H Hallberg
Apr 1, 1984·Clinical Endocrinology·A D Struthers, J L Reid
Sep 19, 2000·The Journal of Urology·Y C ParkT Kurita
Apr 12, 2015·The Veterinary Journal·Sandra HoffmannGetu Abraham
Nov 18, 2000·Microcirculation : the Official Journal of the Microcirculatory Society, Inc·D L DyessM I Townsley
Oct 25, 2002·The Journal of Pharmacy and Pharmacology·Sheila A Doggrell
Jun 12, 2008·Comparative Biochemistry and Physiology. Toxicology & Pharmacology : CBP·Vito BellantuonoClaudio Lippe
Jul 8, 2000·Circulation Research·L R QueenA Ferro
Aug 1, 1993·Circulation Research·J K Miyashiro, E O Feigl
Dec 18, 2004·American Journal of Physiology. Heart and Circulatory Physiology·Sheila M GardinerTerence Bennett
Jan 1, 1993·Journal of Neurochemistry·R J Summers, L R McMartin
Sep 1, 1988·Journal of Autonomic Pharmacology·K Vidal-Beretervide, L Castañeda
Mar 1, 1987·Journal of Autonomic Pharmacology·M C MichelO E Brodde
Jan 1, 1988·Fundamental & Clinical Pharmacology·K Vidal-BeretervideM Schmidt
Dec 10, 2009·Phytotherapy Research : PTR·Tengfei ZhangXiu-Min Li
Jan 24, 2003·American Journal of Physiology. Cell Physiology·Chih-Ko YehMichael S Katz
Jul 3, 2019·Assay and Drug Development Technologies·Hermann A M Mucke
Oct 22, 2003·The Journal of Pharmacology and Experimental Therapeutics·Gennadi M KravtsovFai Tang
Sep 11, 2014·British Journal of Pharmacology·Mark A BirrellMaria G Belvisi
Feb 7, 2014·Molecular Pharmacology·Karl T Schmidt, David Weinshenker
Feb 12, 2014·The Journal of Pharmacology and Experimental Therapeutics·Stacey L TannheimerMichael Salmon
Feb 28, 2003·The Journal of Pharmacology and Experimental Therapeutics·Sandeep RathiSatish Rattan
May 7, 2002·Canadian Journal of Physiology and Pharmacology·Danica BrousseauLouis Dumont
Feb 27, 2003·The European Journal of Neuroscience·Sachia G KhasarJon D Levine
Nov 1, 1987·British Journal of Clinical Pharmacology·P M McCaffreyR G Shanks
Oct 1, 1987·British Journal of Pharmacology·P D MitchellP A West
Aug 27, 2003·Journal of Pharmacological Sciences·Yoshitaka TomiyamaMasuo Akahane
Feb 18, 2011·British Journal of Pharmacology·J Daniel HothersallJames R Baker
May 1, 1985·Naunyn-Schmiedeberg's Archives of Pharmacology·R R RuffoloJ S Horng
Mar 1, 1987·Acta Physiologica Scandinavica·H Hallberg, O Almgren
Jan 1, 1988·Fundamental & Clinical Pharmacology·K Vidal-Beretervide
Oct 1, 1993·Clinical and Experimental Pharmacology & Physiology·J M Haynes, J N Pennefather
Feb 1, 1985·British Journal of Pharmacology·L C Blaber, A D Fryer
May 1, 1984·Acta Pharmacologica Et Toxicologica·L H JohanssonE Rosengren
Jan 1, 1990·Annals of the New York Academy of Sciences·K R Borkowski
Nov 1, 1993·Medicinal Research Reviews·J R Arch, A J Kaumann
Oct 14, 2005·The Journal of Pharmacology and Experimental Therapeutics·Sheila M GardinerTerence Bennett
May 28, 2017·Scientific Reports·Hiu Yee KwanZhi-Ling Yu
Feb 1, 1987·The Journal of Pharmacy and Pharmacology·F A Moya-Huff, T J Maher
Jul 1, 1986·British Journal of Pharmacology·G A Bentley, J Starr
Nov 5, 2014·Cancer Prevention Research·Andy ChangYing Huang
Feb 1, 1989·The American Journal of Physiology·J M MadisonW E Finkbeiner
Apr 28, 2021·Circulation Research·Filip BerishaViacheslav O Nikolaev
Aug 15, 1998·Biochemical and Biophysical Research Communications·J TamaokiA Nagai
Feb 17, 2000·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·I GrittiG S Roi

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