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Volumn 165, Issue 8, 2012, Pages 2672-2683

Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β 2-adrenoceptor agonists

Author keywords

Adrenoceptor; Agonist; Association rate (k on); Competition binding; Dissociation rate (k off); Equilibrium; Intrinsic activity; Kinetics

Indexed keywords

ADRENALIN; BETA 2 ADRENERGIC RECEPTOR; BETA 2 ADRENERGIC RECEPTOR STIMULATING AGENT; CARMOTEROL; FORMOTEROL; INDACATEROL; ISOPRENALINE; LONG ACTING DRUG; SALBUTAMOL; SALMETEROL;

EID: 84859059730     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2011.01639.x     Document Type: Article
Times cited : (71)

References (48)
  • 2
    • 0028300203 scopus 로고
    • Why are long-acting beta-adrenoceptor agonists long-acting?
    • Anderson GP, Linden A, Rabe KF (1994). Why are long-acting beta-adrenoceptor agonists long-acting? Eur Respir J 7: 569-578. (Pubitemid 24099018)
    • (1994) European Respiratory Journal , vol.7 , Issue.3 , pp. 569-578
    • Anderson, G.P.1    Linden, A.2    Rabe, K.F.3
  • 3
    • 33645882522 scopus 로고    scopus 로고
    • In vitro and in vivo pharmacological characterization of 5-[(R)2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2- one (Indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action
    • Battram C, Charlton SJ, Cuenoud B, Dowling MR, Fairhurst RA, Farr D et al. (2006). In vitro and in vivo pharmacological characterization of 5-[(R)2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2- one (Indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action. J Pharmacol Exp Ther 317: 762-770.
    • (2006) J Pharmacol Exp Ther , vol.317 , pp. 762-770
    • Battram, C.1    Charlton, S.J.2    Cuenoud, B.3    Dowling, M.R.4    Fairhurst, R.A.5    Farr, D.6
  • 4
    • 77955656197 scopus 로고    scopus 로고
    • A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators
    • Beattie D, Bradley M, Brearley A, Charlton SJ, Cuenoud BM, Fairhurst RA et al. (2010). A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators. Bioorg Med Chem Lett 20: 5302-5307.
    • (2010) Bioorg Med Chem Lett , vol.20 , pp. 5302-5307
    • Beattie, D.1    Bradley, M.2    Brearley, A.3    Charlton, S.J.4    Cuenoud, B.M.5    Fairhurst, R.A.6
  • 5
    • 77953028976 scopus 로고    scopus 로고
    • The short, the long and the 'ultra-long': Why duration of bronchodilator action matters in chronic obstructive pulmonary disease
    • Beeh KM, Beier J (2010). The short, the long and the 'ultra-long': why duration of bronchodilator action matters in chronic obstructive pulmonary disease. Adv Ther 27: 150-159.
    • (2010) Adv Ther , vol.27 , pp. 150-159
    • Beeh, K.M.1    Beier, J.2
  • 7
  • 8
    • 0017184389 scopus 로고
    • A rapid and sensitive method for quantitation of microgram quantities of protein utilizing principle of protein-dye binding
    • Bradford MM (1976). A rapid and sensitive method for quantitation of microgram quantities of protein utilizing principle of protein-dye binding. Anal Biochem 72: 248-254.
    • (1976) Anal Biochem , vol.72 , pp. 248-254
    • Bradford, M.M.1
  • 9
    • 37749048011 scopus 로고    scopus 로고
    • Efficacy and safety of single therapeutic and supratherapeutic doses of indacaterol versus salmeterol and salbutamol in patients with asthma
    • Brookman LJ, Knowles LJ, Barbier M, Elharrar B, Fuhr R, Pascoe S (2007). Efficacy and safety of single therapeutic and supratherapeutic doses of indacaterol versus salmeterol and salbutamol in patients with asthma. Curr Med Res Opin 23: 3113-3122.
    • (2007) Curr Med Res Opin , vol.23 , pp. 3113-3122
    • Brookman, L.J.1    Knowles, L.J.2    Barbier, M.3    Elharrar, B.4    Fuhr, R.5    Pascoe, S.6
  • 10
    • 33847659232 scopus 로고    scopus 로고
    • Miniaturized receptor binding assays: Complications arising from ligand depletion
    • DOI 10.1177/1087057106297788
    • Carter CM, Leighton-Davies JR, Charlton SJ (2007). Miniaturized receptor binding assays: complications arising from ligand depletion. J Biomol Screen 12: 255-266. (Pubitemid 46364429)
    • (2007) Journal of Biomolecular Screening , vol.12 , Issue.2 , pp. 255-266
    • Carter, C.M.S.1    Leighton-Davies, J.R.2    Charlton, S.J.3
  • 12
    • 69249213484 scopus 로고    scopus 로고
    • Agonist efficacy and receptor desensitization: From partial truths to a fuller picture
    • Review
    • Charlton SJ (2009). Agonist efficacy and receptor desensitization: from partial truths to a fuller picture. Br J Pharmacol 158: 165-168. Review.
    • (2009) Br J Pharmacol , vol.158 , pp. 165-168
    • Charlton, S.J.1
  • 13
    • 0015861774 scopus 로고
    • Relationship between inhibition constant (K1) and concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic-reaction
    • Cheng Y, Prusoff WH (1973). Relationship between inhibition constant (K1) and concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic-reaction. Biochem Pharmacol 22: 3099-3108.
    • (1973) Biochem Pharmacol , vol.22 , pp. 3099-3108
    • Cheng, Y.1    Prusoff, W.H.2
  • 15
    • 69249219006 scopus 로고    scopus 로고
    • On the mechanism of the persistent action of salmeterol: What is the current position?
    • Coleman RA (2009). On the mechanism of the persistent action of salmeterol: what is the current position? Br J Pharmacol 158: 180-182.
    • (2009) Br J Pharmacol , vol.158 , pp. 180-182
    • Coleman, R.A.1
  • 17
    • 33748325882 scopus 로고    scopus 로고
    • Drug-target residence time and its implications for lead optimization
    • DOI 10.1038/nrd2082, PII NRD2082
    • Copeland RA, Pompliano DL, Meek TD (2006). Drug-target residence time and its implications for lead optimization. Nat Rev Drug Discov 5: 730-739. (Pubitemid 44323700)
    • (2006) Nature Reviews Drug Discovery , vol.5 , Issue.9 , pp. 730-739
    • Copeland, R.A.1    Pompliano, D.L.2    Meek, T.D.3
  • 18
    • 0023753716 scopus 로고
    • Certain beta-blockers can decrease beta-adrenergic receptor number: I. Acute reduction in receptor number by tertatolol and bopindolol
    • De Blasi A, Fratelli M, Marasco O (1988). Certain beta-blockers can decrease beta-adrenergic receptor number: I. Acute reduction in receptor number by tertatolol and bopindolol. Circ Res 63: 273-278.
    • (1988) Circ Res , vol.63 , pp. 273-278
    • De Blasi, A.1    Fratelli, M.2    Marasco, O.3
  • 19
    • 1542743648 scopus 로고    scopus 로고
    • 2-Adrenergic Receptor
    • DOI 10.1021/bi035825a
    • Devanathan S, Yao Z, Salamon Z, Kobilka B, Tollin G (2004). Plasmon-waveguide resonance studies of ligand binding to the human beta 2-adrenergic receptor. Biochemistry 43: 3280-3288. (Pubitemid 38352278)
    • (2004) Biochemistry , vol.43 , Issue.11 , pp. 3280-3288
    • Devanathan, S.1    Yao, Z.2    Salamon, Z.3    Kobilka, B.4    Tollin, G.5
  • 21
    • 0033534194 scopus 로고    scopus 로고
    • Tiotropium (spiriva(TM)): Mechanistical considerations and clinical profile in obstructive lung disease
    • DOI 10.1016/S0024-3205(98)00588-8, PII S0024320598005888
    • Disse B, Speck GA, Rominger KL, Witek TJ Jr, Hammer R (1999). Tiotropium (Spiriva): mechanistical considerations and clinical profile in obstructive lung disease. Life Sci 64: 457-464. (Pubitemid 29066693)
    • (1999) Life Sciences , vol.64 , Issue.6-7 , pp. 457-464
    • Disse, B.1    Speck, G.A.2    Rominger, K.L.3    Witek Jr., T.J.4    Hammer, R.5
  • 22
    • 0025196023 scopus 로고
    • The effects of (+/-)-, (+)- and (-)-celiprolol and bromoacetylalprenololmentane at the beta-adrenoceptors of rat isolated cardiovascular preparations
    • Doggrell SA (1990). The effects of (+/-)-, (+)- and (-)-celiprolol and bromoacetylalprenololmentane at the beta-adrenoceptors of rat isolated cardiovascular preparations. J Pharm Pharmacol 42: 319-324.
    • (1990) J Pharm Pharmacol , vol.42 , pp. 319-324
    • Doggrell, S.A.1
  • 23
    • 33749358578 scopus 로고    scopus 로고
    • 3 receptor
    • DOI 10.1038/sj.bjp.0706819, PII 0706819
    • Dowling MR, Charlton SJ (2006). Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M-3 receptor. Br J Pharmacol 148: 927-937. (Pubitemid 44543610)
    • (2006) British Journal of Pharmacology , vol.148 , Issue.7 , pp. 927-937
    • Dowling, M.R.1    Charlton, S.J.2
  • 24
    • 66149087828 scopus 로고
    • Salmeterol: A novel drug for the treatment of asthma
    • Anderson GP, Morley J (eds). Birkhauser Verlag: Basel
    • Johnson M (1992). Salmeterol: a novel drug for the treatment of asthma. In: Anderson GP, Morley J (eds). New Drugs for Asthma. Birkhauser Verlag: Basel, pp. 79-95.
    • (1992) New Drugs for Asthma , pp. 79-95
    • Johnson, M.1
  • 25
    • 84859075785 scopus 로고    scopus 로고
    • Indacaterol, a novel once-daily beta(2)-agonist, demonstrates 24-hour efficacy and is well tolerated in patients with persistent
    • Kanniess F, Cameron R, Owen R, Higgins M (2006). Indacaterol, a novel once-daily beta(2)-agonist, demonstrates 24-hour efficacy and is well tolerated in patients with persistent. J Allergy Clin Immunol 117: S196-S197.
    • (2006) J Allergy Clin Immunol , vol.117
    • Kanniess, F.1    Cameron, R.2    Owen, R.3    Higgins, M.4
  • 26
    • 0024536402 scopus 로고
    • ICI 147,798: A slowly dissociable beta adrenoceptor antagonist that causes insurmountable beta-1 and surmountable beta-2 adrenoceptor antagonism in isolated tissues
    • Keith RA, Hwang TF, Murthy VS, Kau ST, Salama AI, Giles RE (1989). ICI 147,798: a slowly dissociable beta adrenoceptor antagonist that causes insurmountable beta-1 and surmountable beta-2 adrenoceptor antagonism in isolated tissues. J Pharmacol Exp Ther 248: 240-248. (Pubitemid 19063496)
    • (1989) Journal of Pharmacology and Experimental Therapeutics , vol.248 , Issue.1 , pp. 240-248
    • Keith, R.A.1    Hwang, T.F.2    Murthy, V.S.3    Kau, S.T.4    Salama, A.I.5    Giles, R.E.6
  • 27
    • 0019159625 scopus 로고
    • Tissue levels and displacement of in vivo labelled beta-adrenergic receptors by FM 24, an irreversible or slowly dissociable beta-blocker
    • DOI 10.1016/0014-2999(80)90182-X
    • Le Fur G, Paillard JJ, Rougeot C, Uzan A (1980). Tissue levels and displacement of in vivo labelled beta-adrenergic receptors by FM 24, an irreversible or slowly dissociable beta-blocker. Eur J Pharmacol 67: 413-418. (Pubitemid 11241391)
    • (1980) European Journal of Pharmacology , vol.67 , Issue.4 , pp. 413-418
    • Le, F.G.1    Paillard, J.J.2    Rougeot, C.3    Uzan, A.4
  • 28
    • 0026664509 scopus 로고
    • Beta-adrenoceptor ligands - Characterization and quantification of drug effects
    • Lemoine H (1992). Beta-adrenoceptor ligands - characterization and quantification of drug effects. Quant Struct-Act Rel 11: 211-218.
    • (1992) Quant Struct-Act Rel , vol.11 , pp. 211-218
    • Lemoine, H.1
  • 29
    • 0018744343 scopus 로고
    • In vitro and in vivo kinetic analysis of the interaction of a norbornyl derivative of propranolol with beta-adrenergic receptors of brain and C6 glioma cells; an irreversible or slowly reversible ligand
    • Lucas M, Homburger V, Dolphin A, Bockaert J (1979). In vitro and in vivo kinetic analysis of the interaction of a norbornyl derivative of propranolol with beta-adrenergic receptors of brain and C6 glioma cells; an irreversible or slowly reversible ligand. Mol Pharmacol 15: 588-597. (Pubitemid 9203074)
    • (1979) Molecular Pharmacology , vol.15 , Issue.3 , pp. 588-597
    • Lucas, M.1    Homburger, V.2    Dolphin, A.3    Bockaert, J.4
  • 30
    • 0021336303 scopus 로고
    • The kinetics of competitive radioligand binding predicted by the law of mass action
    • Motulsky HJ, Mahan LC (1984). The kinetics of competitive radioligand binding predicted by the law of mass-action. Mol Pharmacol 25: 1-9. (Pubitemid 14223246)
    • (1984) Molecular Pharmacology , vol.25 , Issue.1 , pp. 1-9
    • Motulsky, H.J.1    Mahan, L.C.2
  • 31
    • 0023728938 scopus 로고
    • The potency and kinetics of the beta-adrenergic receptors on human-neutrophils
    • Mueller H, Motulsky HJ, Sklar LA (1988). The potency and kinetics of the beta-adrenergic receptors on human-neutrophils. Mol Pharmacol 34: 347-353.
    • (1988) Mol Pharmacol , vol.34 , pp. 347-353
    • Mueller, H.1    Motulsky, H.J.2    Sklar, L.A.3
  • 33
    • 0032407926 scopus 로고    scopus 로고
    • A comparison of the onset of action of salbutamol and formoterol in reversing methacholine-induced bronchoconstriction
    • DOI 10.1016/S0954-6111(98)90140-8
    • van Noord JA, Smeets JJ, Maesen FP (1998). A comparison of the onset of action of salbutamol and formoterol in reversing methacholine-induced bronchoconstriction. Respir Med 92: 1346-1351. (Pubitemid 29002772)
    • (1998) Respiratory Medicine , vol.92 , Issue.12 , pp. 1346-1351
    • Van Noord, J.A.1    Smeets, J.J.2    Maesen, F.P.V.3
  • 34
    • 0031471788 scopus 로고    scopus 로고
    • Inhaled dry-powder formoterol and salmeterol in asthmatic patients: Onset of action, duration of effect and potency
    • DOI 10.1183/09031936.97.10112489
    • Palmqvist M, Persson G, Lazer L, Rosenborg J, Larsson P, Lötvall J (1997). Inhaled dry-powder formoterol and salmeterol in asthmatic patients: onset of action, duration of effect and potency. Eur Respir J 10: 2484-2489. (Pubitemid 28048620)
    • (1997) European Respiratory Journal , vol.10 , Issue.11 , pp. 2484-2489
    • Palmqvist, M.1    Persson, G.2    Lazer, L.3    Rosenborg, J.4    Larsson, P.5    Lotvall, J.6
  • 35
    • 0024211087 scopus 로고
    • The receptor binding profile of the new antihypertensive agent nebivolol and its stereoisomers compared with various beta-adrenergic blockers
    • Pauwels PJ, Gommeren W, Van Lommen G, Janssen PA, Leysen JE (1988). The receptor binding profile of the new antihypertensive agent nebivolol and its stereoisomers compared with various beta-adrenergic blockers. Mol Pharmacol 34: 843-851. (Pubitemid 19014407)
    • (1988) Molecular Pharmacology , vol.34 , Issue.6 , pp. 843-851
    • Pauwels, P.J.1    Gommeren, W.2    Van Lommen, G.3    Janssen, P.A.J.4    Leysen, J.E.5
  • 37
    • 77957585604 scopus 로고    scopus 로고
    • Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists
    • Rosethorne EM, Turner RJ, Fairhurst RA, Charlton SJ (2010). Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists. Naunyn Schmiedebergs Arch Pharmacol 382: 255-263.
    • (2010) Naunyn Schmiedebergs Arch Pharmacol , vol.382 , pp. 255-263
    • Rosethorne, E.M.1    Turner, R.J.2    Fairhurst, R.A.3    Charlton, S.J.4
  • 38
    • 0029865450 scopus 로고    scopus 로고
    • Design of drugs involving the concepts and theories of drug metabolism and pharmacokinetics
    • DOI 10.1002/(SICI)1098-1128(199605)16:3<243::AID-MED2>3.0.CO;2-Z
    • Smith DA, Jones BC, Walker DK (1996). Design of drugs involving the concepts and theories of drug metabolism and pharmacokinetics. Med Res Rev 16: 243-266. (Pubitemid 26146807)
    • (1996) Medicinal Research Reviews , vol.16 , Issue.3 , pp. 243-266
    • Smith, D.A.1    Jones, B.C.2    Walker, D.K.3
  • 39
    • 55249126351 scopus 로고    scopus 로고
    • A cell-based assay to assess the persistence of action of agonists acting at recombinant human beta(2) adrenoceptors
    • Summerhill S, Stroud T, Nagendra R, Perros-Huguet C, Trevethick M (2008). A cell-based assay to assess the persistence of action of agonists acting at recombinant human beta(2) adrenoceptors. J Pharmacol Toxicol Methods 58: 189-197.
    • (2008) J Pharmacol Toxicol Methods , vol.58 , pp. 189-197
    • Summerhill, S.1    Stroud, T.2    Nagendra, R.3    Perros-Huguet, C.4    Trevethick, M.5
  • 40
    • 67649380868 scopus 로고    scopus 로고
    • Nebulized formoterol effect on bronchodilation and satisfaction in COPD patients compared to QID ipratropium/albuterol MDI
    • Sutherland ER, Brazinsky S, Feldman G, McGinty J, Tomlinson L, Denis-Mize K (2009). Nebulized formoterol effect on bronchodilation and satisfaction in COPD patients compared to QID ipratropium/albuterol MDI. Curr Med Res Opin 25: 653-661.
    • (2009) Curr Med Res Opin , vol.25 , pp. 653-661
    • Sutherland, E.R.1    Brazinsky, S.2    Feldman, G.3    McGinty, J.4    Tomlinson, L.5    Denis-Mize, K.6
  • 41
    • 69549098265 scopus 로고    scopus 로고
    • Exploring the mechanism of agonist efficacy: A relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor
    • Sykes DA, Dowling MR, Charlton SJ (2009). Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor. Mol Pharmacol 76: 543-551.
    • (2009) Mol Pharmacol , vol.76 , pp. 543-551
    • Sykes, D.A.1    Dowling, M.R.2    Charlton, S.J.3
  • 43
    • 77958533581 scopus 로고    scopus 로고
    • Long-acting beta-agonists in the management of chronic obstructive pulmonary disease: Current and future agents
    • Tashkin DP, Fabbri LM (2010). Long-acting beta-agonists in the management of chronic obstructive pulmonary disease: current and future agents. Respir Res 11: 149.
    • (2010) Respir Res , vol.11 , pp. 149
    • Tashkin, D.P.1    Fabbri, L.M.2
  • 44
    • 0032982607 scopus 로고    scopus 로고
    • 2 sympathomimetics in isolated receptor membranes: Evidence against prolonged effects of salmeterol and formoterol on receptor-coupled adenylyl cyclase
    • Teschemacher A, Lemoine H (1999). Kinetic analysis of drug-receptor interactions of long-acting beta(2), sympathomimetics in isolated receptor membranes: Evidence against prolonged effects of salmeterol and formoterol on receptor-coupled adenylyl cyclase. J Pharmacol Exp Ther 288: 1084-1092. (Pubitemid 29254145)
    • (1999) Journal of Pharmacology and Experimental Therapeutics , vol.288 , Issue.3 , pp. 1084-1092
    • Teschemacher, A.1    Lemoine, H.2
  • 45
    • 77956309074 scopus 로고    scopus 로고
    • Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
    • Vauquelin G, Charlton SJ (2010). Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action. Br J Pharmacol 161: 488-508.
    • (2010) Br J Pharmacol , vol.161 , pp. 488-508
    • Vauquelin, G.1    Charlton, S.J.2
  • 46
    • 0026440948 scopus 로고
    • Atypical molecular pharmacology of a new long-acting beta 2-adrenoceptor agonist, TA 2005
    • Voss HP, Donnell D, Bast A (1992). Atypical molecular pharmacology of a new long-acting beta 2-adrenoceptor agonist, TA 2005. Eur J Pharmacol 227: 403-409.
    • (1992) Eur J Pharmacol , vol.227 , pp. 403-409
    • Voss, H.P.1    Donnell, D.2    Bast, A.3
  • 47
    • 0026782139 scopus 로고
    • Rapid onset of action of inhaled formoterol in asthmatic patients
    • Wegener T, Hedenström H, Melander B (1992). Rapid onset of action of inhaled formoterol in asthmatic patients. Chest 102: 535-538.
    • (1992) Chest , vol.102 , pp. 535-538
    • Wegener, T.1    Hedenström, H.2    Melander, B.3
  • 48
    • 0019823390 scopus 로고
    • Quantitative analysis of drug-receptor interactions: I. Determination of kinetic and equilibrium properties
    • Weiland GA, Molinoff PB (1981). Quantitative analysis of drug-receptor interactions: I. Determination of kinetic and equilibrium properties. Life Sci 27: 313-330. (Pubitemid 12224162)
    • (1981) Life Sciences , vol.29 , Issue.4 , pp. 313-330
    • Weiland, G.A.1    Molinoff, P.B.2


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