메뉴 건너뛰기




Volumn 79, Issue 3, 2011, Pages 389-399

THRX-198321 Is a bifunctional muscarinic receptor antagonist and β2-adrenoceptor agonist (MABA) that binds in a bimodal and multivalent manner

Author keywords

[No Author keywords available]

Indexed keywords

ADRENERGIC RECEPTOR STIMULATING AGENT; ATROPINE; BETA 2 ADRENERGIC RECEPTOR; BIPHENYL 2 YLCARBAMIC ACID 1 [9 [2 HYDROXY 2 (8 HYDROXY 2 OXO 1,2 DIHYDROQUINOLIN 5 YL)ETHYLAMINO]NONYL]PIPERIDIN 4 YL ESTER; BIPHENYL CARBAMIC ACID PIPERIDINYL ESTER; CARBAMIC ACID; ESTER DERIVATIVE; ISOPRENALINE; MUSCARINIC M2 RECEPTOR; MUSCARINIC M3 RECEPTOR; MUSCARINIC RECEPTOR BLOCKING AGENT; OBIDOXIME; OXOTREMORINE; PROPRANOLOL; RADIOLIGAND; THRX 198321; UNCLASSIFIED DRUG;

EID: 79951997039     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.110.069120     Document Type: Article
Times cited : (39)

References (36)
  • 3
    • 0021363316 scopus 로고
    • Atypical beta-adrenoceptor on brown adipocytes as target for anti-obesity drugs
    • Arch JR, Ainsworth AT, Cawthorne MA, Piercy V, Sennitt MV, Thody VE, Wilson C, and Wilson S (1984) Atypical beta-adrenoceptor on brown adipocytes as target for anti-obesity drugs. Nature 309:163-165. (Pubitemid 14142787)
    • (1984) Nature , vol.309 , Issue.5964 , pp. 163-165
    • Arch, J.R.S.1    Ainsworth, A.T.2    Cawthorne, M.A.3
  • 5
    • 68149158110 scopus 로고    scopus 로고
    • Pharmacologic treatments for chronic obstructive pulmonary disease: A mixed-treatment comparison meta-analysis
    • Baker WL, Baker EL, and Coleman CI (2009) Pharmacologic treatments for chronic obstructive pulmonary disease: a mixed-treatment comparison meta-analysis. Pharmacotherapy 29:891-905.
    • (2009) Pharmacotherapy , vol.29 , pp. 891-905
    • Baker, W.L.1    Baker, E.L.2    Coleman, C.I.3
  • 6
    • 16344392540 scopus 로고    scopus 로고
    • Bronchodilator efficacy of combined salmeterol and tiotropium in patients with chronic obstructive pulmonary disease
    • Baloira Villar A and Vilariño Pombo C (2005) [Bronchodilator efficacy of combined salmeterol and tiotropium in patients with chronic obstructive pulmonary disease]. Arch Bronconeumol 41:130-134.
    • (2005) Arch Bronconeumol , vol.41 , pp. 130-134
    • Baloira Villar, A.1    Vilariño Pombo, C.2
  • 7
    • 24144458943 scopus 로고    scopus 로고
    • Reducing the frequency and severity of exacerbations of chronic obstructive pulmonary disease
    • Calverley PM (2004) Reducing the frequency and severity of exacerbations of chronic obstructive pulmonary disease. Proc Am Thorac Soc 1:121-124.
    • (2004) Proc Am Thorac Soc , vol.1 , pp. 121-124
    • Calverley, P.M.1
  • 8
    • 8644251968 scopus 로고    scopus 로고
    • The functional impact of adding salmeterol and tiotropium in patients with stable COPD
    • DOI 10.1016/j.rmed.2004.05.003, PII S0954611104001878
    • Cazzola M, Centanni S, Santus P, Verga M, Mondoni M, di Marco F, and Matera MG (2004) The functional impact of adding salmeterol and tiotropium in patients with stable COPD. Respir Med 98:1214-1221. (Pubitemid 39497224)
    • (2004) Respiratory Medicine , vol.98 , Issue.12 , pp. 1214-1221
    • Cazzola, M.1    Centanni, S.2    Santus, P.3    Verga, M.4    Mondoni, M.5    Di, M.F.6    Matera, M.G.7
  • 9
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
    • Cheng Y and Prusoff WH (1973) relationship between the inhibition constant (K1) and the 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
  • 11
    • 0027054955 scopus 로고
    • Two allosteric modulators interact at a common site on cardiac muscarinic receptors
    • Ellis J and Seidenberg M (1992) Two allosteric modulators interact at a common site on cardiac muscarinic receptors. Mol Pharmacol 42:638-641. (Pubitemid 23027627)
    • (1992) Molecular Pharmacology , vol.42 , Issue.4 , pp. 638-641
    • Ellis, J.1    Seidenberg, M.2
  • 12
    • 0029841642 scopus 로고    scopus 로고
    • Sustained activation of a G protein-coupled receptor via "anchored" agonist binding. Molecular localization of the salmeterol exosite within the 2-adrenergic receptor
    • Green SA, Spasoff AP, Coleman RA, Johnson M, and Liggett SB (1996) Sustained activation of a G protein-coupled receptor via "anchored" agonist binding. Molecular localization of the salmeterol exosite within the 2-adrenergic receptor. J Biol Chem 271:24029-24035.
    • (1996) J Biol Chem , vol.271 , pp. 24029-24035
    • Green, S.A.1    Spasoff, A.P.2    Coleman, R.A.3    Johnson, M.4    Liggett, S.B.5
  • 14
    • 70349781296 scopus 로고    scopus 로고
    • An optical dynamic mass redistribution assay reveals biased signaling of dualsteric GPCR activators
    • Kebig A, Kostenis E, Mohr K, and Mohr-Andrä M (2009) An optical dynamic mass redistribution assay reveals biased signaling of dualsteric GPCR activators. J Recept Signal Transduct Res 29:140-145.
    • (2009) J Recept Signal Transduct Res , vol.29 , pp. 140-145
    • Kebig, A.1    Kostenis, E.2    Mohr, K.3    Mohr-Andrä, M.4
  • 15
    • 0027522536 scopus 로고
    • Further concerns over Cheng-Prusoff analysis
    • Leff P and Dougall IG (1993) Further concerns over Cheng-Prusoff analysis. Trends Pharmacol Sci 14:110-112. (Pubitemid 23113114)
    • (1993) Trends in Pharmacological Sciences , vol.14 , Issue.4 , pp. 110-112
    • Leff, P.1    Dougall, I.G.2
  • 16
    • 0029094516 scopus 로고
    • Analysis of competitive agonist-antagonist interactions by nonlinear regression
    • Lew MJ and Angus JA (1995) Analysis of competitive agonist-antagonist interactions by nonlinear regression. Trends Pharmacol Sci 16:328-337.
    • (1995) Trends Pharmacol Sci , vol.16 , pp. 328-337
    • Lew, M.J.1    Angus, J.A.2
  • 18
    • 0032476812 scopus 로고    scopus 로고
    • Polyvalent interactions in biological systems: Implications for design and use of multivalent ligands and inhibitors
    • Mammen M, Choi SK, and Whitesides GM (1998a) Polyvalent interactions in biological systems: implications for design and use of multivalent ligands and inhibitors. Angew Chem Int Ed 37:2754-2794. (Pubitemid 29008561)
    • (1998) Angewandte Chemie - International Edition , vol.37 , Issue.20 , pp. 2754-2794
    • Mammen, M.1    Choi, S.-K.2    Whitesides, G.M.3
  • 19
    • 0000598486 scopus 로고    scopus 로고
    • Using a Convenient, Quantitative Model for Torsional Entropy to Establish Qualitative Trends for Molecular Processes That Restrict Conformational Freedom
    • Mammen M, Shakhnovich EI, and Whitesides GM (1998b) Using a convenient, quantitative model for torsional entropy to establish qualitative trends for molecular processes that restrict conformational freedom. J Org Chem 63:3168-3175. (Pubitemid 128500459)
    • (1998) Journal of Organic Chemistry , vol.63 , Issue.10 , pp. 3168-3175
    • Mammen, M.1    Shakhnovich, E.I.2    Whitesides, G.M.3
  • 20
    • 33845338724 scopus 로고    scopus 로고
    • Projections of global mortality and burden of disease from 2002 to 2030
    • Mathers CD and Loncar D (2006) Projections of global mortality and burden of disease from 2002 to 2030. PLoS Med 3:e442.
    • (2006) PLoS Med , vol.3
    • Mathers, C.D.1    Loncar, D.2
  • 24
    • 0031722980 scopus 로고    scopus 로고
    • Selective muscarinic antagonists. I. Synthesis and antimuscarinic properties of 4-piperidyl benzhydrylcarbamate derivatives
    • Naito R, Takeuchi M, Morihira K, Hayakawa M, Ikeda K, Shibanuma T, and Isomura Y (1998a) Selective muscarinic antagonists. I. Synthesis and antimuscarinic properties of 4-piperidyl benzhydrylcarbamate derivatives. Chem Pharm Bull (Tokyo) 46:1274-1285. (Pubitemid 28407257)
    • (1998) Chemical and Pharmaceutical Bulletin , vol.46 , Issue.8 , pp. 1274-1285
    • Naito, R.1    Takeuchi, M.2    Morihira, K.3    Hayakawa, M.4    Ikeda, K.5    Shibanuma, T.6    Isomura, Y.7
  • 26
    • 0032938071 scopus 로고    scopus 로고
    • 2-adrenergic receptors
    • DOI 10.1023/A:1007784109255
    • Smith C and Teitler M (1999) Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors. Cardiovasc Drugs Ther 13:123-126. (Pubitemid 29224837)
    • (1999) Cardiovascular Drugs and Therapy , vol.13 , Issue.2 , pp. 123-126
    • Smith, C.1    Teitler, M.2
  • 28
    • 34547208823 scopus 로고    scopus 로고
    • 2 muscarinic receptor
    • DOI 10.1124/mol.106.033746
    • Steinfeld T, Mammen M, Smith JA, Wilson RD, and Jasper JR (2007) A novel multivalent ligand that bridges the allosteric and orthosteric binding sites of the M2 muscarinic receptor. Mol Pharmacol 72:291-302. (Pubitemid 47124109)
    • (2007) Molecular Pharmacology , vol.72 , Issue.2 , pp. 291-302
    • Steinfeld, T.1    Mammen, M.2    Smith, J.A.M.3    Wilson, R.D.4    Jasper, J.R.5
  • 31
    • 40249111478 scopus 로고    scopus 로고
    • Concomitant treatment with nebulized formoterol and tiotropium in subjects with COPD: A placebo-controlled trial
    • Tashkin DP, Littner M, Andrews CP, Tomlinson L, Rinehart M, and Denis-Mize K (2008) Concomitant treatment with nebulized formoterol and tiotropium in subjects with COPD: a placebo-controlled trial. Respir Med 102:479-487.
    • (2008) Respir Med , vol.102 , pp. 479-487
    • Tashkin, D.P.1    Littner, M.2    Andrews, C.P.3    Tomlinson, L.4    Rinehart, M.5    Denis-Mize, K.6
  • 32
    • 0038681406 scopus 로고    scopus 로고
    • 2 receptors
    • Tränkle C and Mohr K (1997) Divergent modes of action among cationic allosteric modulators of muscarinic M2 receptors. Mol Pharmacol 51:674-682. (Pubitemid 27172996)
    • (1997) Molecular Pharmacology , vol.51 , Issue.4 , pp. 674-682
    • Trankle, C.1    Mohr, K.2
  • 33
    • 57649170953 scopus 로고    scopus 로고
    • A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand
    • Valant C, Gregory KJ, Hall NE, Scammells PJ, Lew MJ, Sexton PM, and Christopoulos A (2008) A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. J Biol Chem 283:29312-29321.
    • (2008) J Biol Chem , vol.283 , pp. 29312-29321
    • Valant, C.1    Gregory, K.J.2    Hall, N.E.3    Scammells, P.J.4    Lew, M.J.5    Sexton, P.M.6    Christopoulos, A.7
  • 35
    • 33645116728 scopus 로고    scopus 로고
    • Effects of tiotropium with and without formoterol on airflow obstruction and resting hyperinflation in patients with COPD
    • van Noord JA, Aumann JL, Janssens E, Verhaert J, Smeets JJ, Mueller A, and Cornelissen PJ (2006) Effects of tiotropium with and without formoterol on airflow obstruction and resting hyperinflation in patients with COPD. Chest 129:509-517.
    • (2006) Chest , vol.129 , pp. 509-517
    • Van Noord, J.A.1    Aumann, J.L.2    Janssens, E.3    Verhaert, J.4    Smeets, J.J.5    Mueller, A.6    Cornelissen, P.J.7


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.