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Volumn 308, Issue 3, 2004, Pages 1062-1072

Application of a Kinetic Model to the Apparently Complex Behavior of Negative and Positive Allosteric Modulators of Muscarinic Acetylcholine Receptors

Author keywords

[No Author keywords available]

Indexed keywords

ALCURONIUM; BROMINE DERIVATIVE; G PROTEIN COUPLED RECEPTOR; GALLAMINE; HEPTANE 1,7 BIS(DIMETHYL 3 PHTHALIMIDOPROPYL)AMMONIUM BROMIDE; METHYLSCOPOLAMINE; MUSCARINIC M2 RECEPTOR; N METHYLSCOPOLAMINE H 3; RADIOLIGAND; UNCLASSIFIED DRUG;

EID: 1342323325     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.103.059840     Document Type: Article
Times cited : (50)

References (38)
  • 1
    • 0030445626 scopus 로고    scopus 로고
    • Allosteric regulation of muscarinic receptors
    • Birdsall NJ, Lazareno S, and Matsui H (1996) Allosteric regulation of muscarinic receptors. Prog Brain Res 109:147-151.
    • (1996) Prog Brain Res , vol.109 , pp. 147-151
    • Birdsall, N.J.1    Lazareno, S.2    Matsui, H.3
  • 2
    • 0017184389 scopus 로고
    • A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
    • Bradford MM (1976) A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254.
    • (1976) Anal Biochem , vol.72 , pp. 248-254
    • Bradford, M.M.1
  • 3
    • 0025603686 scopus 로고
    • 1 receptor binding and function by 2-amino-3-benzoylthiophenes
    • 1 receptor binding and function by 2-amino-3-benzoylthiophenes. Mol Pharmacol 38:939-949.
    • (1990) Mol Pharmacol , vol.38 , pp. 939-949
    • Bruns, R.F.1    Fergus, J.H.2
  • 4
    • 0036143908 scopus 로고    scopus 로고
    • Allosteric site on muscarinic acetylcholine receptors: A single amino acid in transmembrane region 7 is critical to the subtype selectivities of caracurine V derivatives and alkane-bisammonium ligands
    • Buller S, Zlotos DP, Mohr K, and Ellis J (2002) Allosteric site on muscarinic acetylcholine receptors: a single amino acid in transmembrane region 7 is critical to the subtype selectivities of caracurine V derivatives and alkane-bisammonium ligands. Mol Pharmacol 61:160-168.
    • (2002) Mol Pharmacol , vol.61 , pp. 160-168
    • Buller, S.1    Zlotos, D.P.2    Mohr, K.3    Ellis, J.4
  • 6
    • 0032436491 scopus 로고    scopus 로고
    • Assessing the distribution of parameters in models of ligand-receptor interaction: To log or not to log
    • Christopoulos A (1998) Assessing the distribution of parameters in models of ligand-receptor interaction: to log or not to log. Trends Pharmacol Sci 19:351-357.
    • (1998) Trends Pharmacol Sci , vol.19 , pp. 351-357
    • Christopoulos, A.1
  • 7
    • 0009196548 scopus 로고    scopus 로고
    • Quantification of allosteric interactions at G protein-coupled receptors using radioligand binding assays
    • (Enna SJ ed). Wiley & Sons, New York
    • Christopoulos A (2000) Quantification of allosteric interactions at G protein-coupled receptors using radioligand binding assays, in Current Protocols in Pharmacology (Enna SJ ed), pp 1.22.21-1.22.40. Wiley & Sons, New York.
    • (2000) Current Protocols in Pharmacology , pp. 12221-12240
    • Christopoulos, A.1
  • 8
    • 0036490942 scopus 로고    scopus 로고
    • Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery
    • Christopoulos A (2002) Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nat Rev Drug Discov 1:198-210.
    • (2002) Nat Rev Drug Discov , vol.1 , pp. 198-210
    • Christopoulos, A.1
  • 9
    • 0032777107 scopus 로고    scopus 로고
    • Qualitative and quantitative assessment of relative agonist efficacy
    • Christopoulos A and El-Fakahany EE (1999) Qualitative and quantitative assessment of relative agonist efficacy. Biochem Pharmacol 58:735-748.
    • (1999) Biochem Pharmacol , vol.58 , pp. 735-748
    • Christopoulos, A.1    El-Fakahany, E.E.2
  • 10
    • 0036258990 scopus 로고    scopus 로고
    • G protein-coupled receptor allosterism and complexing
    • Christopoulos A and Kenakin T (2002) G protein-coupled receptor allosterism and complexing. Pharmacol Rev 54:323-374.
    • (2002) Pharmacol Rev , vol.54 , pp. 323-374
    • Christopoulos, A.1    Kenakin, T.2
  • 13
    • 0019137579 scopus 로고
    • A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor
    • De Lean A, Stadel JM, and Lefkowitz RJ (1980) A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor. J Biol Chem 255:7108-7117.
    • (1980) J Biol Chem , vol.255 , pp. 7108-7117
    • De Lean, A.1    Stadel, J.M.2    Lefkowitz, R.J.3
  • 14
    • 0034677966 scopus 로고    scopus 로고
    • Drug discovery: A historical perspective
    • Drews J (2000) Drug discovery: a historical perspective. Science (Wash DC) 287:1960-1964.
    • (2000) Science (Wash DC) , vol.287 , pp. 1960-1964
    • Drews, J.1
  • 15
    • 0022408262 scopus 로고
    • The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium
    • Ehlert FJ (1985) The relationship between muscarinic receptor occupancy and adenylate cyclase inhibition in the rabbit myocardium. Mol Pharmacol 28:410-421.
    • (1985) Mol Pharmacol , vol.28 , pp. 410-421
    • Ehlert, F.J.1
  • 16
    • 0023958554 scopus 로고
    • Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods
    • Ehlert FJ (1988) Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods. Mol Pharmacol 33:187-194.
    • (1988) Mol Pharmacol , vol.33 , pp. 187-194
    • Ehlert, F.J.1
  • 17
    • 0031009786 scopus 로고    scopus 로고
    • Allosteric binding sites on muscarinic receptors
    • Ellis J (1997) Allosteric binding sites on muscarinic receptors. Drug Dev Res 40:193-204.
    • (1997) Drug Dev Res , vol.40 , pp. 193-204
    • Ellis, J.1
  • 18
    • 0034676312 scopus 로고    scopus 로고
    • Therapeutic opportunities for muscarinic receptors in the central nervous system
    • Felder CC, Bymaster FP, Ward J, and DeLapp N (2000) Therapeutic opportunities for muscarinic receptors in the central nervous system. J Med Chem 43:4333-4353.
    • (2000) J Med Chem , vol.43 , pp. 4333-4353
    • Felder, C.C.1    Bymaster, F.P.2    Ward, J.3    DeLapp, N.4
  • 19
    • 0032076016 scopus 로고    scopus 로고
    • Allosteric modulators of ligand binding to muscarinic acetylcholine receptors
    • Holzgrabe U and Mohr K (1998) Allosteric modulators of ligand binding to muscarinic acetylcholine receptors. Drug Disc Today 3:214-222.
    • (1998) Drug Disc Today , vol.3 , pp. 214-222
    • Holzgrabe, U.1    Mohr, K.2
  • 21
    • 0021061677 scopus 로고
    • Time-dependent decreases in binding affinity of agonists for β-adrenergic receptors of intact S49 lymphoma cells
    • Insel PA, Mahan LC, Motulsky HJ, Stoolman LM, and Koachman AM (1983) Time-dependent decreases in binding affinity of agonists for β-adrenergic receptors of intact S49 lymphoma cells. J Biol Chem 258:13597-13605.
    • (1983) J Biol Chem , vol.258 , pp. 13597-13605
    • Insel, P.A.1    Mahan, L.C.2    Motulsky, H.J.3    Stoolman, L.M.4    Koachman, A.M.5
  • 24
    • 0030218059 scopus 로고    scopus 로고
    • Two-point kinetic experiments to quantify allosteric effects on radioligand dissociation
    • Kostenis E and Mohr K (1996) Two-point kinetic experiments to quantify allosteric effects on radioligand dissociation. Trends Pharmacol Sci 17:280-283.
    • (1996) Trends Pharmacol Sci , vol.17 , pp. 280-283
    • Kostenis, E.1    Mohr, K.2
  • 25
    • 0029126526 scopus 로고
    • Detection, quantitation and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors
    • Lazareno S and Birdsall NJM (1995) Detection, quantitation and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors. Mol Pharmacol 48:362-378.
    • (1995) Mol Pharmacol , vol.48 , pp. 362-378
    • Lazareno, S.1    Birdsall, N.J.M.2
  • 26
    • 0036892882 scopus 로고    scopus 로고
    • Analogs of WIN 62, 577 define a second allosteric site on muscarinic receptors
    • Lazareno S, Popham A, and Birdsall NJ (2002) Analogs of WIN 62, 577 define a second allosteric site on muscarinic receptors. Mol Pharmacol 62:1492-1505.
    • (2002) Mol Pharmacol , vol.62 , pp. 1492-1505
    • Lazareno, S.1    Popham, A.2    Birdsall, N.J.3
  • 27
    • 0025875643 scopus 로고
    • Allosteric antagonists of the muscarinic acetylcholine receptor
    • Lee NH and El-Fakahany EE (1991) Allosteric antagonists of the muscarinic acetylcholine receptor. Biochem Pharmacol 42:199-205.
    • (1991) Biochem Pharmacol , vol.42 , pp. 199-205
    • Lee, N.H.1    El-Fakahany, E.E.2
  • 30
    • 0028231689 scopus 로고
    • Mechanisms of steric and cooperative actions of alcuronium on cardiac muscarinic acetylcholine receptors
    • Proska J and Tuček S (1994) Mechanisms of steric and cooperative actions of alcuronium on cardiac muscarinic acetylcholine receptors. Mol Pharmacol 45:709-717.
    • (1994) Mol Pharmacol , vol.45 , pp. 709-717
    • Proska, J.1    Tuček, S.2
  • 31
    • 0020533362 scopus 로고
    • Modification of the binding properties of muscarinic receptors by gallamine
    • Stockton JM, Birdsall NJM, Burgen ASV, and Hulme EC (1983) Modification of the binding properties of muscarinic receptors by gallamine. Mol Pharmacol 23:551-557.
    • (1983) Mol Pharmacol , vol.23 , pp. 551-557
    • Stockton, J.M.1    Birdsall, N.J.M.2    Burgen, A.S.V.3    Hulme, E.C.4
  • 32
    • 0021321393 scopus 로고
    • Agonist-induced changes in β-adrenergic receptors on intact cells
    • Toews ML and Perkins JP (1984) Agonist-induced changes in β-adrenergic receptors on intact cells. J Biol Chem 259:2227-2235.
    • (1984) J Biol Chem , vol.259 , pp. 2227-2235
    • Toews, M.L.1    Perkins, J.P.2
  • 33
    • 0020622203 scopus 로고
    • High-affinity binding of agonists to β-adrenergic receptors on intact cells
    • Toews ML, Kendall Harden T, and Perkins JP (1983) High-affinity binding of agonists to β-adrenergic receptors on intact cells. Proc Natl Acad Sci USA 80:3553-3557.
    • (1983) Proc Natl Acad Sci USA , vol.80 , pp. 3553-3557
    • Toews, M.L.1    Kendall Harden, T.2    Perkins, J.P.3
  • 35
    • 0029055030 scopus 로고
    • Allosteric modulation of muscarinic acetylcholine receptors
    • Tuček S and Proska J (1995) Allosteric modulation of muscarinic acetylcholine receptors. Trends Pharmacol Sci 16:205-212.
    • (1995) Trends Pharmacol Sci , vol.16 , pp. 205-212
    • Tuček, S.1    Proska, J.2
  • 36
    • 0025203309 scopus 로고
    • Positive cooperativity in the binding of alcuronium and N-methylscopolamine to muscarinic acetylcholine receptors
    • Tuček S, Musilkova J, Nedoma J, Proska J, Shelkvnikov S, and Vorlicek J (1990) Positive cooperativity in the binding of alcuronium and N-methylscopolamine to muscarinic acetylcholine receptors. Mol Pharmacol 38:674-680.
    • (1990) Mol Pharmacol , vol.38 , pp. 674-680
    • Tuček, S.1    Musilkova, J.2    Nedoma, J.3    Proska, J.4    Shelkvnikov, S.5    Vorlicek, J.6
  • 37
    • 0028062082 scopus 로고
    • Identification of drugs competing with d-tubocurarine for an allosteric site on cardiac muscarinic receptors
    • Waelbroeck M (1994) Identification of drugs competing with d-tubocurarine for an allosteric site on cardiac muscarinic receptors. Mol Pharmacol 46:685-692.
    • (1994) Mol Pharmacol , vol.46 , pp. 685-692
    • Waelbroeck, M.1
  • 38
    • 0029083945 scopus 로고
    • Cooperativity manifest in the binding properties of purified cardiac muscarinic receptors
    • Wregget KA and Wells JW (1995) Cooperativity manifest in the binding properties of purified cardiac muscarinic receptors. J Biol Chem 270:22488-22499.
    • (1995) J Biol Chem , vol.270 , pp. 22488-22499
    • Wregget, K.A.1    Wells, J.W.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.