메뉴 건너뛰기




Volumn 319, Issue 2, 2006, Pages 710-723

Determining the potency and molecular mechanism of action of insurmountable antagonists

Author keywords

[No Author keywords available]

Indexed keywords

APLAVIROC; DARIFENACIN; FRI 73657; MARAVIROC; N [4 [[[6,7 DIHYDRO 2 (4 METHYLPHENYL) 5H BENZOCYCLOHEPTEN 8 YL]CARBONYL]AMINO]BENZYL] N,N DIMETHYL 2H TETRAHYDROPYRAN 4 AMINIUM CHLORIDE; RECEPTOR BLOCKING AGENT; SR 48 968; UNCLASSIFIED DRUG; VICRIVIROC;

EID: 33751183557     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.106.107375     Document Type: Article
Times cited : (160)

References (32)
  • 2
    • 0009644628 scopus 로고
    • Some quantitative uses of drug antagonists
    • Arunlakshana O and Schild HO (1959) Some quantitative uses of drug antagonists. Br J Pharmacol 14:48-58.
    • (1959) Br J Pharmacol , vol.14 , pp. 48-58
    • Arunlakshana, O.1    Schild, H.O.2
  • 3
    • 0018974870 scopus 로고
    • Antagonists of an indirectly acting agonist: Block by propranolol and sotalol of the action of tyramine on rat heart
    • Black JW, Jenkinson DH, and Kenakin TP (1980) Antagonists of an indirectly acting agonist: block by propranolol and sotalol of the action of tyramine on rat heart. Eur J Pharmacol 65:1-10.
    • (1980) Eur J Pharmacol , vol.65 , pp. 1-10
    • Black, J.W.1    Jenkinson, D.H.2    Kenakin, T.P.3
  • 4
    • 0021058380 scopus 로고
    • Operational models of pharmacological agonist
    • Black JW and Leff P (1983) Operational models of pharmacological agonist. Proc R Soc Lond B Biol Sci 220:141-162.
    • (1983) Proc R Soc Lond B Biol Sci , vol.220 , pp. 141-162
    • Black, J.W.1    Leff, P.2
  • 5
    • 0035123776 scopus 로고    scopus 로고
    • Pharmacological characterization of muscarinic receptors in dog isolated ciliary and urinary bladder smooth muscle
    • Choppin A and Eglen RM (2001) Pharmacological characterization of muscarinic receptors in dog isolated ciliary and urinary bladder smooth muscle. Br J Pharmacol 132:835-842.
    • (2001) Br J Pharmacol , vol.132 , pp. 835-842
    • Choppin, A.1    Eglen, R.M.2
  • 6
    • 0009196548 scopus 로고    scopus 로고
    • Overview of receptor allosterism
    • (Enna SJ, Williams M, Ferkany JW, Porsolt RD, Kenakin TP, and Sullivan JP eds) John Wiley and Sons, Inc., New York
    • Christopoulos A (2000) Overview of receptor allosterism, in Current Protocols in Pharmacology (Enna SJ, Williams M, Ferkany JW, Porsolt RD, Kenakin TP, and Sullivan JP eds) Vol 1, pp 1.21.21-1.21.45, John Wiley and Sons, Inc., New York.
    • (2000) Current Protocols in Pharmacology , vol.1
    • Christopoulos, A.1
  • 7
    • 0036258990 scopus 로고    scopus 로고
    • G-protein coupled receptor allosterism and complexing
    • Christopolous A and Kenakin TP (2002) G-protein coupled receptor allosterism and complexing. Pharmacol Rev 54:323-374.
    • (2002) Pharmacol Rev , vol.54 , pp. 323-374
    • Christopolous, A.1    Kenakin, T.P.2
  • 8
    • 0018910336 scopus 로고
    • Rate of formation and decay of aziridinium ion derived from various 2-haloalkylamines
    • Cook DA, Archibald L, and Kenakin TP (1980) Rate of formation and decay of aziridinium ion derived from various 2-haloalkylamines. Proc West Pharmacol Soc 23:365-368.
    • (1980) Proc West Pharmacol Soc , vol.23 , pp. 365-368
    • Cook, D.A.1    Archibald, L.2    Kenakin, T.P.3
  • 9
    • 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
  • 10
    • 27144491979 scopus 로고    scopus 로고
    • Analysis of allosterism in functional assays
    • Ehlert FJ (2005) Analysis of allosterism in functional assays. J Pharmacol Exp Ther 315:740-754.
    • (2005) J Pharmacol Exp Ther , vol.315 , pp. 740-754
    • Ehlert, F.J.1
  • 11
    • 0030002637 scopus 로고    scopus 로고
    • HIV-1 entry cofactor: Functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor
    • Feng Y, Broder CC, Kennedy PE, and Berger EA (1996) HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor. Science (Wash DC) 272:872-877.
    • (1996) Science (Wash DC) , vol.272 , pp. 872-877
    • Feng, Y.1    Broder, C.C.2    Kennedy, P.E.3    Berger, E.A.4
  • 12
    • 0002177268 scopus 로고
    • The quantitative effects of antagonistic drugs
    • Gaddum JH (1937) The quantitative effects of antagonistic drugs. J Physiol (Lond) 89:7P-9P.
    • (1937) J Physiol (Lond) , vol.89
    • Gaddum, J.H.1
  • 13
    • 70449154105 scopus 로고
    • Theories of drug antagonism
    • Gaddum JH (1957) Theories of drug antagonism. Pharmacol Rev 9:211-218.
    • (1957) Pharmacol Rev , vol.9 , pp. 211-218
    • Gaddum, J.H.1
  • 15
    • 0033669603 scopus 로고    scopus 로고
    • Modeling the functional effects of allosteric modulators at pharmacological receptors: An extension of the two-state model of receptor activation
    • Hall DA (2000) Modeling the functional effects of allosteric modulators at pharmacological receptors: an extension of the two-state model of receptor activation. Mol Pharmacol 58:1412-1423.
    • (2000) Mol Pharmacol , vol.58 , pp. 1412-1423
    • Hall, D.A.1
  • 16
    • 1842333847 scopus 로고    scopus 로고
    • Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors
    • Jakubic J, Bacakova L, Lisa V, El-Fakahany EE, and Tucek S (1997) Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol Pharmacol 52:172-179.
    • (1997) Mol Pharmacol , vol.52 , pp. 172-179
    • Jakubic, J.1    Bacakova, L.2    Lisa, V.3    El-Fakahany, E.E.4    Tucek, S.5
  • 17
    • 4444324531 scopus 로고    scopus 로고
    • Allosteric modulators: The new generation of receptor antagonist
    • Kenakin TP (2004a) Allosteric modulators: the new generation of receptor antagonist. Mol Interv 4:222-229.
    • (2004) Mol Interv , vol.4 , pp. 222-229
    • Kenakin, T.P.1
  • 18
    • 3543061611 scopus 로고    scopus 로고
    • G-protein coupled receptors as allosteric machines
    • Kenakin TP (2004b) G-protein coupled receptors as allosteric machines. Receptors Channels 10:51-60.
    • (2004) Receptors Channels , vol.10 , pp. 51-60
    • Kenakin, T.P.1
  • 19
    • 27844519281 scopus 로고    scopus 로고
    • New concepts in drug discovery: Collateral efficacy and permissive antagonism
    • Kenakin TP (2005) New concepts in drug discovery: collateral efficacy and permissive antagonism. Nat Rev Drug Discov 4:919-927.
    • (2005) Nat Rev Drug Discov , vol.4 , pp. 919-927
    • Kenakin, T.P.1
  • 20
    • 0033637590 scopus 로고    scopus 로고
    • Tachykinin-induced contraction of the guinea-pig isolated oesophageal mucosa is mediated by NK2 receptors
    • Kerr KP, Thai B, and Coupar IM (2000) Tachykinin-induced contraction of the guinea-pig isolated oesophageal mucosa is mediated by NK2 receptors. Br J Pharmacol 131:1461-1467.
    • (2000) Br J Pharmacol , vol.131 , pp. 1461-1467
    • Kerr, K.P.1    Thai, B.2    Coupar, I.M.3
  • 21
    • 0029094516 scopus 로고    scopus 로고
    • Analysis of competitive agonist-antagonist interactions by nonlinear regression
    • Lew MJ and Angus JA (1996) Analysis of competitive agonist-antagonist interactions by nonlinear regression. Trends Pharmacol Sci 16:328-337.
    • (1996) Trends Pharmacol Sci , vol.16 , pp. 328-337
    • Lew, M.J.1    Angus, J.A.2
  • 22
    • 0034306496 scopus 로고    scopus 로고
    • Dynamic mechanisms of non-classical antagonism by competitive AT1 receptor antagonists
    • Lew MJ, Ziogas J, and Christopoulos A (2000) Dynamic mechanisms of non-classical antagonism by competitive AT1 receptor antagonists. Trends Pharmacol Sci 21:376-381.
    • (2000) Trends Pharmacol Sci , vol.21 , pp. 376-381
    • Lew, M.J.1    Ziogas, J.2    Christopoulos, A.3
  • 23
    • 3543144738 scopus 로고    scopus 로고
    • Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro
    • Maeda K, Nakata H, Koh Y, Miyakawa T, Ogata H, Takaoka Y, Sbibayama S, Sagawa K, Fukushima D, Moravek J, et al. (2004) Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro. J Virol 78:8654-8662.
    • (2004) J Virol , vol.78 , pp. 8654-8662
    • Maeda, K.1    Nakata, H.2    Koh, Y.3    Miyakawa, T.4    Ogata, H.5    Takaoka, Y.6    Sbibayama, S.7    Sagawa, K.8    Fukushima, D.9    Moravek, J.10
  • 24
    • 0034624258 scopus 로고    scopus 로고
    • Peptide and non-peptide bradykinin B2 receptor agonists and antagonists: A reappraisal of their pharmacology in guinea pig ileum
    • Meini S, Patacchini R, Lecci A, Quartara L, and Maggi CA (2000) Peptide and non-peptide bradykinin B2 receptor agonists and antagonists: a reappraisal of their pharmacology in guinea pig ileum. Eur J Pharmacol 409:185-194.
    • (2000) Eur J Pharmacol , vol.409 , pp. 185-194
    • Meini, S.1    Patacchini, R.2    Lecci, A.3    Quartara, L.4    Maggi, C.A.5
  • 25
    • 0014448392 scopus 로고
    • The mechanism of action of 2-halogenoethylamines at the adrenergic α-receptor and a further investigation of the "spare receptor" hypothesis
    • Moran JF, Triggle CR, and Triggle DJ (1969) The mechanism of action of 2-halogenoethylamines at the adrenergic α-receptor and a further investigation of the "spare receptor" hypothesis. J Pharm Pharmacol 21:38-47.
    • (1969) J Pharm Pharmacol , vol.21 , pp. 38-47
    • Moran, J.F.1    Triggle, C.R.2    Triggle, D.J.3
  • 27
    • 78651175536 scopus 로고
    • The uptake of atropine and related drugs by intestinal smooth muscle of the guinea pig in relation to acetylcholine receptors
    • Paton WDM and Rang HP (1965) The uptake of atropine and related drugs by intestinal smooth muscle of the guinea pig in relation to acetylcholine receptors. Proc R Soc Lond B Biol Sci 163:1-44.
    • (1965) Proc R Soc Lond B Biol Sci , vol.163 , pp. 1-44
    • Paton, W.D.M.1    Rang, H.P.2
  • 31
    • 15744391870 scopus 로고    scopus 로고
    • The CCR5 receptor-based mechanism of action of 873140, a potent allosteric non-competitive HIV entry-inhibitor
    • Watson C, Jenkinson S, Kazmierski W, and Kenakin TP (2005) The CCR5 receptor-based mechanism of action of 873140, a potent allosteric non-competitive HIV entry-inhibitor. Mol Pharmacol 67:1268-1282.
    • (2005) Mol Pharmacol , vol.67 , pp. 1268-1282
    • Watson, C.1    Jenkinson, S.2    Kazmierski, W.3    Kenakin, T.P.4
  • 32
    • 0032507962 scopus 로고    scopus 로고
    • Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development
    • Zou YR, Kottmann AH, Kuroda M, Taniuchi I, and Littman DR (1998) Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature (Lond) 393:595-599.
    • (1998) Nature (Lond) , vol.393 , pp. 595-599
    • Zou, Y.R.1    Kottmann, A.H.2    Kuroda, M.3    Taniuchi, I.4    Littman, D.R.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.