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Volumn 17, Issue 30, 2010, Pages 3488-3502

Allosteric enhancers of A1 adenosine receptors: State of the art and new horizons for drug development

Author keywords

A1 adenosine receptor; Allosteric modulators; Enhancer; Neuropatic pain; Neuroprotection

Indexed keywords

2 AMINO 3 (3 CHLOROBENZOYL) 4,5,6,7 TETRAHYDROBENZO[B]THIOPHENE; 2 AMINO 4,5 DIMETHYL 3 (3 TRIFLUOROMETHYLBENZOYL)THIOPHENE; 2 AMINO 6 BENZYL 3 (4 CHLOROBENZOYL) 4,5,6,7 TETRAHYDROTHIENO[2,3 C]PYRIDINE; 4 AMINOBUTYRIC ACID A RECEPTOR; ADENOSINE; ADENOSINE A1 RECEPTOR; ADENOSINE A1 RECEPTOR AGONIST; ADENOSINE A2A RECEPTOR; ADENOSINE A2B RECEPTOR; ADENOSINE A3 RECEPTOR; ADENYLATE CYCLASE; CALCIUM CHANNEL; G PROTEIN COUPLED RECEPTOR; INOSITOL PHOSPHATE; POTASSIUM CHANNEL; UNCLASSIFIED DRUG; 2 AMINOTHIAZOLE; 2-AMINOTHIAZOLE; THIAZOLE DERIVATIVE; THIOPHENE DERIVATIVE;

EID: 77957961698     PISSN: 09298673     EISSN: None     Source Type: Journal    
DOI: 10.2174/092986710792927831     Document Type: Article
Times cited : (39)

References (66)
  • 1
    • 34447632041 scopus 로고    scopus 로고
    • Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology
    • Leach, K.; Sexton, P.M.; Christopoulos, A. Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. Trends Pharmacol. Sci., 2007, 28, 382-389.
    • (2007) Trends Pharmacol. Sci , vol.28 , pp. 382-389
    • Leach, K.1    Sexton, P.M.2    Christopoulos, A.3
  • 2
    • 36448968578 scopus 로고    scopus 로고
    • Allosteric modulation of heterodimeric G protein-coupled receptors
    • Milligan, G.; Smith, N.J. Allosteric modulation of heterodimeric G protein-coupled receptors. Trends Pharmacol. Sci., 2007, 28, 615-620.
    • (2007) Trends Pharmacol. Sci , vol.28 , pp. 615-620
    • Milligan, G.1    Smith, N.J.2
  • 3
    • 34447638166 scopus 로고    scopus 로고
    • Allosteric enhancers, allosteric agonists and ago-allosteric modulators: Where do they bind and how do they act?
    • Schwartz, T.W.; Holst, B. Allosteric enhancers, allosteric agonists and ago-allosteric modulators: where do they bind and how do they act? Trends Pharmacol. Sci., 2007, 28, 366-373.
    • (2007) Trends Pharmacol. Sci , vol.28 , pp. 366-373
    • Schwartz, T.W.1    Holst, B.2
  • 4
    • 0036490942 scopus 로고    scopus 로고
    • Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery
    • Christopoulos, A. Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nat. Rev. Drug Discov., 2002, 1, 198-210.
    • (2002) Nat. Rev. Drug Discov , vol.1 , pp. 198-210
    • Christopoulos, A.1
  • 5
    • 0346996805 scopus 로고    scopus 로고
    • Allosteric enhancers of A1 adenosine receptors increase receptor-G protein coupling and counteract Guanine nucleotide effects on agonist binding
    • Figler, H.; Olsson, R.A.; Linden, J. Allosteric enhancers of A1 adenosine receptors increase receptor-G protein coupling and counteract Guanine nucleotide effects on agonist binding. Mol. Pharmacol., 2003, 64, 1557-1564.
    • (2003) Mol. Pharmacol , vol.64 , pp. 1557-1564
    • Figler, H.1    Olsson, R.A.2    Linden, J.3
  • 6
    • 0019137579 scopus 로고
    • A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled -adrenergic receptor
    • De Lean, A.; Stadel, J.M.; Lefkowitz, R.J. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled -adrenergic receptor. J. Biol. Chem., 1980, 255, 7108-7117
    • (1980) J. Biol. Chem , vol.255 , pp. 7108-7117
    • de Lean, A.1    Stadel, J.M.2    Lefkowitz, R.J.3
  • 7
    • 67650489125 scopus 로고    scopus 로고
    • Orthosteric/allosteric bitopic ligands: Going hybrid at GPCRs
    • Valant, C.; Sexton, P.M.; Christopoulos, A. Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs. Mol. Interv., 2009, 9, 125-135
    • (2009) Mol. Interv , vol.9 , pp. 125-135
    • Valant, C.1    Sexton, P.M.2    Christopoulos, A.3
  • 9
    • 0033766981 scopus 로고    scopus 로고
    • Extracellular metabolism of ATP and other nucleotides
    • Zimmermann, H. Extracellular metabolism of ATP and other nucleotides. Naunyn Schmied. Arch. Pharmacol., 2000, 362, 299-309.
    • (2000) Naunyn Schmied. Arch. Pharmacol , vol.362 , pp. 299-309
    • Zimmermann, H.1
  • 10
    • 0031754497 scopus 로고    scopus 로고
    • Receptors for purines and pyrimidines
    • Ralevic, V.; Burnstock, G. Receptors for purines and pyrimidines. Pharmacol. Rev., 1998, 50, 413-492.
    • (1998) Pharmacol. Rev , vol.50 , pp. 413-492
    • Ralevic, V.1    Burnstock, G.2
  • 11
    • 0018634064 scopus 로고
    • Adenosine regulates via two different types of receptors, the accumulation of cyclic AMP in cultured brain cells
    • van Calker, D.M.; Muller, M.; Hamprecht, B. Adenosine regulates via two different types of receptors, the accumulation of cyclic AMP in cultured brain cells. J. Neurochem., 1979, 33, 999-1005.
    • (1979) J. Neurochem , vol.33 , pp. 999-1005
    • van Calker, D.M.1    Muller, M.2    Hamprecht, B.3
  • 12
    • 16644387822 scopus 로고    scopus 로고
    • Phospholipase C is involved in the adenosine-activated signal transduction pathway conferring protection against iodoacetic acid-induced injury in primary rat neuronal cultures
    • Rogel, A.; Bromberg, Y.; Sperling, O.; Zoref-Shani, E. Phospholipase C is involved in the adenosine-activated signal transduction pathway conferring protection against iodoacetic acid-induced injury in primary rat neuronal cultures. Neurosi. Lett., 2005, 373, 218-221.
    • (2005) Neurosi. Lett , vol.373 , pp. 218-221
    • Rogel, A.1    Bromberg, Y.2    Sperling, O.3    Zoref-Shani, E.4
  • 13
    • 0038771191 scopus 로고    scopus 로고
    • Signalling from adenosine receptors to mitogen-activated protein kinases
    • Schulte, G.; Fredholm, B.B. Signalling from adenosine receptors to mitogen-activated protein kinases. Cell Signal., 2003, 15, 813-827.
    • (2003) Cell Signal , vol.15 , pp. 813-827
    • Schulte, G.1    Fredholm, B.B.2
  • 14
    • 0036139634 scopus 로고    scopus 로고
    • Preliminary efficacy assessment of intrathecal injection of an American formulation of adenosine in humans
    • Eisenach, J.C.; Hood D.D.; Curry, R. Preliminary efficacy assessment of intrathecal injection of an American formulation of adenosine in humans. Anesthesiology, 2002, 96, 29-34
    • (2002) Anesthesiology , vol.96 , pp. 29-34
    • Eisenach, J.C.1    Hood, D.D.2    Curry, R.3
  • 15
    • 0345561561 scopus 로고    scopus 로고
    • Actions of caffeine in the brain with special reference to factors that contribute to its widespread use
    • Fredholm, B.B.; Bättig, K.; Holmen, J.; Nehlig, A.; Zvartau, E. Actions of caffeine in the brain with special reference to factors that contribute to its widespread use. Pharmacol. Rev., 1999, 51, 83-133.
    • (1999) Pharmacol. Rev , vol.51 , pp. 83-133
    • Fredholm, B.B.1    Bättig, K.2    Holmen, J.3    Nehlig, A.4    Zvartau, E.5
  • 16
    • 0034846624 scopus 로고    scopus 로고
    • Adenosine, adenosine receptors and myocardial protection: An updated overview
    • Mubagwa, K.; Flameng, W. Adenosine, adenosine receptors and myocardial protection: an updated overview. Cardiovasc. Res., 2001, 52, 25-39.
    • (2001) Cardiovasc. Res , vol.52 , pp. 25-39
    • Mubagwa, K.1    Flameng, W.2
  • 17
    • 33645034489 scopus 로고    scopus 로고
    • Adenosine receptors: Promising targets for the development of novel therapeutics and diagnostics for asthma
    • Russo, C.; Arcidiacono, G.; Polosa R. Adenosine receptors: promising targets for the development of novel therapeutics and diagnostics for asthma. Fundam. Clin. Pharmacol., 2006, 20, 9-19.
    • (2006) Fundam. Clin. Pharmacol , vol.20 , pp. 9-19
    • Russo, C.1    Arcidiacono, G.2    Polosa, R.3
  • 19
    • 0036374565 scopus 로고    scopus 로고
    • Lipopolysaccharide binds to and activates A(1) adenosine receptors on human pulmonary artery endothelial cells
    • Wilson, C.N.; Batra, V.K. Lipopolysaccharide binds to and activates A(1) adenosine receptors on human pulmonary artery endothelial cells. J. Endotoxin. Res., 2002, 8, 263-271.
    • (2002) J. Endotoxin. Res , vol.8 , pp. 263-271
    • Wilson, C.N.1    Batra, V.K.2
  • 20
    • 33748461247 scopus 로고    scopus 로고
    • Adenosine A1 receptor-mediated inhibition of myocardial norepinephrine release involves neither phospholipase C nor protein kinase C but does involve adenylyl cyclase
    • Schutte, F.; Burgdorf, C.; Richardt, G.; Kurz, T. Adenosine A1 receptor-mediated inhibition of myocardial norepinephrine release involves neither phospholipase C nor protein kinase C but does involve adenylyl cyclase. Can. J. Physiol. Pharmacol., 2006, 84, 573-577.
    • (2006) Can. J. Physiol. Pharmacol , vol.84 , pp. 573-577
    • Schutte, F.1    Burgdorf, C.2    Richardt, G.3    Kurz, T.4
  • 21
    • 33751288406 scopus 로고    scopus 로고
    • Protein kinase C-mediated preconditioning of cardiac myocytes: Role of adenosine receptor and KATP channel
    • Liang B.T. Protein kinase C-mediated preconditioning of cardiac myocytes: role of adenosine receptor and KATP channel. Am. J. Physiol. Heart Circ. Physiol., 1997, 273, H847-853.
    • (1997) Am. J. Physiol. Heart Circ. Physiol , vol.273
    • Liang, B.T.1
  • 22
  • 23
    • 33644798286 scopus 로고    scopus 로고
    • Endogenous adenosine protects preconditioned heart during early minutes of reperfusion by activating Akt
    • Solenkova, N.V.; Solodushko, V.; Cohen, M.V.; Downey, J.M. Endogenous adenosine protects preconditioned heart during early minutes of reperfusion by activating Akt. Am. J. Physiol. Heart Circ. Physiol., 2006, 290, H441-449.
    • (2006) Am. J. Physiol. Heart Circ. Physiol , vol.290
    • Solenkova, N.V.1    Solodushko, V.2    Cohen, M.V.3    Downey, J.M.4
  • 24
    • 33846068738 scopus 로고    scopus 로고
    • Ischemic preconditioning modulates ischemia-reperfusion injury in the rat lung: Role of adenosine receptors
    • Yldiz, G.; Demiryurek, A.T.; Gumusel, B.; Lippton, H. Ischemic preconditioning modulates ischemia-reperfusion injury in the rat lung: role of adenosine receptors. Eur. J. Pharmacol., 2007, 556, 144-150.
    • (2007) Eur. J. Pharmacol , vol.556 , pp. 144-150
    • Yldiz, G.1    Demiryurek, A.T.2    Gumusel, B.3    Lippton, H.4
  • 26
    • 0036525756 scopus 로고    scopus 로고
    • Adenosine A1 receptor antagonists in the kidney: Effects in fluid-retaining disorders
    • Welch, W.J. Adenosine A1 receptor antagonists in the kidney: effects in fluid-retaining disorders. Curr. Opin. Pharmacol., 2002, 2,165-170.
    • (2002) Curr. Opin. Pharmacol , vol.2 , pp. 165-170
    • Welch, W.J.1
  • 27
    • 38749132550 scopus 로고    scopus 로고
    • Adenosine receptor antagonists: Translating medicinal chemistry and pharmacology into clinical utility
    • Baraldi, P.G.; Tabrizi, M.A.; Gessi, S.; Borea, P.A. Adenosine receptor antagonists: translating medicinal chemistry and pharmacology into clinical utility. Chem. Rev., 2008, 108, 238-263.
    • (2008) Chem. Rev , vol.108 , pp. 238-263
    • Baraldi, P.G.1    Tabrizi, M.A.2    Gessi, S.3    Borea, P.A.4
  • 28
    • 60449099749 scopus 로고    scopus 로고
    • Allosteric modulation of adenosine receptors
    • a) Göblyös, A.; IJzerman, A.P
    • a) Göblyös, A.; IJzerman, A.P. Allosteric modulation of adenosine receptors. Purinergic Signal., 2009, 5, 51-61
    • (2009) Purinergic Signal , vol.5 , pp. 51-61
  • 32
    • 0035271616 scopus 로고    scopus 로고
    • Allosteric modulators of G protein-coupled receptors
    • IJzerman, A.P.; Kouronakis, A.; van der Klein, P. Allosteric modulators of G protein-coupled receptors. Il Farmaco, 2001, 56, 67-71.
    • (2001) Il Farmaco , vol.56 , pp. 67-71
    • Ijzerman, A.P.1    Kouronakis, A.2    van der Klein, P.3
  • 33
    • 0025603686 scopus 로고
    • Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes
    • Bruns, R.F.; Fergus, J.H. Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes. Mol. Pharmacol., 1990, 38, 939-949.
    • (1990) Mol. Pharmacol , vol.38 , pp. 939-949
    • Bruns, R.F.1    Fergus, J.H.2
  • 34
  • 35
    • 0032590063 scopus 로고    scopus 로고
    • Adenosine A1 receptor-dependent and-independent effects of the allosteric enhancer PD 81,723
    • Musser, B.; Mudumbi, R.V.; Liu, J.; Olson, R.D.; Vestal, R.E. Adenosine A1 receptor-dependent and-independent effects of the allosteric enhancer PD 81,723. J. Pharmacol. Exp. Ther., 1999, 288, 446-454
    • (1999) J. Pharmacol. Exp. Ther , vol.288 , pp. 446-454
    • Musser, B.1    Mudumbi, R.V.2    Liu, J.3    Olson, R.D.4    Vestal, R.E.5
  • 36
    • 0029895280 scopus 로고    scopus 로고
    • Effects of long-term treatment with the allosteric enhancer, PD-81,723, on Chinese hamster ovary cells expressing recombinant human A1 adenosine receptors
    • Bhattacharya, S.; Linden, J. Effects of long-term treatment with the allosteric enhancer, PD-81,723, on Chinese hamster ovary cells expressing recombinant human A1 adenosine receptors. Mol. Pharmacol., 1996, 50, 104-111.
    • (1996) Mol. Pharmacol , vol.50 , pp. 104-111
    • Bhattacharya, S.1    Linden, J.2
  • 37
    • 0027247826 scopus 로고
    • The adenosine binding enhancer, PD 81,723 inhibits epileptiform bursting in the hippocampal brain slice
    • Janusz, C.A.; Berman R.F: The adenosine binding enhancer, PD 81,723 inhibits epileptiform bursting in the hippocampal brain slice. Brain Res., 1993, 619, 131-136.
    • (1993) Brain Res , vol.619 , pp. 131-136
    • Janusz, C.A.1    Berman, R.F.2
  • 38
    • 0027340584 scopus 로고
    • Selective potentiation by an A1 adenosine receptor enhancer of the negative dromotropic action of adenosine in the guinea pig heart
    • Amoah-Apraku, B.; Xu, J.; Lu, J J.Y.; Pelleg, A.; Bruns, R.F.; Belardinelli, L: Selective potentiation by an A1 adenosine receptor enhancer of the negative dromotropic action of adenosine in the guinea pig heart. J. Pharmacol. Exp. Ther., 1993, 266, 611-617.
    • (1993) J. Pharmacol. Exp. Ther , vol.266 , pp. 611-617
    • Amoah-Apraku, B.1    Xu, J.2    Lu, J.J.Y.3    Pelleg, A.4    Bruns, R.F.5    Belardinelli, L.6
  • 39
    • 0028888293 scopus 로고
    • The allosteric enhancer P.D. 81,723, stabilizes human A1 adenosine receptor coupling to G proteins
    • Bhattacharaya, S.; Linden, J. The allosteric enhancer, PD 81,723, stabilizes human A1 adenosine receptor coupling to G proteins. Biochim. Biophys. Acta, 1995, 1265, 15-21
    • (1995) Biochim. Biophys. Acta , vol.1265 , pp. 15-21
    • Bhattacharaya, S.1    Linden, J.2
  • 40
    • 0029895280 scopus 로고    scopus 로고
    • Effects of long-term treatment with the allosteric enhancer, PD81,723, on Chinese hamster ovary cells expressing recombinant human A1 adenosine receptors
    • Bhattacharaya, S.; Linden, J. Effects of long-term treatment with the allosteric enhancer, PD81,723, on Chinese hamster ovary cells expressing recombinant human A1 adenosine receptors. Mol. Pharmacol., 1996, 50, 104-111
    • (1996) Mol. Pharmacol , vol.50 , pp. 104-111
    • Bhattacharaya, S.1    Linden, J.2
  • 41
    • 0035863033 scopus 로고    scopus 로고
    • Differential effects of the allosteric enhancer (2amino-4,5-dimethyl-thienyl)][3-(trifluoromethyl)phenyl]methanone (PD 81,723) on agonist and antagonist binding and function at the human wild-type and a mutant (T277A) adenosine A1 receptor
    • Kourounakis, A.P.; Visser, C.; De Groote, M.; IJzerman, A.P. Differential effects of the allosteric enhancer (2amino-4,5-dimethyl-thienyl)][3-(trifluoromethyl)phenyl]methanone (PD 81,723) on agonist and antagonist binding and function at the human wild-type and a mutant (T277A) adenosine A1 receptor. Biochem. Pharmacol., 2001, 61, 137-144.
    • (2001) Biochem. Pharmacol , vol.61 , pp. 137-144
    • Kourounakis, A.P.1    Visser, C.2    de Groote, M.3    Ijzerman, A.P.4
  • 42
    • 2042463610 scopus 로고
    • Cardiac functional responses to adenosine by PD 81,723, an allosteric enhancer of the adenosine A1 receptor
    • Mudumbi, R.V.; Montamat, S.C.; Bruns, R.F.; Vestal, R.E. Cardiac functional responses to adenosine by PD 81,723, an allosteric enhancer of the adenosine A1 receptor. Am. J. Physiol., 1993, 264, H1017-H1022.
    • (1993) Am. J. Physiol , vol.264 , pp. 1017-1022
    • Mudumbi, R.V.1    Montamat, S.C.2    Bruns, R.F.3    Vestal, R.E.4
  • 43
    • 0029816510 scopus 로고    scopus 로고
    • PD 81,723, an allosteric enhancer of the A1 adenosine receptor, lowers the threshold for ischemic preconditioning in dogs
    • Mizamura, T.; Auchampach, J.A.; Linden, J.; Bruns, R.F.; Gross, G.J. PD 81,723, an allosteric enhancer of the A1 adenosine receptor, lowers the threshold for ischemic preconditioning in dogs. Circ. Res., 1996, 79, 415-423.
    • (1996) Circ. Res , vol.79 , pp. 415-423
    • Mizamura, T.1    Auchampach, J.A.2    Linden, J.3    Bruns, R.F.4    Gross, G.J.5
  • 45
    • 0033539111 scopus 로고    scopus 로고
    • Allosteric modulation of the adenosine A1 receptor: Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding
    • van der Klein, P.A.M.; Kourounakis, A.P.; IJzerman, A.P. Allosteric modulation of the adenosine A1 receptor: synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding, J. Med. Chem., 1999, 42, 3629-3635.
    • (1999) J. Med. Chem , vol.42 , pp. 3629-3635
    • van der Klein, P.A.M.1    Kourounakis, A.P.2    Ijzerman, A.P.3
  • 46
    • 0033916799 scopus 로고    scopus 로고
    • Elucidation of stucture-activity relationships of 2-amino-3benzoylthiophenes:Study of their allosteric enhanceing vs. antagonistic activity on adenosine A1 receptors
    • Kourounakis, A.P.; van der Klein, P.A.M.; IJzerman, A.P. Elucidation of stucture-activity relationships of 2-amino-3benzoylthiophenes:study of their allosteric enhanceing vs. antagonistic activity on adenosine A1 receptors. Drug Dev. Res., 2000, 49, 227-237.
    • (2000) Drug Dev. Res , vol.49 , pp. 227-237
    • Kourounakis, A.P.1    van der Klein, P.A.M.2    Ijzerman, A.P.3
  • 48
    • 3142576214 scopus 로고    scopus 로고
    • 2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: New 3, 4-, and 5-modifications
    • Luetjens, H.; Zickgraf, A.; Figler, H.; Linden, J.; Olsson, R.A.; Scammells, P.J. 2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications. J. Med. Chem., 2003, 46, 1870-1877.
    • (2003) J. Med. Chem , vol.46 , pp. 1870-1877
    • Luetjens, H.1    Zickgraf, A.2    Figler, H.3    Linden, J.4    Olsson, R.A.5    Scammells, P.J.6
  • 49
    • 18144408044 scopus 로고    scopus 로고
    • Allosteric modulation of adenosine A1 receptor coupling to G-proteins in brain
    • For a complete pharmacological characterization of T-62 see
    • For a complete pharmacological characterization of T-62 see: a) Childers, S.R.; Li, X.; Xiao, R.; Eisanach, J.C. Allosteric modulation of adenosine A1 receptor coupling to G-proteins in brain. J. Neurochem., 2005, 93, 715-723
    • (2005) J. Neurochem , vol.93 , pp. 715-723
    • Childers, S.R.1    Li, X.2    Xiao, R.3    Eisanach, J.C.4
  • 50
    • 0036276780 scopus 로고    scopus 로고
    • Spinal noradrenergic activation mediates allodynia reduction from an allosteric adenosine modulator in a rat model of neuropathic pain
    • Li, X.; Conklin, D.; Ma, W.; Zhu, X. Eisenach, J.C. Spinal noradrenergic activation mediates allodynia reduction from an allosteric adenosine modulator in a rat model of neuropathic pain. Pain 2002, 97, 117-125
    • (2002) Pain , vol.97 , pp. 117-125
    • Li, X.1    Conklin, D.2    Ma, W.3    Zhu, X.4    Eisenach, J.C.5
  • 51
    • 0038814252 scopus 로고    scopus 로고
    • Allosteric adenosine receptor modulation reduces hypersensitivity following peripheral inflammation by a central mechanism
    • Li, X.; Conklin, D.; Pan, H.-L.; Eisenach, J.C. Allosteric adenosine receptor modulation reduces hypersensitivity following peripheral inflammation by a central mechanism. J. Pharmacol. Exp. Ther., 2003, 305, 950-955
    • (2003) J. Pharmacol. Exp. Ther , vol.305 , pp. 950-955
    • Li, X.1    Conklin, D.2    Pan, H.-L.3    Eisenach, J.C.4
  • 52
    • 77957956904 scopus 로고    scopus 로고
    • ClinicalTrials.gov Identifier: NCT00809679
    • ClinicalTrials.gov Identifier: NCT00809679.
  • 53
    • 4644221135 scopus 로고    scopus 로고
    • Synthesis of 2-amino-3heteroaroylthiophenes and evaluation of their activity as potential allosteric enhancers at the human A1 receptor
    • Baraldi, P.G.; Pavani, M.G.; Shryock J.C.; Moorman, A.R.; Iannotta, V.; Borea, P.A.; Romagnoli, R. Synthesis of 2-amino-3heteroaroylthiophenes and evaluation of their activity as potential allosteric enhancers at the human A1 receptor. Eur. J. Med. Chem., 2004, 39, 855-865.
    • (2004) Eur. J. Med. Chem , vol.39 , pp. 855-865
    • Baraldi, P.G.1    Pavani, M.G.2    Shryock, J.C.3    Moorman, A.R.4    Iannotta, V.5    Borea, P.A.6    Romagnoli, R.7
  • 55
    • 32844467152 scopus 로고    scopus 로고
    • Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers
    • Nikolakopoulos, G.; Figler, H.; Linden, J.; Scammells, P.J. Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers. Bioorg. Med. Chem., 2006, 14, 2358-2365.
    • (2006) Bioorg. Med. Chem , vol.14 , pp. 2358-2365
    • Nikolakopoulos, G.1    Figler, H.2    Linden, J.3    Scammells, P.J.4
  • 56
    • 0346996805 scopus 로고    scopus 로고
    • Allosteric enhancers of A1 adenosine receptors increase receptor-G protein coupling and counteract guanine nucleotide effects on agonist binding
    • Figler, H.; Olsson, R.A.; Linden, J. Allosteric enhancers of A1 adenosine receptors increase receptor-G protein coupling and counteract guanine nucleotide effects on agonist binding. Mol. Pharmacol., 2003, 64, 1557-1564.
    • (2003) Mol. Pharmacol , vol.64 , pp. 1557-1564
    • Figler, H.1    Olsson, R.A.2    Linden, J.3
  • 57
    • 71749111336 scopus 로고    scopus 로고
    • 3and 6infstituted 2-amino-4,5,6,7-tetrahydro[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists
    • Aurelio, L.; Valant, C.; Figler, H.; Flynn, B.L.; Linden, J.; Sexton, P.M.; Christopoulos, A.; Scammells, P.J. 3and 6infstituted 2-amino-4,5,6,7-tetrahydro[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. Bioorg. Med. Chem., 2009, 17, 7353-7361
    • (2009) Bioorg. Med. Chem , vol.17 , pp. 7353-7361
    • Aurelio, L.1    Valant, C.2    Figler, H.3    Flynn, B.L.4    Linden, J.5    Sexton, P.M.6    Christopoulos, A.7    Scammells, P.J.8
  • 59
    • 67650756920 scopus 로고    scopus 로고
    • Allosteric modulators of the adenosine A1 receptor: Synthesis and pharmacological evaluation of 4-infstituted 2-amino-3-benzoylthiophenes
    • Aurelio, L.; Valant, C.; Flynn, B.L.; Sexton, P.M.; Christopoulos, A.; Scammells, P.J. Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-infstituted 2-amino-3-benzoylthiophenes. J. Med. Chem., 2009, 52, 4543-4547.
    • (2009) J. Med. Chem , vol.52 , pp. 4543-4547
    • Aurelio, L.1    Valant, C.2    Flynn, B.L.3    Sexton, P.M.4    Christopoulos, A.5    Scammells, P.J.6
  • 60
    • 38849185360 scopus 로고    scopus 로고
    • 5infstituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers
    • Aurelio, L.; Figler, H.; Flynn, B.L.; Linden, J.; Scammells, P.J. 5infstituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers. Bioorg. Med. Chem., 2008, 16, 1319-1327.
    • (2008) Bioorg. Med. Chem , vol.16 , pp. 1319-1327
    • Aurelio, L.1    Figler, H.2    Flynn, B.L.3    Linden, J.4    Scammells, P.J.5
  • 63
    • 34047231267 scopus 로고    scopus 로고
    • On the stability of aminoselenophene-3-carboxylates: Potential dualacting selenium-containing allosteric enhancers of A1 adenosine receptor binding
    • Aumann, K.M.; Scammells, P.J.; White, J.M.; Schiesser, C.H. On the stability of aminoselenophene-3-carboxylates: potential dualacting selenium-containing allosteric enhancers of A1 adenosine receptor binding. Org. Biomol. Chem., 2007, 5, 1276-1281.
    • (2007) Org. Biomol. Chem , vol.5 , pp. 1276-1281
    • Aumann, K.M.1    Scammells, P.J.2    White, J.M.3    Schiesser, C.H.4
  • 65
    • 23444458267 scopus 로고    scopus 로고
    • 6-Aryl-8H-indeno[1,2-d]thiazol-2ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency
    • Chordia, M.D.; Zigler, M.; Murphree, L.J.; Figler, H.; Macdonald, T.L.; Olsson, R.A.; Linden J. 6-Aryl-8H-indeno[1,2-d]thiazol-2ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency. J. Med. Chem., 2005, 48, 5131-5139.
    • (2005) J. Med. Chem , vol.48 , pp. 5131-5139
    • Chordia, M.D.1    Zigler, M.2    Murphree, L.J.3    Figler, H.4    Macdonald, T.L.5    Olsson, R.A.6    Linden, J.7
  • 66
    • 13844310156 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of 2-aminothiazoles and their amide derivatives on human adenosine receptors: Lack of effect of 2aminothiazoles as allosteric enhancers
    • Göblyös, A.; Santiago, S.N.; Pietra, D.; Mulder-Krieger, T.; von Frijtag Drabbe Künzel, J.; Brussee, J.; IJzerman, A.P. Synthesis and biological evaluation of 2-aminothiazoles and their amide derivatives on human adenosine receptors: lack of effect of 2aminothiazoles as allosteric enhancers. Bioorg. Med. Chem., 2005, 13, 2079-2087.
    • (2005) Bioorg. Med. Chem , vol.13 , pp. 2079-2087
    • Göblyös, A.1    Santiago, S.N.2    Pietra, D.3    Mulder-Krieger, T.4    von Frijtag Drabbe Künzel,, J.5    Brussee, J.6    Ijzerman, A.P.7


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