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Items: 1 to 20 of 156

1.

Characterization of the potent and highly selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] in rodent models of movement disorders and depression.

Hodgson RA, Bertorelli R, Varty GB, Lachowicz JE, Forlani A, Fredduzzi S, Cohen-Williams ME, Higgins GA, Impagnatiello F, Nicolussi E, Parra LE, Foster C, Zhai Y, Neustadt BR, Stamford AW, Parker EM, Reggiani A, Hunter JC.

J Pharmacol Exp Ther. 2009 Jul;330(1):294-303. doi: 10.1124/jpet.108.149617. Epub 2009 Mar 30.

4.

Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders.

Hodgson RA, Bedard PJ, Varty GB, Kazdoba TM, Di Paolo T, Grzelak ME, Pond AJ, Hadjtahar A, Belanger N, Gregoire L, Dare A, Neustadt BR, Stamford AW, Hunter JC.

Exp Neurol. 2010 Oct;225(2):384-90. doi: 10.1016/j.expneurol.2010.07.011. Epub 2010 Jul 23.

PMID:
20655910
5.

Effects of the selective adenosine A2A receptor antagonist, SCH 412348, on the parkinsonian phenotype of MitoPark mice.

Smith KM, Browne SE, Jayaraman S, Bleickardt CJ, Hodge LM, Lis E, Yao L, Rittle SL, Innocent N, Mullins DE, Boykow G, Reynolds IJ, Hill D, Parker EM, Hodgson RA.

Eur J Pharmacol. 2014 Apr 5;728:31-8. doi: 10.1016/j.ejphar.2014.01.052. Epub 2014 Jan 31.

PMID:
24486705
6.

JNJ-40255293, a novel adenosine A2A/A1 antagonist with efficacy in preclinical models of Parkinson's disease.

Atack JR, Shook BC, Rassnick S, Jackson PF, Rhodes K, Drinkenburg WH, Ahnaou A, Te Riele P, Langlois X, Hrupka B, De Haes P, Hendrickx H, Aerts N, Hens K, Wellens A, Vermeire J, Megens AA.

ACS Chem Neurosci. 2014 Oct 15;5(10):1005-19. doi: 10.1021/cn5001606. Epub 2014 Sep 24.

PMID:
25203719
7.

Binding of the radioligand [3H]-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatal membranes.

Zocchi C, Ongini E, Ferrara S, Baraldi PG, Dionisotti S.

Br J Pharmacol. 1996 Apr;117(7):1381-6.

8.

Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines.

Neustadt BR, Liu H, Hao J, Greenlee WJ, Stamford AW, Foster C, Arik L, Lachowicz J, Zhang H, Bertorelli R, Fredduzzi S, Varty G, Cohen-Williams M, Ng K.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):967-71. doi: 10.1016/j.bmcl.2008.11.075. Epub 2008 Nov 24.

PMID:
19109019
9.

Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.

Dionisotti S, Ongini E, Zocchi C, Kull B, Arslan G, Fredholm BB.

Br J Pharmacol. 1997 Jun;121(3):353-60.

11.

Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, 5-[5-amino-3-(4-fluorophenyl)pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one (ASP5854), in models of Parkinson's disease and cognition.

Mihara T, Mihara K, Yarimizu J, Mitani Y, Matsuda R, Yamamoto H, Aoki S, Akahane A, Iwashita A, Matsuoka N.

J Pharmacol Exp Ther. 2007 Nov;323(2):708-19. Epub 2007 Aug 7.

12.

Adenosine A2A receptors and depression.

El Yacoubi M, Costentin J, Vaugeois JM.

Neurology. 2003 Dec 9;61(11 Suppl 6):S82-7.

PMID:
14663017
13.

2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1.

Matasi JJ, Caldwell JP, Zhang H, Fawzi A, Cohen-Williams ME, Varty GB, Tulshian DB.

Bioorg Med Chem Lett. 2005 Aug 15;15(16):3670-4.

PMID:
15978806
14.
15.

The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist.

Zocchi C, Ongini E, Conti A, Monopoli A, Negretti A, Baraldi PG, Dionisotti S.

J Pharmacol Exp Ther. 1996 Feb;276(2):398-404.

PMID:
8632302
16.

The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.

Jones CK, Bubser M, Thompson AD, Dickerson JW, Turle-Lorenzo N, Amalric M, Blobaum AL, Bridges TM, Morrison RD, Jadhav S, Engers DW, Italiano K, Bode J, Daniels JS, Lindsley CW, Hopkins CR, Conn PJ, Niswender CM.

J Pharmacol Exp Ther. 2012 Feb;340(2):404-21. doi: 10.1124/jpet.111.187443. Epub 2011 Nov 16.

18.

Synthesis and preclinical evaluation of 2-(2-furanyl)-7-[2-[4-[4-(2-[11C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine ([11C]Preladenant) as a PET tracer for the imaging of cerebral adenosine A2A receptors.

Zhou X, Khanapur S, Huizing AP, Zijlma R, Schepers M, Dierckx RA, van Waarde A, de Vries EF, Elsinga PH.

J Med Chem. 2014 Nov 13;57(21):9204-10. doi: 10.1021/jm501065t. Epub 2014 Oct 15.

PMID:
25279444
19.

Adenosine A₂A receptors inhibit delayed rectifier potassium currents and cell differentiation in primary purified oligodendrocyte cultures.

Coppi E, Cellai L, Maraula G, Pugliese AM, Pedata F.

Neuropharmacology. 2013 Oct;73:301-10. doi: 10.1016/j.neuropharm.2013.05.035. Epub 2013 Jun 13.

PMID:
23770463
20.

Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists.

Shah U, Boyle CD, Chackalamannil S, Neustadt BR, Lindo N, Greenlee WJ, Foster C, Arik L, Zhai Y, Ng K, Wang S, Monopoli A, Lachowicz JE.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4199-203. doi: 10.1016/j.bmcl.2008.05.074. Epub 2008 May 22.

PMID:
18562199

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