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Items: 32


Dopamine D4 Receptor-Selective Compounds Reveal Structure-Activity Relationships that Engender Agonist Efficacy.

Keck TM, Free RB, Day MM, Brown SL, Maddaluna MS, Fountain G, Cooper C, Fallon B, Holmes M, Stang CT, Burkhardt R, Bonifazi A, Ellenberger MP, Newman AH, Sibley DR, Wu C, Boateng CA.

J Med Chem. 2019 Apr 11;62(7):3722-3740. doi: 10.1021/acs.jmedchem.9b00231. Epub 2019 Apr 1.


New roles for dopamine D2 and D3 receptors in pancreatic beta cell insulin secretion.

Farino ZJ, Morgenstern TJ, Maffei A, Quick M, De Solis AJ, Wiriyasermkul P, Freyberg RJ, Aslanoglou D, Sorisio D, Inbar BP, Free RB, Donthamsetti P, Mosharov EV, Kellendonk C, Schwartz GJ, Sibley DR, Schmauss C, Zeltser LM, Moore H, Harris PE, Javitch JA, Freyberg Z.

Mol Psychiatry. 2019 Jan 9. doi: 10.1038/s41380-018-0344-6. [Epub ahead of print]


Identification of Positive Allosteric Modulators of the D1 Dopamine Receptor That Act at Diverse Binding Sites.

Luderman KD, Conroy JL, Free RB, Southall N, Ferrer M, Sanchez-Soto M, Moritz AE, Willette BKA, Fyfe TJ, Jain P, Titus S, Hazelwood LA, Aubé J, Lane JR, Frankowski KJ, Sibley DR.

Mol Pharmacol. 2018 Oct;94(4):1197-1209. doi: 10.1124/mol.118.113175. Epub 2018 Aug 1.


Structure-Activity Investigation of a G Protein-Biased Agonist Reveals Molecular Determinants for Biased Signaling of the D2 Dopamine Receptor.

Chun LS, Vekariya RH, Free RB, Li Y, Lin DT, Su P, Liu F, Namkung Y, Laporte SA, Moritz AE, Aubé J, Frankowski KJ, Sibley DR.

Front Synaptic Neurosci. 2018 Feb 21;10:2. doi: 10.3389/fnsyn.2018.00002. eCollection 2018.


The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors.

Verma RK, Abramyan AM, Michino M, Free RB, Sibley DR, Javitch JA, Lane JR, Shi L.

PLoS Comput Biol. 2018 Jan 16;14(1):e1005948. doi: 10.1371/journal.pcbi.1005948. eCollection 2018 Jan.


Advances and challenges in the search for D2 and D3 dopamine receptor-selective compounds.

Moritz AE, Free RB, Sibley DR.

Cell Signal. 2018 Jan;41:75-81. doi: 10.1016/j.cellsig.2017.07.003. Epub 2017 Jul 14. Review.


Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R).

Kumar V, Moritz AE, Keck TM, Bonifazi A, Ellenberger MP, Sibley CD, Free RB, Shi L, Lane JR, Sibley DR, Newman AH.

J Med Chem. 2017 Feb 23;60(4):1478-1494. doi: 10.1021/acs.jmedchem.6b01688. Epub 2017 Feb 10.


Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.

Zou MF, Keck TM, Kumar V, Donthamsetti P, Michino M, Burzynski C, Schweppe C, Bonifazi A, Free RB, Sibley DR, Janowsky A, Shi L, Javitch JA, Newman AH.

J Med Chem. 2016 Apr 14;59(7):2973-88. doi: 10.1021/acs.jmedchem.5b01612. Epub 2016 Apr 1.


Structural basis for Na(+)-sensitivity in dopamine D2 and D3 receptors.

Michino M, Free RB, Doyle TB, Sibley DR, Shi L.

Chem Commun (Camb). 2015 May 21;51(41):8618-21. doi: 10.1039/c5cc02204e.


Identification of G protein-biased agonists that fail to recruit β-arrestin or promote internalization of the D1 dopamine receptor.

Conroy JL, Free RB, Sibley DR.

ACS Chem Neurosci. 2015 Apr 15;6(4):681-92. doi: 10.1021/acschemneuro.5b00020. Epub 2015 Feb 20.


Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonists.

Furman CA, Roof RA, Moritz AE, Miller BN, Doyle TB, Free RB, Banala AK, Paul NM, Kumar V, Sibley CD, Newman AH, Sibley DR.

Eur Neuropsychopharmacol. 2015 Sep;25(9):1448-61. doi: 10.1016/j.euroneuro.2014.11.013. Epub 2014 Nov 29.


(-)-Stepholidine is a potent pan-dopamine receptor antagonist of both G protein- and β-arrestin-mediated signaling.

Meade JA, Free RB, Miller NR, Chun LS, Doyle TB, Moritz AE, Conroy JL, Watts VJ, Sibley DR.

Psychopharmacology (Berl). 2015 Mar;232(5):917-30. doi: 10.1007/s00213-014-3726-8. Epub 2014 Sep 18.


Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor.

Free RB, Chun LS, Moritz AE, Miller BN, Doyle TB, Conroy JL, Padron A, Meade JA, Xiao J, Hu X, Dulcey AE, Han Y, Duan L, Titus S, Bryant-Genevier M, Barnaeva E, Ferrer M, Javitch JA, Beuming T, Shi L, Southall NT, Marugan JJ, Sibley DR.

Mol Pharmacol. 2014 Jul;86(1):96-105. doi: 10.1124/mol.113.090563. Epub 2014 Apr 22.


Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.

Xiao J, Free RB, Barnaeva E, Conroy JL, Doyle T, Miller B, Bryant-Genevier M, Taylor MK, Hu X, Dulcey AE, Southall N, Ferrer M, Titus S, Zheng W, Sibley DR, Marugan JJ.

J Med Chem. 2014 Apr 24;57(8):3450-63. doi: 10.1021/jm500126s. Epub 2014 Apr 10.


Discovery, optimization, and characterization of a novel series of dopamine D2 versus D3 receptor selective antagonists.

Xiao J, Free RB, Barnaeva E, Conroy J, Doyle T, Bryant-Genevier M, Taylor MK, Southall N, Hu X, Ferrer M, Titus S, Zheng W, Sibley DR, Marugan JJ.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 25 [updated 2013 Sep 3].


D1-D2 dopamine receptor synergy promotes calcium signaling via multiple mechanisms.

Chun LS, Free RB, Doyle TB, Huang XP, Rankin ML, Sibley DR.

Mol Pharmacol. 2013 Aug;84(2):190-200. doi: 10.1124/mol.113.085175. Epub 2013 May 16.


Identifying novel protein-protein interactions using co-immunoprecipitation and mass spectroscopy.

Free RB, Hazelwood LA, Sibley DR.

Curr Protoc Neurosci. 2009 Jan;Chapter 5:Unit 5.28. doi: 10.1002/0471142301.ns0528s46.


Reciprocal modulation of function between the D1 and D2 dopamine receptors and the Na+,K+-ATPase.

Hazelwood LA, Free RB, Cabrera DM, Skinbjerg M, Sibley DR.

J Biol Chem. 2008 Dec 26;283(52):36441-53. doi: 10.1074/jbc.M805520200. Epub 2008 Nov 4.


D1 and D2 dopamine receptor expression is regulated by direct interaction with the chaperone protein calnexin.

Free RB, Hazelwood LA, Cabrera DM, Spalding HN, Namkung Y, Rankin ML, Sibley DR.

J Biol Chem. 2007 Jul 20;282(29):21285-300. Epub 2007 Mar 29.


cAMP-Coupled riboflavin trafficking in placental trophoblasts: a dynamic and ordered process.

D'Souza VM, Foraker AB, Free RB, Ray A, Shapiro PS, Swaan PW.

Biochemistry. 2006 May 16;45(19):6095-104.


Pharmacological characterization of recombinant bovine alpha3beta4 neuronal nicotinic receptors stably expressed in HEK 293 cells.

Free RB, von Fischer ND, Boyd RT, McKay DB.

Neurosci Lett. 2003 Jun 12;343(3):180-4.


Characterization of [(3)H]epibatidine binding to nicotinic receptors from bovine adrenal medulla.

McKay DB, Free RB, Kaser DJ, McKay SB.

Ann N Y Acad Sci. 2002 Oct;971:162-4. Review. No abstract available.


Evidence for constitutive expression of bovine adrenal a3beta4* nicotinic acetylcholine receptors.

Free RB, McKay SB, Boyd RT, McKay DB.

Ann N Y Acad Sci. 2002 Oct;971:145-7.


Effects of methyllycaconitine and related analogues on bovine adrenal alpha3beta4* nicotinic acetylcholine receptors.

Bryant DL, Free RB, Thomasy SM, Lapinsky DJ, Ismail KA, Arason KM, Bergmeier SC, McKay DB.

Ann N Y Acad Sci. 2002 Oct;971:139-41. Review.


[3H]Epibatidine binding to bovine adrenal medulla: evidence for alpha3beta4* nicotinic receptors.

Free RB, Bryant DL, McKay SB, Kaser DJ, McKay DB.

Neurosci Lett. 2002 Jan 25;318(2):98-102.


Structure-activity studies with ring E analogues of methyllycaconitine on bovine adrenal alpha3beta4* nicotinic receptors.

Bryant DL, Free RB, Thomasy SM, Lapinsky DJ, Ismail KA, McKay SB, Bergmeier SC, McKay DB.

Neurosci Res. 2002 Jan;42(1):57-63.


Ring E analogs of methyllycaconitine (MLA) as novel nicotinic antagonists.

Bergmeier SC, Lapinsky DJ, Free RB, McKay DB.

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2263-6.


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