1: Kopinathan A, Draper-Joyce C, Szabo M, Christopoulos A, Scammells PJ, Lane JR, Capuano B. Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity at the Dopamine D2 Receptor. J Med Chem. 2019 Jan 10;62(1):371-377. doi: 10.1021/acs.jmedchem.8b00192. Epub 2018 Jul 2. PMID: 29890071.
2: Draper-Joyce CJ, Verma RK, Michino M, Shonberg J, Kopinathan A, Klein Herenbrink C, Scammells PJ, Capuano B, Abramyan AM, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR. The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions. Sci Rep. 2018 Jan 19;8(1):1208. doi: 10.1038/s41598-018-19642-1. PMID: 29352161; PMCID: PMC5775417.
3: Verma RK, Abramyan AM, Michino M, Free RB, Sibley DR, Javitch JA, Lane JR, Shi L. The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors. PLoS Comput Biol. 2018 Jan 16;14(1):e1005948. doi: 10.1371/journal.pcbi.1005948. PMID: 29337986; PMCID: PMC5786319.
4: Draper-Joyce CJ, Michino M, Verma RK, Klein Herenbrink C, Shonberg J, Kopinathan A, Scammells PJ, Capuano B, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR. The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor. Biochem Pharmacol. 2018 Feb;148:315-328. doi: 10.1016/j.bcp.2018.01.002. Epub 2018 Jan 9. PMID: 29325769; PMCID: PMC5800995.
5: Rossi M, Fasciani I, Marampon F, Maggio R, Scarselli M. The First Negative Allosteric Modulator for Dopamine D2 and D3 Receptors, SB269652 May Lead to a New Generation of Antipsychotic Drugs. Mol Pharmacol. 2017 Jun;91(6):586-594. doi: 10.1124/mol.116.107607. Epub 2017 Mar 6. PMID: 28265019; PMCID: PMC5438131.
6: Mistry SN, Shonberg J, Draper-Joyce CJ, Klein Herenbrink C, Michino M, Shi L, Christopoulos A, Capuano B, Scammells PJ, Lane JR. Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand. J Med Chem. 2015 Sep 10;58(17):6819-43. doi: 10.1021/acs.jmedchem.5b00585. Epub 2015 Aug 28. PMID: 26258690; PMCID: PMC10823399.
7: Shonberg J, Draper-Joyce C, Mistry SN, Christopoulos A, Scammells PJ, Lane JR, Capuano B. Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroi soquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor. J Med Chem. 2015 Jul 9;58(13):5287-307. doi: 10.1021/acs.jmedchem.5b00581. Epub 2015 Jun 24. PMID: 26052807.
8: Lane JR, Donthamsetti P, Shonberg J, Draper-Joyce CJ, Dentry S, Michino M, Shi L, López L, Scammells PJ, Capuano B, Sexton PM, Javitch JA, Christopoulos A. A new mechanism of allostery in a G protein-coupled receptor dimer. Nat Chem Biol. 2014 Sep;10(9):745-52. doi: 10.1038/nchembio.1593. Epub 2014 Aug 10. PMID: 25108820; PMCID: PMC4138267.
9: Presgraves SP, Borwege S, Millan MJ, Joyce JN. Involvement of dopamine D(2)/D(3) receptors and BDNF in the neuroprotective effects of S32504 and pramipexole against 1-methyl-4-phenylpyridinium in terminally differentiated SH- SY5Y cells. Exp Neurol. 2004 Nov;190(1):157-70. doi: 10.1016/j.expneurol.2004.06.021. PMID: 15473989.