Structure–activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-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
We recently demonstrated that SB269652 (1) engages one protomer of a dopamine D2 receptor (D2R) dimer in a bitopic mode to allosterically inhibit the binding of dopamine at the other protomer. Herein, we investigate structural deter- minants for allostery, focusing on modifications to three moieties...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
American Chemical Society
2015
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| Online Access: | http://eprints.nottingham.ac.uk/30314/ http://eprints.nottingham.ac.uk/30314/ http://eprints.nottingham.ac.uk/30314/ http://eprints.nottingham.ac.uk/30314/1/jm-2015-00581p.R2%20-%20JMC%2058%2813%29%202015%205287.pdf |