Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor |
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| Authors: | Austin N E Avenell K Y Boyfield I Branch C L Hadley M S Jeffrey P Johnson C N Macdonald G J Nash D J Riley G J Smith A B Stemp G Thewlis K M Vong A K Wood M |
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| Institution: | SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK. |
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| Abstract: | Starting from the dopamine D3 receptor antagonist SB-277011 1, a series of 2,3,4,5-tetrahydro-1H-3-benzazepines has been identified with high affinity for the dopamine D3 receptor and selectivity over the D2 receptor. The 3-acetamido-2-fluorocinnamide derivative 20 gave high D3 receptor affinity (pKi 8.4) with 130-fold selectivity over the 2, receptor. |
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