4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors. |
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| Authors: | K W Moore K Bonner E A Jones F Emms P D Leeson R Marwood S Patel S Patel M Rowley S Thomas R W Carling |
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| Affiliation: | Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Harlow, Essex, UK. Kevin_Moore@Merck.com |
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| Abstract: | The syntheses of a number of different N-linked heterocyclic pyrazole replacements based on the structure 1 are described (compounds 3-12) as hD4 ligands. After further optimisation the best compound identified was 13 which has high affinity for hD4 (5.2 nM) and >300-fold selectivity for hD4 receptors over hD2 and hD3 receptors. |
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