- TETRAHYDROPYRIDINE DERIVATIVES AS DOPAMINE RECEPTOR SUBTYPE LIGANDS
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A class of 1,2,3,6-tetrahydropyridine derivatives, substituted in the 4-position by a fused bicyclic heteroaromatic moiety and in the 1-position by an optionally substituted benzyl moiety, are ligands for dopamine receptor subtypes within the body, in particular the D 4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.
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- 4-Heterocyclyl tetrahydropyridines as selective ligands for the human dopamine D4 receptor.
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A series of 1,2,3,6-tetrahydropyridines 3 were synthesised, which resulted in selective high affinity dopamine D4 ligands. The SAR of heterocyclic replacements and aromatic substitution was investigated, leading to compounds of nanomolar bindin
- Haworth,Harrison,Kulagowski,Leeson,Owens,Ridgill,Teall,Fielding,Chapman,Emms,Marwood,Patel,Moss
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p. 2211 - 2216
(2007/10/03)
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