4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.
Article Details
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Moore KW, Bonner K, Jones EA, Emms F, Leeson PD, Marwood R, Patel S, Patel S, Rowley M, Thomas S, Carling RW
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.
Bioorg Med Chem Lett. 1999 May 3;9(9):1285-90.
- PubMed ID
- 10340615 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Clozapine Dopamine D2 receptor Ki (nM) 74 N/A N/A Details Clozapine Dopamine D3 receptor Ki (nM) 200 N/A N/A Details Clozapine Dopamine D4 receptor Ki (nM) 10 N/A N/A Details