4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.

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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

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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.

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