Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.

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Lober S, Aboul-Fadl T, Hubner H, Gmeiner P

Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):633-6.

PubMed ID

11844688 [ View in PubMed

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Abstract

Based on the lead molecule FAUC 113, a series of di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives was synthesized and investigated for their dopamine receptor binding profile. The carbonitrile 11a (FAUC 327) showed excellent pharmacological properties combining high D4 affinity (K(i)=1.5 nM) and selectivity with significant intrinsic activity (31%) in low nanomolar concentrations (EC50=1.5 nM).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	Dopamine D2 receptor	Ki (nM)	28	N/A	N/A	Details
Clozapine	Dopamine D2 receptor	Ki (nM)	41	N/A	N/A	Details
Clozapine	Dopamine D3 receptor	Ki (nM)	960	N/A	N/A	Details
Clozapine	Dopamine D4 receptor	Ki (nM)	16	N/A	N/A	Details