2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.

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Bergauer M, Hubner H, Gmeiner P

2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):1937-40.

PubMed ID

12113813 [ View in PubMed

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Abstract

Solution-phase synthesis and a solid-phase supported approach to piperazinylmethyl substituted pyrroles are described. Receptor binding studies and the measurement of D4 ligand efficacy led to the ethynylpyrrole 1d (FAUC 356) exerting selective D4 binding and substantial ligand efficacy (66%, EC(50)=1.9nM). This activity profile might be of interest for the treatment of ADHD.

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