Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
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Lober S, Hubner H, Utz W, Gmeiner P
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
J Med Chem. 2001 Aug 16;44(17):2691-4.
- PubMed ID
- 11495580 [ View in PubMed]
- Abstract
Structure dependent efficacy studies in the field of selective D4 ligands led to the 2-aminomethyl substituted azaindole 2 (FAUC 213) that displayed strong D4 binding, high subtype selectivity, and complete antagonist properties in ligand-induced mitogenesis experiments. According to our schematic molecular model, the intrinsic activity of the regioisomers investigated is controlled by the ability of the heterocyclic unit to interact with both elements of the D4 binding-site crevice, the aromatic microdomain in TM6, and a serine residue in TM5.
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