| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374396 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
Abstract
Aminomethyl-substituted biaryls bearing a pyrazole or triazole moiety were synthesized and investigated for dopamine and serotonin receptor binding. The N-arylpyrazoles 3b,f,g and 4 revealed Ki values in the subnanomolar range (0.28–0.70 nM) for the dopamine D4 receptor subtype. Employing both mitogenesis and GTPγS assays, ligand efficacy was evaluated indicating partial agonist properties. Interestingly, the tetrahydropyrimidine 4 (FAUC 2020) displayed significant intrinsic selectivity for D2long over D2short.
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Related Topics
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Organic Chemistry
Authors
Stefan Löber, Harald Hübner, Peter Gmeiner,