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ID: ALA1147793
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype.
Authors: Löber S, Hübner H, Gmeiner P.
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 GTPgammaS assays, ligand efficacy was evaluated indicating partial agonist properties. Interestingly, the tetrahydropyrimidine 4 (FAUC 2020) displayed significant intrinsic selectivity for D2(long) over D2(short).
CiteXplore: 16563764