Gmeiner P, Hübner H (2005)
Publication Type: Journal article
Publication year: 2005
Publisher: Wiley-VCH Verlag
Book Volume: 338
Pages Range: 276-280
Employing the D3 and D4 selective methoxynaphthalines nafadotride and FAUC 182, respectively, as lead compounds, the pyrazolo[1,5-a]pyridine-3-carboxamides of type 1a and 2a as well as their 2-substituted regioisomers 1b and 2b were synthesized when following an ex-chiral pool approach. Dopamine receptor binding studies involving the target compounds (1a,b, 2a,b) and the respective optical antipodes ent-1a,b and ent-2a,b revealed the heterocyclic carboxamide 2a as a strong and selective D4 ligand (Ki = 8.6 nM). According to a mitogenesis assay, 2a shows D4 partial agonist effects (29%, EC50 = 6.7 nM) and, thus, might be of interest for the treatment of sexual dysfunction. © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.
APA:
Gmeiner, P., & Hübner, H. (2005). Chirospecific and Subtype Selective Dopamine Receptor Binding of Heterocyclic Methoxynaphthamide Analogs. Archiv Der Pharmazie, 338, 276-280. https://doi.org/10.1002/ardp.200400997
MLA:
Gmeiner, Peter, and Harald Hübner. "Chirospecific and Subtype Selective Dopamine Receptor Binding of Heterocyclic Methoxynaphthamide Analogs." Archiv Der Pharmazie 338 (2005): 276-280.
BibTeX: Download