151265-01-9Relevant academic research and scientific papers
Chirospecific and subtype selective dopamine receptor binding of heterocyclic methoxynaphthamide analogs
Bettinetti, Laura,Huebner, Harald,Gmeiner, Peter
, p. 276 - 280 (2005)
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.
Monocyclic Analogues of the μ-Opioid Agonist 3,8-Diazabicyclooctanes: Synthesis, Modeling, and Activity
Barlocco, Daniela,Villa, Stefania,Fratta, Walter,Fadda, Paola,Colombo, Diego,Toma, Lucio
, p. 11547 - 11556 (2007/10/02)
Several monocyclic derivatives structurally related to the μ-opioid agonist 3-cinnamyl-8-propionyl-3,8-diazabicyclooctane have been synthesized and tested in binding studies using the μ-selective 3H-DAMGO as ligand.Modeling studies have been performed on the same compounds in order to explain the observed lack of affinity towards μ-opioid receptors.
