Chirospecific and subtype selective dopamine receptor binding of heterocyclic methoxynaphthamide analogs
Chirospecific and subtype selective dopamine receptor binding of heterocyclic methoxynaphthamide analogs
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DOI：
10.1002/ardp.200400997
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发表时间：
2005-06-01
影响因子：
5.1
通讯作者：
Gmeiner, P
中科院分区：
文献类型：
--
作者：
Bettinetti, L;Hübner, H;Gmeiner, P
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 (K-i = 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.
