501663-08-7Relevant academic research and scientific papers
Fused azaindole derivatives: Molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725
L?ber, Stefan,Hübner, Harald,Gmeiner, Peter
, p. 2377 - 2380 (2002)
Computational studies based on the similarity of molecular electrostatic potential maps initiated the synthesis of the tricyclic target compounds 1 (FAUC 725) and 2. Receptor binding studies at the dopamine receptor subtypes D1, D2long, D2short, D3 and D4 showed that the azaindole 1 revealed D3 affinity (Ki=0.54 nM) comparable to the lead pramipexole and enhanced selectivity over D2 and D4. Mitogenesis experiments indicated substantial intrinsic activity for the D3 selective dipropylamine 1. Based on the structure of (S)-3-PPP, bioisosteric replacement and conformational restriction leading to the test compound 2 was not fruitful.
