Author/Authors :
Virendra Kumar Mishra، نويسنده , , Deqi Guo، نويسنده , , Jeffrey D. Daubert، نويسنده , , Joel A. Cassel، نويسنده , , Robert N. DeHaven، نويسنده , , Erik Mansson، نويسنده , , Diane L. DeHaven-Hudkins، نويسنده , , Alan L. Maycock، نويسنده ,
Abstract :
A novel series of kappa (κ) opioid receptor agonists were synthesized by incorporating the key structural features of known κ opioid agonists while replacing the aryl acetamide portion with substituted amino acid conjugates. Compounds 3j (Ki = 6.7 nM), 3k (Ki = 3.6 nM), 3l (Ki = 4.6 nM), 3m (Ki = 0.83 nM) and 3o (Ki = 2 nM) possessed potent affinities for the κ opioid receptor in vitro with reasonable selectivity over other opioid receptors.
