Amino acid conjugates as kappa opioid receptor agonists |
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Authors: | Kumar Virendra Guo Deqi Daubert Jeffrey D Cassel Joel A DeHaven Robert N Mansson Erik DeHaven-Hudkins Diane L Maycock Alan L |
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Institution: | Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. vkumar@adolor.com |
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Abstract: | A novel series of kappa (kappa) opioid receptor agonists were synthesized by incorporating the key structural features of known kappa 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 kappa opioid receptor in vitro with reasonable selectivity over other opioid receptors. |
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