Synthesis and evaluation of novel peripherally restricted κ-opioid receptor agonists
✍ Scribed by Virendra Kumar; Deqi Guo; Joel A. Cassel; Jeffrey D. Daubert; Robert N. DeHaven; Diane L. DeHaven-Hudkins; Erin K. Gauntner; Susan L. Gottshall; Susan L. Greiner; Michael Koblish; Patrick J. Little; Erik Mansson; Alan L. Maycock
- Book ID
- 108073532
- Publisher
- Elsevier Science
- Year
- 2005
- Tongue
- English
- Weight
- 128 KB
- Volume
- 15
- Category
- Article
- ISSN
- 0960-894X
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The tryptophan isomers of the cyclic tetrapeptide CJ-15,208, reported to be a kappa opioid receptor (KOR) antagonist [Saito, T.; Hirai, H.; Kim, Y. J.; Kojima, Y.; Matsunaga, Y.; Nishida, H.; Sakakibara, T.; Suga, O.; Sujaku, T.; Kojima, N. J. Antibiot. (Tokyo)2002, 55, 847-854.], were synthesized t
## Abstract For Abstract see ChemInform Abstract in Full Text.
The four stereoisomers of the two peripherally selective K-opioid agonists EMD 60 400 and EMD 61 753 were synthesized, tested for stereoisomeric purity, and examined for affinity to the K opioid receptor. The relationships between the configuration of these molecules and their biological activity ar