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The search for selective kappa opioid receptor (κOR) agonists with an improved safety profile is an area of interest in opioid research. SLL-1206 is a κOR agonist with single-digit nanomolar activities. SLL-1206 exhibits substantially improved physicochemical and pharmacokinetic properties, and reduces central nervous system effects.

The authors are grateful to Medicilon Preclinical Research LLC. for pharmacokinetic studies on SLL-1206.

Reference:

Qian He, et al. Discovery of an M-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaine as a Selective, Potent, and Orally Active κ-Opioid Receptor Agonist with an Improved Central Nervous System Safety Profile. J Med Chem. 2021 Aug 26;64(16):12414-12433. doi: 10.1021/acs.jmedchem.1c01082.