SLL-1206是一種κ阿片受體激動劑，具有顯著改善的理化和藥代動力學特性。作者感謝hjc黄金城對SLL-1206進行的藥代動力學研究

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 s 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.