Discovery of an Ortho-Substituted -Cyclopropylmethyl-7α-phenyl-6,14-ethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with Subsided Sedative Effect.

Research into kappa opioid receptor (KOR) agonists with attenuated central-nervous-system side effects is a critical focus for developing productive and safe analgesics. Herein, a series of -substituted -cyclopropylmethyl-7α-phenyl-6,14-ethano-tetrahydronorthebaines were designed, synthesized, and subjected to bioassays. Compound exhibited high subtype selectivity and potent agonistic activity toward KOR (KOR, = 3.

Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone.

The discovery and development of novel μ-opioid receptor (MOR) antagonists is a significant area to combat Opioid Use Disorder (OUD). In this work, a series of para-substituted N-cyclopropylmethyl-nornepenthone derivatives were designed and synthesized and pharmacologically assayed. Compound 6a was identified as a selective MOR antagonist both in vitro and in vivo.

Switchable encapsulation of polysulfides in the transition between sulfur and lithium sulfide.

Encapsulation strategies are widely used for alleviating dissolution and diffusion of polysulfides, but they experience nonrecoverable structural failure arising from the repetitive severe volume change during lithium-sulfur battery cycling. Here we report a methodology to construct an electrochemically recoverable protective layer of polysulfides using an electrolyte additive. The additive nitrogen-doped carbon dots maintain their "dissolved" status in the electrolyte at the full charge state, and some of them function as active sites for lithium sulfide growth at the full discharge state.