Structure-Activity Relationship Study of CYM51010, an agonist for the µ-δ Opioid Receptor Heterodimer.

Although opioid analgesics are indispensable in treating pain, these drugs are accompanied by life-threatening side effects. While clinically relevant opioid drugs target the µ opioid receptor (MOR), a heterodimer between the MOR and the δ opioid receptor (DOR) has emerged as another target to develop safer analgesics. Although some heterodimer-preferring agonists have been reported so far, it is still difficult to activate the MOR/DOR heterodimer selectively in the presence of MOR or DOR monomers/homodimers.

Wide-Awake Local Anesthesia No Tourniquet Surgery for Zone VII Extensor Tendon Reconstruction: Stages in Active Range of Motion From Intraoperative to Final Recovery.

Purpose: We investigated chronological changes in active range of motion (ROM) of the metacarpophalangeal (MCP) joint after zone VII extensor tendon reconstruction with wide-awake local anesthesia no tourniquet (WALANT) surgery.

Methods: Reconstruction of the extensor tendons ruptured in zone VII of 82 fingers in 40 patients was performed using WALANT techniques. The mean patient age was 71.

The first structure-activity relationship study of oxytocin as a positive allosteric modulator for the µ opioid receptor.

Positive allosteric modulators (PAMs) of G protein-coupled receptors (GPCRs) have drawn attention as novel drug candidates. PAMs can enhance the activities of endogenous agonists which are not only secreted at appropriate times and in parts of the body, but also are immediately metabolized. Therefore, they are expected to show fewer side effects than exogeneous orthosteric ligands.

Wide-awake Surgery for Congenital Thumb Flexion Anomaly in a Child.

We report a rare case of absent thumb IP joint flexion in bilateral thumbs due to anomalous tendon slips of the flexor pollicis longus. Cutting the anomalous insertions failed to improve active flexion of the IP joints. Successful treatment was achieved by evaluating the musculotendinous units of the original flexor pollicis longus and the anomalous flexor pollicis longus tendon during a wide-awake surgery.