Mechanisms of inhibitory action of TRK-130 (Naltalimide), a μ-opioid receptor partial agonist, on the micturition reflex

Abstract

These results suggest that TRK-130 enhances the bladder storage function by modulating the afferent limb of the micturition reflex through µ-opioid receptors in the spinal cord. TRK-130 could be a more effective and safer therapeutic agent with a different fashion from antimuscarinics and conventional opioids for overactive bladder.

Predictors of Postoperative Urinary Retention in Outpatient Minimally Invasive Hysterectomy

“…Although the mechanism of action remains unclear, patients who receive larger doses of narcotics may have more postoperative pain, which my impact their ability to void [19]. There may also be a direct effect of opioids on bladder function, but further studies are required before this association is made [20].…”

A2A Adenosine Receptor Partial Agonism Related to Structural Rearrangements in an Activation Microswitch

“…Development of partial agonist drugs is therefore of interest whenever overstimulation of a GPCR needs to be prevented by tuning the receptor response (Hauser et al, 2017). GPCR partial agonists currently used in the clinic or investigated for their therapeutic potential include drugs targeting opioid receptors (Browne et al, 2020;Chan et al, 2017;Fujimura et al, 2017;Khroyan et al, 2017;Schmid et al, 2017), adrenergic receptors (Calverley et al, 2007), dopamine receptors (Frank et al, 2017;Tarland et al, 2018), and serotonin receptors (Chen et al, 2018;Huang et al, 2017;Yoshinaga et al, 2018;Zheng et al, 2017). Partial agonists are also under consideration as potential treatments for obesity (Wargent et al, 2013) and heart failure (Greene et al, 2016).…”