Mu Opioid Receptor Modulators

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent relates to a novel class of compounds that act as modulators of the mu opioid receptor (MOR). These compounds are designed to selectively activate the G protein-coupled signaling pathway of MOR, while minimizing activation of the beta-arrestin pathway, which is associated with many adverse opioid side effects. The core invention provides compositions and methods for pain relief, treatment of opioid overdose and addiction, and modulation of opioid receptor activity with reduced risk of typical opioid-induced side effects such as respiratory depression, constipation, and addiction. Notably, the compounds (such as PZM21) demonstrate strong analgesic effects with potentially lower liability for addiction and side effects than traditional opioids like morphine.

Use CasesContent extracted from patent full text and abstract with AI.

• Prescription analgesics for treating moderate to severe acute or chronic pain (e.g., post-surgical pain, cancer pain, neuropathic pain).
• Medications for treating opioid overdose with a lower risk of respiratory depression compared to standard opioids.
• Therapy for opioid addiction, potentially as a replacement or adjunct to current treatments such as methadone or buprenorphine.
• Treatment for psychiatric disorders (e.g., depression, anxiety) where modulation of the opioid system is beneficial.
• Use as research tools for studying pain pathways and opioid receptor function, especially with signaling selectivity.
• Development of safer pain management drugs in clinical settings to reduce opioid-related mortality and morbidity.

BenefitsContent extracted from patent full text and abstract with AI.

• Reduced risk of life-threatening respiratory depression, a side effect common in traditional opioid drugs.
• Lower propensity to cause constipation, a major limiting factor in opioid therapy.
• Minimized addiction and dependence potential due to attenuated reward pathway activation in the brain.
• Selective pain relief for affective pain (emotional/central pain) without strongly affecting spinal reflexes, reducing unwanted side effects.
• Greater safety margin and better tolerability, allowing for improved dosing and patient outcomes.
• Ability to treat pain effectively while mitigating reinforcement-related behaviors (e.g., drug-seeking), important for safer chronic use.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.