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Therapeutic Innovations Against Opioid Tolerance and Addiction
Purpose of ReviewOpioids have a long history of use for relief of pain dating back thousands of years. Opium derived from the poppy plant is one of...
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Genetic mouse models in opioid research: current status and future directions
Synthetic and semi-synthetic opioids are prescribed for the management of severe pain conditions, but their long-term use is often leading to...
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G protein-biased LPAR1 agonism of prototypic antidepressants: Implication in the identification of novel therapeutic target for depression
Prototypic antidepressants, such as tricyclic/tetracyclic antidepressants (TCAs), have multiple pharmacological properties and have been considered...
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Recent Advances in Peripheral Opioid Receptor Therapeutics
Purpose of ReviewAlthough opioids are excellent analgesics, they are associated with severe short- and long-term side effects that are especially...
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Pharmacological and genetic manipulations at the µ-opioid receptor reveal arrestin-3 engagement limits analgesic tolerance and does not exacerbate respiratory depression in mice
Opioid drugs are widely used analgesics that activate the G protein-coupled µ-opioid receptor, whose endogenous neuropeptide agonists, endorphins and...
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The Pharmacology of Buprenorphine Microinduction for Opioid Use Disorder
Although expanding the availability of buprenorphine—a first-line pharmacotherapy for opioid-use disorder (OUD)—has increased the capacity of...
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G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery
G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and an important class of drug targets, play a role in maintaining...
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A Large-Scale Observational Study on the Temporal Trends and Risk Factors of Opioid Overdose: Real-World Evidence for Better Opioids
BackgroundThe USA is in the midst of an opioid overdose epidemic. To address the epidemic, we conducted a large-scale population study on opioid...
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Essential role of P-glycoprotein in the mechanism of action of oliceridine
Mu opioid receptor (MOR) agonists comprise the most effective analgesics, but their therapeutic utility is limited by adverse effects. One approach...
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Current and Future Therapeutic Options in Pain Management: Multi-mechanistic Opioids Involving Both MOR and NOP Receptor Activation
Opioids are widely used in chronic pain management, despite major concerns about their risk of adverse events, particularly abuse, misuse, and...
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Nociceptin Receptor-Related Agonists as Safe and Non-addictive Analgesics
As clinical use of currently available opioid analgesics is often impeded by dose-limiting adverse effects, such as abuse liability and respiratory...
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Orthosteric ligand selectivity and allosteric probe dependence at Hydroxycarboxylic acid receptor HCAR2
Hydroxycarboxylic acid receptor 2 (HCAR2), a member of Class A G-protein-coupled receptor (GPCR) family, plays a pivotal role in anti-lipolytic and...
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Transcriptomic profiling of reward and sensory brain areas in perinatal fentanyl exposed juvenile mice
Use of the synthetic opioid fentanyl increased ~300% in the last decade, including among women of reproductive ages. Adverse neonatal outcomes and...
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Heroin and its metabolites: relevance to heroin use disorder
Heroin is an opioid agonist commonly abused for its rewarding effects. Since its synthesis at the end of the nineteenth century, its popularity as a...
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Acupuncture/Electroacupuncture as an Alternative in Current Opioid Crisis
Opioid drugs are the first line of defense in severe pain but the adverse effects associated with opioids are considered as a serious issue...
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Effectiveness of interventions for prevention of common infections in people who use opioids: a protocol for a systematic review of systematic reviews
BackgroundThe North American opioid crisis is driven by opioid-related mortality and morbidity, including opioid use-associated infections (OUAIs),...
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G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders
Neuropsychiatric disorders are multifactorial disorders with diverse aetiological factors. Identifying treatment targets is challenging because the...
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A Brief Review on the Novel Therapies for Painful Diabetic Neuropathy
Purpose of ReviewAlmost half of people diagnosed with diabetes mellitus will develop painful diabetic neuropathy (PDN), a condition greatly impacting...
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Untangling the complexity of opioid receptor function
Mu opioid receptor agonists are among the most powerful analgesic medications but also among the most addictive. The current opioid crisis has...
