Opioid Family Related Drug Discovery Products
Creative Biolabs has the assays you can rely on for high throughput screening, lead optimization, characterizing and discovering targets, and uncovering the complexity of disease pathways. We can offer membrane protein in vitro assay kits that save valuable laboratory time and is ideal for high throughput screening.
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
Over 4000 years have passed since the discovery of opioids, and morphine's analgesic properties have been studied since since it was discovered in 1805. Despite the fact that long-term opioid use causes tolerance, physical dependency, and addiction, morphine is still the medicine of choice for treating acute pain. The opioid receptors, which are GPCR family A members, include the nociceptin/orphanin FQ receptor (NOP), the μ-opioid receptor (MOR), the δ-opioid receptor (DOR), and the κ-opioid receptor (KOR). These receptors share 49–58% of their main sequences, according to homology studies. High structural similarity amongst the ORs further supports the idea that they are all members of the same family.
Creative Biolabs is proud to offer our clients a series of opioid family drug discovery tools with the best quality and most competitive price:
Overview of Opioid Family
- OPRM1 (μ-opioid receptor)
The μ-opioid receptor is susceptible to internalization upon ligand binding, a complicated regulation mechanism that may result in decreased receptor activation even in the presence of ligand. μ-Receptor function is recovered as a result of receptor internalization and recycling back to the cell surface. Differential agonist-dependent signaling and desensitization were found in later experiments, pointing to biased responses involving GPCR kinases (GRKs), PKC, and β-arrestins.
Fig.1. Post-translational modification (PTM) of μ-opioid receptor. (Duarte & Devi, 2020)
- OPRD1 (δ-opioid receptor)
The δ-opioid receptor can be activated by antagonists in both G-protein-dependent and -independent signaling pathways. Desensitization of the receptor occurs as a result of agonist-induced activation of the δ-opioid receptor, which for some agonists is ascribed to receptor internalization. Endogenous opioids, peptides, and small molecules have been found to bind to opioid receptors, and internalization of the receptor has been seen. The endosomal sorting complex needed for transport (ESCRT) mechanism mainly targets opioid receptors for degradation.
Fig.2. The behavioural consequences of functional selectivity at the δ-opioid receptor. (Pradhan, 2012)
- OPRK1 (κ-opioid receptor)
The physiological responses nociception, stress, mood, eating, gastrointestinal motility, and diuresis have all been linked to κ-opioid receptors. Therapeutically, κ-opioid receptor agonists are being investigated as prospective substitutes for μ analgesics since they have a limited potential for addiction and have little effects on respiratory and gastrointestinal transit. Additionally, κ agonists have the potential to treat or prevent the hyperalgesia brought on by long-term usage of m opioid receptor treatments. The central activation of k opioid receptors causes dose-dependent dysphoria, and some agonists, such salvinorin A, cause hallucinations, therefore the clinical usefulness of κ agonists is constrained. Dynorphin, an endogenous κ-ligand, can be released during stress and has been associated to pro-addictive behaviors and drug relapse. Dynorphin behavioral correlates include dysphoria, depression, and anxiety.
References
- Duarte, M.L.; Devi, L.A. Post-translational modifications of opioid receptors. Trends in neurosciences. 2020, 43(6): 417-432.
- Pradhan, A. A.; et al. Ligand‐directed signalling within the opioid receptor family. British journal of pharmacology. 2012, 167(5): 960-969.
