AAV ACTOne Gi-GPCR Assay Kit-OPRM1

The AAV ACTOne Gi-GPCR Assay Kit-OPRM1 is designed specifically for screening drugs/compounds that target the Opioid receptor, Mu (OPRM1) by combination AAV and ACTOne technologies.

The Opioid Receptor Mu 1 (OPRM1), also known as the Mu-Opioid Receptor (MOR), is a G protein-coupled receptor (GPCR) that is a central component of the opioid system, which regulates pain, reward, and addictive behaviors. OPRM1 is the primary target for endogenous opioid peptides such as endorphins and enkephalins, as well as exogenous opioids like morphine, heroin, and fentanyl. When activated by its ligands, OPRM1 primarily couples with the Gi/Go class of G proteins, leading to the inhibition of adenylate cyclase, a decrease in cyclic AMP (cAMP) levels, and modulation of ion channels, particularly potassium and calcium channels. This results in hyperpolarization of neurons and a reduction in neuronal excitability, which underlies the receptor’s analgesic effects. OPRM1 is widely expressed in the central nervous system, particularly in areas associated with pain perception, reward, and stress, such as the thalamus, spinal cord, brainstem, and limbic system. Activation of OPRM1 produces strong analgesia, euphoria, and feelings of well-being, which is why it is a key target for pain relief. However, these same effects also contribute to the high potential for abuse and addiction associated with opioid drugs. In addition to its role in pain management and reward, OPRM1 is involved in regulating mood, stress, and gastrointestinal function. Dysregulation of OPRM1 signaling is implicated in various conditions, including opioid use disorder, chronic pain, and mood disorders. Given its critical role in both therapeutic and addictive effects of opioids, OPRM1 is a major focus in the development of safer pain medications, treatments for opioid addiction, and interventions for opioid overdose, such as the opioid antagonist naloxone, which blocks the receptor to reverse the effects of opioid overdose.

This kit uses AAV vectors with a CMV promoter to co-express the OPRM1 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential OPRM1-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of OPRM1 drugs, such as agonists and antagonists, in a live-cell environment.

• SKU: KI001-OPRM1
• Targeting GPCR: Opioid receptor, Mu (OPRM1)
• GPCR Type: Gi-GPCR
• Kit components: AAV-CNG/AAV-OPRM1 and ACTOne MP Dye
• Storage:  -80°C for long term (> 1 year);  -20°C for short term(1-2 months);  4 °C for 1-2 weeks.
• Shipping: Dry ice.