The receptor for endogenous opioids, such as beta-endorphin and endomorphin, also binds natural and synthetic opioids, including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphine, and methadone. It is activated by enkephalin peptides, particularly Met-enkephalin-Arg-Phe, which binds with high affinity. Upon agonist binding, the receptor couples with an inactive GDP-bound heterotrimeric G-protein complex, prompting GDP-GTP exchange in the G-protein alpha subunit. This leads to dissociation into GTP-bound G-alpha and beta-gamma subunits, which activate downstream signaling pathways.
The receptor primarily couples with pertussis toxin-sensitive G-proteins (G(i) and G(o)), such as GNAI1, GNAI2, GNAI3, and GNAO1 isoforms, while also interacting with pertussis toxin-insensitive G-proteins (GNAZ and GNA15). It mediates responses such as adenylate cyclase inhibition, calcium channel suppression, potassium channel activation, and regulation of MAPK, PLC, PKC, PI3K, and NF-kappa-B pathways. Temporal signaling is modulated by RGSZ proteins like RGS9, RGS17, and RGS4.
Phosphorylation by GPRK kinases and beta-arrestin association triggers receptor desensitization, terminating signal transduction. The phosphorylated receptor undergoes clathrin-mediated endocytosis, beta-arrestin-dependent internalization, and recycling. Agonist-specific receptor phosphorylation regulates ERK pathway activation via G-protein- or beta-arrestin-dependent mechanisms. The receptor exhibits rapid recycling as a class A GPCR, with trafficking and signaling modulated by heterooligomerization with other GPCRs.
| Product Name | Recombinant Human Mu-Type Opioid Receptor (OPRM1) Protein (His) |
| Accession | P35372 |
| Purity | Greater than 85% as determined by SDS-PAGE. |
| Host Species | Human |
| Gene | OPRM1 |
| Source | in vitro E.coli expression system |
| Protein Expression Range | 1-400aa |
| Tag | N-10His |
| Molecular Mass | 47.6 kDa |
| Form | Liquid or Lyophilized powder |
| Buffer | Liquid form: default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol. Lyophilized powder form: the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose, pH 8.0. |
| Storage | 1. Store at -20¡«C/-80¡«C upon receipt, aliquoting is necessary for mutiple use. 2. Avoid repeated freeze-thaw cycles. 3. Store working aliquots at 4¡«C for up to one week. 4. In general, protein in liquid form is stable for up to 6 months at -20¡«C/-80¡«C. Protein in lyophilized powder form is stable for up to 12 months at -20¡«C/-80¡«C. |
