9.A.14.13.18 Mu-type opioid receptor of 400 aas and 7 TMSs, OprM1. Receptor for endogenous opioids such as
beta-endorphin and endomorphin and for natural and synthetic
opioids including morphine, heroin, DAMGO, fentanyl, etorphine,
buprenorphin and methadone. Agonist binding to the receptor induces
coupling to an inactive GDP-bound heterotrimeric G-protein complex and
subsequent exchange of GDP for GTP in the G-protein alpha subunit
leading to dissociation of the G-protein complex with the free GTP-bound
G-protein alpha and the G-protein beta-gamma dimer activating
downstream cellular effectors. The agonist- and cell type-specific
activity is predominantly coupled to pertussis toxin-sensitive G(i) and
G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1
and Alpha-2, and to a lesser extend to pertussis toxin-insensitive G
alpha proteins GNAZ and GNA15. They mediate an array of downstream
cellular responses, including inhibition of adenylate cyclase activity as well as both N-type and L-type calcium channels, and activation of inward
rectifying potassium channels (Knapman and Connor 2015). Activation of the astrocytic μ-opioid receptor elicits fast glutamate release through TREK-1-containing K2P channel in hippocampal astrocytes (Woo et al. 2018).
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Accession Number: | P35372 |
Protein Name: | Mu-type opioid receptor |
Length: | 400 |
Molecular Weight: | 44779.00 |
Species: | Homo sapiens (Human) [9606] |
Number of TMSs: | 7 |
Location1 / Topology2 / Orientation3: |
Cytoplasm1 |
Substrate |
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1: MDSSAAPTNA SNCTDALAYS SCSPAPSPGS WVNLSHLDGN LSDPCGPNRT DLGGRDSLCP
61: PTGSPSMITA ITIMALYSIV CVVGLFGNFL VMYVIVRYTK MKTATNIYIF NLALADALAT
121: STLPFQSVNY LMGTWPFGTI LCKIVISIDY YNMFTSIFTL CTMSVDRYIA VCHPVKALDF
181: RTPRNAKIIN VCNWILSSAI GLPVMFMATT KYRQGSIDCT LTFSHPTWYW ENLLKICVFI
241: FAFIMPVLII TVCYGLMILR LKSVRMLSGS KEKDRNLRRI TRMVLVVVAV FIVCWTPIHI
301: YVIIKALVTI PETTFQTVSW HFCIALGYTN SCLNPVLYAF LDENFKRCFR EFCIPTSSNI
361: EQQNSTRIRQ NTRDHPSTAN TVDRTNHQLE NLEAETAPLP