Search
hypocretin receptor; orexin receptor (Hcrtr)
Function:
- receptor for peptide neurotransmitters hypocretin or orexin
- two receptor genes have been identified (Hcrtr1 & Hcrtr2)
- G-protein coupled receptors
- role in sleep-wake cycle via orexin [3]
Pharmacology:
- orexin receptor antagonist suvorexant FDA-approved to treat insomnia
Related
hypocretin; orexin (HCRT, OX, PPORX, PPOX)
Specific
orexin receptor type 1; Ox1r; hypocretin receptor type 1 (HCRTR1)
orexin receptor type 2; Ox2r; hypocretin receptor type 2 (HCRTR2)
General
G-protein coupled receptor; serpentine receptor
Properties
COMPARTMENT: cellular membrane
MOTIF: exoplasmic domain {N-TERMINAL}
ligand-binding site
transmembrane domain {TM1}
transmembrane domain {TM2}
transmembrane domain {TM3}
transmembrane domain {TM4}
transmembrane domain {TM5}
transmembrane domain {TM6}
transmembrane domain {TM7}
transmembrane domain (7)
guanine nucleotide exchange domain
NAME: guanine nucleotide exchange domain
binding site
SITE: C-TERMINAL-CYS
EFFECTOR-BOUND: palmitate
BOUND-VIA: carboxylate
cytoplasmic domain {C-TERMINAL}
References
- Peyron et al, Nature Med 6:991,2000
- Sakurai et al, Cell 92:573, 1998
- FDA News Release. August 13, 2014
FDA approves new type of sleep drug, Belsomra
http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm409950.htm