Orexin receptor type 1 (Ox1R or OX
1), also known as hypocretin receptor type 1 (HcrtR1), is a
protein that in humans is encoded by the HCRTR1
gene.
Function
The orexin 1 receptor (OX
1), is a
G-protein coupled receptor that is heavily expressed in projections from the
lateral hypothalamus and is involved in the regulation of feeding behaviour. OX
1 selectively binds the
orexin-A neuropeptide. It shares 64% identity with
OX2.
Ligands
Agonists
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Orexin-A
Antagonists
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RTIOX-276
RTIOX-276 is an orexin antagonist. RTIOX-276 binds selectively to the orexin 1 receptor (KE = 8.5nM) and lacks significant affinity for the orexin 2 receptor (KE = > 10,000nM). RTIOX-276 may have therapeutic utility for the treatment of cocain ...
- Selective OX
1 antagonist
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ACT-335827
ACT-335827 is an orally available, selective orexin 1 receptor antagonist with anxiolytic effects in animals. Unlike other orexin receptor antagonists, ACT-335827 lacks sedative effects and was found to have no impact on sleep architecture
...
- Selective OX
1 antagonist
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Almorexant - Dual OX
1 and
OX2 antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
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Lemborexant - Dual OX
1 and
OX2 antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
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Nemorexant
Daridorexant, sold under the brand name Quviviq, is an orexin antagonist medication which is used for the treatment of insomnia. Daridorexant is taken by mouth.
Side effects of daridorexant include headache, somnolence, and fatigue. The medic ...
- Dual OX
1 and OX
2 antagonist
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SB-334,867
SB-334867 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors. It has been shown to produce sedative and anorec ...
- Selective OX
1 antagonist
*
SB-408,124
SB-408124 is a drug which is a non-peptide antagonist selective for the orexin receptor subtype OX1, with around 70x selectivity for OX1 over OX2 receptors, and improved oral bioavailability compared to the older OX1 antagonist SB-334867
SB-3 ...
- Selective OX
1 antagonist
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SB-649,868
SB-649868 is a dual orexin receptor antagonist that was being developed by GlaxoSmithKline as a treatment for insomnia.
A phase I clinical trial evaluated doses up to 80 mg, resulting in significant improvement in sleep latency without a ...
- Dual OX
1 and
OX2 antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
*
Suvorexant
Suvorexant, sold under the brand name Belsomra, is an orexin antagonist medication which is used in the treatment of insomnia. It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or mainte ...
- Dual OX
1 and
OX2 antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
See also
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Orexin receptor
References
External links
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Further reading
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G protein-coupled receptors
{{transmembranereceptor-stub