HCRTR1

Synonyms

HCRTR1, Hypocretin Receptor 1, Hypocretin (Orexin) Receptor 1, Orexin receptor type 1, Hypocretin receptor type 1, Ox-1-R, Orexin Receptor 1, Ox1-R, Ox1R

Description

Orexin receptor type 1 (OX1R) is a critical participant in the regulation of motivated behavior. It is a moderately selective excitatory receptor for orexin-A and, with a lower affinity, for orexin-B neuropeptide. It triggers an increase in cytoplasmic Ca2+ levels in response to orexin-A binding.

KO Status

RenMab: F1 (+/-)

RenLite: Immunization

Drug Information

Launched drugs: 2
Drugs in clinical trials: 7
Latest Research Phase: Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Suvorexant

MK-4305

Approved

Merck Sharp & Dohme Corp

Sleep Initiation and Maintenance Disorders, Sleep Apnea Syndromes, Hepatic Insufficiency, Alzheimer Disease

Lemborexant

LEM-5, E-2006, LEM-10

Approved

Eisai Co Ltd

Sleep Initiation and Maintenance Disorders, Sleep Apnea, Obstructive, Respiration Disorders, Kidney Diseases, Sleep Disorders, Circadian Rhythm, Hepatic Insufficiency, Pulmonary Disease, Chronic Obstructive

Daridorexant

ACT-541468

Phase 3 Clinical

Actelion Pharmaceuticals Ltd, Idorsia Pharmaceuticals Ltd

Sleep Initiation and Maintenance Disorders, Renal Insufficiency, Sleep Apnea, Obstructive, Pulmonary Disease, Chronic Obstructive

ACT-539313

SORA, ACT-539313

Phase 2 Clinical

Idorsia Pharmaceuticals Ltd, Actelion Pharmaceuticals Ltd

Binge-Eating Disorder, Anxiety

JNJ-61393215

JNJ-3215, Orexin-1, JNJ-61393215

Phase 2 Clinical

Johnson & Johnson

Anxiety, Depressive Disorder, Major, Depressive Disorder

YZJ-1139

YZJ-1139

Phase 2 Clinical

Yangtze River Pharmaceutical Group Co Ltd

Sleep Initiation and Maintenance Disorders

TS-142

TS-142

Phase 2 Clinical

Taisho Pharmaceutical

Sleep Initiation and Maintenance Disorders, Sleep Apnea Syndromes

AZD-4041

AZD-4041

Phase 1 Clinical

Astrazeneca Pharmaceutical Co Ltd

Smoking Cessation, Tobacco Use Disorder

INDV-2000

C4X3256, C4X_3256, INDV-2000

Phase 1 Clinical

Indivior

Opioid-Related Disorders

ACT-335827

ACT-335827

Pending

Actelion Pharmaceuticals Ltd

Nervous System Diseases

References


Title

Authors

Source

Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior

Sakurai T., Amemiya A., Ishii M., Matsuzaki I., Chemelli R.M., Tanaka H., Williams S.C., Richardson J.A., Kozlowski G.P., Wilson S., Arch J.R.S., Buckingham R.E., Haynes A.C., Carr S.A., Annan R.S., McNulty D.E., Liu W.-S., Terrett J.A., Yanagisawa M.,

Cell 92:573-585(1998)

A mutation in a case of early onset narcolepsy and a generalized absence of hypocretin peptides in human narcoleptic brains

Peyron C., Faraco J., Rogers W., Ripley B., Overeem S., Charnay Y., Nevsimalova S., Aldrich M., Reynolds D., Albin R., Li R., Hungs M., Pedrazzoli M., Padigaru M., Kucherlapati M., Fan J., Maki R., Lammers G.J., Mignot E.,

Nat. Med. 6:991-997(2000)

Polymorphisms in hypocretin/orexin pathway genes and narcolepsy

Olafsdottir B.R., Rye D.B., Scammell T.E., Matheson J.K., Stefansson K., Gulcher J.R.,

Neurology 57:1896-1899(2001)

Complete sequencing and characterization of 21,243 full-length human cDNAs

Ota T., Suzuki Y., Nishikawa T., Otsuki T., Sugiyama T., Irie R., Wakamatsu A., Hayashi K., Sato H., Nagai K., Kimura K., Makita H., Sekine M., Obayashi M., Nishi T., Shibahara T., Tanaka T., Ishii S., Sugano S.,

Nat. Genet. 36:40-45(2004)

The DNA sequence and biological annotation of human chromosome 1

Gregory S.G., Barlow K.F., McLay K.E., Kaul R., Swarbreck D., Dunham A., Scott C.E., Howe K.L., Woodfine K., Spencer C.C.A., Jones M.C., Gillson C., Searle S., Zhou Y., Kokocinski F., McDonald L., Evans R., Phillips K., Bentley D.R.,

Nature 441:315-321(2006)

The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)

The MGC Project Team,

Genome Res. 14:2121-2127(2004)

Hypocretin/orexin, sleep and narcolepsy

Hungs M., Mignot E.,

Bioessays 23:397-408(2001)

To eat or to sleep? Orexin in the regulation of feeding and wakefulness

Willie J.T., Chemelli R.M., Sinton C.M., Yanagisawa M.,

Annu. Rev. Neurosci. 24:429-458(2001)

Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors

Yin J., Babaoglu K., Brautigam C.A., Clark L., Shao Z., Scheuermann T.H., Harrell C.M., Gotter A.L., Roecker A.J., Winrow C.J., Renger J.J., Coleman P.J., Rosenbaum D.M.,

Nat. Struct. Mol. Biol. 23:293-299(2016)