HRH3

Synonyms

HRH3, Histamine Receptor H3, G-protein coupled receptor 97, H3R, Histamine H3 receptor, HH3R, G Protein-Coupled Receptor 97, Receptors, Histamine H3, GPCR97

Description

The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system. Signals through the inhibition of adenylate cyclase and displays high constitutive activity (spontaneous activity in the absence of agonist). Agonist stimulation of isoform 3 neither modified adenylate cyclase activity nor induced intracellular calcium mobilization.

KO Status

RenMab: F1 (+/-)

RenLite: F0

Drug Information

Launched drug: 1
Drugs in clinical trials: 6
Latest Research Phase: Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Pitolisant Hydrochloride

BF-2.649, BF-2649

Approved

Bioprojet

Diabetes Mellitus, Type 1, Sleepiness, Hypoglycemia, Myotonic Dystrophy, Prader-Willi Syndrome, Narcolepsy

SUVN-G3031

SUVN-G3031

Phase 2 Clinical

Suven Life Sciences

Parkinson Disease, Cognition Disorders, Narcolepsy

GSK-239512

GSK-239512, GSK-239512A

Phase 2 Clinical

Glaxosmithkline Plc

Multiple Sclerosis, Relapsing-Remitting, Schizophrenia, Multiple Sclerosis, Alzheimer Disease, Cognitive Dysfunction, Dementia

Bavisant

BEN-2001, JNJ-1074, JNJ-31001074

Phase 2 Clinical

Johnson & Johnson

Sleepiness, Attention Deficit Disorder with Hyperactivity, Alcoholism, Parkinson Disease, Narcolepsy

Irdabisant

CEP-26401

Phase 1 Clinical

Teva

Cognitive Dysfunction, Cognition Disorders

AZD-1979

AZD-1979

Phase 1 Clinical

Astrazeneca Plc

Obesity

[11C]TASP-0410457

[11C]TASP-457, [11C]TASP-0410457

Phase 1 Clinical

National Institute Of Radiological Sciences, Taisho Pharmaceutical Holdings Co Ltd

Diagnostic agents

SLS-010

SLS-010

Preclinical

Ligand Pharmaceuticals Inc

Narcolepsy

MK-7288

MK-7288

Pending

Merck Sharp & Dohme Corp

Sleep Apnea Syndromes

GT-2104

GT-2104

Pending

Mgi Pharma

Migraine Disorders, Anxiety

References

Title

Authors

Source

Cloning and functional expression of the human histamine H3 receptor

Lovenberg T.W., Roland B.L., Wilson S.J., Jiang X., Pyati J., Huvar A., Jackson M.R., Erlander M.G.,

Mol. Pharmacol. 55:1101-1107(1999)

Molecular cloning and characterization of a new human histamine receptor, HH4R

Nakamura T., Itadani H., Hidaka Y., Ohta M., Tanaka K.,

Biochem. Biophys. Res. Commun. 279:615-620(2000)

Genomic organization and characterization of splice variants of the human histamine H3 receptor

Coge F., Guenin S.-P., Audinot V., Renouard-Try A., Beauverger P., Macia C., Ouvry C., Nagel N., Rique H., Boutin J.A., Galizzi J.-P.,

Biochem. J. 355:279-288(2001)

Structure of the human histamine H3 receptor gene (HRH3) and identification of naturally occurring variations

Wiedemann P., Boenisch H., Oerters F., Bruess M.,

J. Neural Transm. 109:443-453(2002)

The DNA sequence and comparative analysis of human chromosome 20

Deloukas P., Matthews L.H., Ashurst J.L., Burton J., Gilbert J.G.R., Jones M., Stavrides G., Almeida J.P., Babbage A.K., Bagguley C.L., Bailey J., Barlow K.F., Bates K.N., Beard L.M., Beare D.M., Beasley O.P., Bird C.P., Blakey S.E., Rogers J.,

Nature 414:865-871(2001)

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)

Cloning and functional expression of the human histamine H3 receptor.

Lovenberg T.W., Roland B.L., Wilson S.J., Jiang X., Pyati J., Huvar A., Jackson M.R., Erlander M.G.,

Mol. Pharmacol. 55:1101-1107(1999)

Molecular cloning and characterization of a new human histamine receptor, HH4R.

Nakamura T., Itadani H., Hidaka Y., Ohta M., Tanaka K.,

Biochem. Biophys. Res. Commun. 279:615-620(2000)

Genomic organization and characterization of splice variants of the human histamine H3 receptor.

Coge F., Guenin S.-P., Audinot V., Renouard-Try A., Beauverger P., Macia C., Ouvry C., Nagel N., Rique H., Boutin J.A., Galizzi J.-P.,

Biochem. J. 355:279-288(2001)

Structure of the human histamine H3 receptor gene (HRH3) and identification of naturally occurring variations.

Wiedemann P., Boenisch H., Oerters F., Bruess M.,

J. Neural Transm. 109:443-453(2002)

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