HRH3
Synonyms
GPCR97, HRH3, Histamine Receptor H3, G-protein coupled receptor 97, H3R, Histamine H3 receptor, HH3R, G Protein-Coupled Receptor 97, Receptors, Histamine H3
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: Immunization
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
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
SUVN-G3031
SUVN-G3031
Phase 2 Clinical
Suven Life Sciences
Parkinson Disease, Cognition Disorders, Narcolepsy
AZD-1979
AZD-1979
Phase 1 Clinical
Astrazeneca Plc
Obesity
Irdabisant
CEP-26401
Phase 1 Clinical
Teva
Cognitive Dysfunction, Cognition Disorders
[11C]TASP-0410457
[11C]TASP-457, [11C]TASP-0410457
Phase 1 Clinical
National Institute Of Radiological Sciences, Taisho Pharmaceutical Holdings Co Ltd
Diagnostic agents
Votucalis(Akari Therapeutics)
Preclinical
Akari Therapeutics
Pruritus, Neuralgia, Dermatitis, Atopic
SLS-010
SLS-010
Preclinical
Ligand Pharmaceuticals Inc
Narcolepsy
AZD-5213
AZD-5213
Pending
Astrazeneca Plc
Diabetic Neuropathies, Tourette Syndrome, Alzheimer Disease, Cognitive Dysfunction
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)