DGIdb - HRH3 Gene Record

HRH3 11255 Druggable Genome

Alternate Names:

11255
HISTAMINE RECEPTOR H3
HRH3
GPCR97
HH3R
604525
5184
ENSG00000101180
OTTHUMG00000032899
HRH3_HUMAN
Q9Y5N1
HISTAMINE H3 RECEPTOR
G-protein coupled receptor 97
H3R
HISTAMINE H3 RECEPTOR (HH3R) (G-PROTEIN COUPLED RECEPTOR 97). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9Y5N1]
PA29458
T64765

Gene Info:

Human Readable Name	G PROTEIN COUPLED RECEPTOR
Human Readable Name	DRUGGABLE GENOME
Interpro Name	GPCR, rhodopsin-like, 7TM
Uniprot Evidence	1: Evidence at protein level
Interpro Type	Family
Uniprot Status	Swiss-Prot
Interpro Acc	IPR000276
Interpro Short Name	7TM_GPCR_Rhodpsn
Target Class	Receptors
Target Subclass	GPCR
Target Subclass	Rhodopsin
Gene Biotype	PROTEIN_CODING

(7 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Inocente C et al., 2012, Pitolisant, an inverse agonist of the histamine H3 receptor: an alternative stimulant for narcolepsy-cataplexy in teenagers with refractory sleepiness., Clin Neuropharmacol
Khanfar MA et al., 2016, Multiple Targeting Approaches on Histamine H3 Receptor Antagonists., Front Neurosci
Schwartz JC, 2011, The histamine H3 receptor: from discovery to clinical trials with pitolisant., Br J Pharmacol
Lacour et al., 2001, Histamine and betahistine in the treatment of vertigo: elucidation of mechanisms of action., CNS Drugs
Gbahou et al., 2010, Effects of betahistine at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo., J. Pharmacol. Exp. Ther.
Barak, 2008, Betahistine: what's new on the agenda?, Expert Opin Investig Drugs
Wei Z et al., 2012, A pharmacogenetic study of risperidone on histamine H3 receptor gene (HRH3) in Chinese Han schizophrenia patients., J Psychopharmacol
Haydar SN et al., 2009, SAR and biological evaluation of SEN12333/WAY-317538: Novel alpha 7 nicotinic acetylcholine receptor agonist., Bioorg Med Chem

PITOLISANT HRH3

Interaction Score: 8.14

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H3 receptor inverse agonist

PMIDs:
22356925 27303254 21615387

Sources:
ChemblInteractions TTD
CHEMBL565540 HRH3

Interaction Score: 6.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19515567

Sources:
DTC
GSK239512 HRH3

Interaction Score: 6.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
BAVISANT HRH3

Interaction Score: 6.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
IRDABISANT HRH3

Interaction Score: 6.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H3 receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions TTD
JNJ-17216498 HRH3

Interaction Score: 6.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
BETAHISTINE HRH3

Interaction Score: 6.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name OBE101,Histalean

Novel drug target Novel Target

PMIDs:
11700150 20530654 18447604

Sources:
TdgClinicalTrial
ABT-288 HRH3

Interaction Score: 6.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
MK-0249 HRH3

Interaction Score: 6.51

Interaction Types & Directionality:

inverse agonist (inhibitory)

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor inverse agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
PF-03654746 HRH3

Interaction Score: 3.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL351231 HRH3

Interaction Score: 3.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
TTD
JNJ-39220675 HRH3

Interaction Score: 3.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PF-03654764 HRH3

Interaction Score: 3.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BODILISANT HRH3

Interaction Score: 3.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CIPRALISANT MALEATE HRH3

Interaction Score: 3.25

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SUVN-G3031 HRH3

Interaction Score: 3.25

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
TTD
GSK189254 HRH3

Interaction Score: 3.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GSK-1004723 HRH3

Interaction Score: 1.63

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Novel Target

Trial Name GSK-1004723

PMIDs:
None found

Sources:
TdgClinicalTrial
RISPERIDONE HRH3

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21652606

Sources:
PharmGKB

Ensembl: ENSG00000101180
- Version: 101_38
Alternate Names:

HRH3 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: Q9Y5N1
- Version: January-2014
Alternate Names:

HRH3 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
RussLampel: ENSG00000101180
- Version: 26-July-2011
Alternate Names:

HRH3 Display Id

HISTAMINE H3 RECEPTOR (HH3R) (G-PROTEIN COUPLED RECEPTOR 97). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9Y5N1] Description

ENSG00000101180 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
HopkinsGroom: Q9Y5N1
- Version: 11-September-2012
Alternate Names:

ENSG00000101180 Ensembl Gene Id

HRH3 Uniprot Gene Name

HRH3_HUMAN Uniprot Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Human Readable Name G PROTEIN COUPLED RECEPTOR

Interpro Name GPCR, rhodopsin-like, 7TM

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
PharmGKB: HRH3
- Version: 18-August-2020
Alternate Names:

PA29458 PharmGKB ID

Gene Info:

Publications:

Wei Z et al., 2012, A pharmacogenetic study of risperidone on histamine H3 receptor gene (HRH3) in Chinese Han schizophrenia patients., J Psychopharmacol
DTC: HRH3
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Haydar SN et al., 2009, SAR and biological evaluation of SEN12333/WAY-317538: Novel alpha 7 nicotinic acetylcholine receptor agonist., Bioorg Med Chem
HingoraniCasas: ENSG00000101180
- Version: 31-May-2017
Alternate Names:

ENSG00000101180 Gene Symbol

HRH3 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: GPCR97
- Version: chembl_23
Alternate Names:

GPCR97 GENE_SYMBOL

HRH3 GENE_SYMBOL

Histamine H3 receptor UNIPROT

Gene Info:

Publications:
dGene: HRH3
- Version: 27-Jun-2013
Alternate Names:

11255 Gene ID

GPCR97 dGene Synonym

HH3R dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: Histamine H3 receptor
- Version: 2020.06.01
Alternate Names:

H3R TTD Gene Abbreviation

T64765 TTD Target ID

Gene Info:

Publications:
Pharos: HRH3
- Version: 01-February-2022
Alternate Names:

Histamine H3 receptor Gene Name

Q9Y5N1 UniProt ID

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

Direct Interaction	yes
Mechanism of Interaction	Histamine H3 receptor inverse agonist

Mechanism of Interaction	Histamine H3 receptor antagonist
Direct Interaction	yes

Mechanism of Interaction	Histamine H3 receptor agonist
Direct Interaction	yes

HRH3	Display Id
HISTAMINE H3 RECEPTOR (HH3R) (G-PROTEIN COUPLED RECEPTOR 97). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9Y5N1]	Description
ENSG00000101180	Ensembl Gene Id

GPCR97	GENE_SYMBOL
HRH3	GENE_SYMBOL
Histamine H3 receptor	UNIPROT

Trial Name	OBE101,Histalean
Novel drug target	Novel Target

Novel drug target	Novel Target
Trial Name	GSK-1004723

HRH3 Gene Record

HRH3 11255 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: inverse agonist (inhibitory) antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histamine H3 receptor inverse agonist

PMIDs: 22356925 27303254 21615387

Sources: ChemblInteractions TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19515567

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H3 receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H3 receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histamine H3 receptor antagonist

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H3 receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name OBE101,Histalean Novel drug target Novel Target

PMIDs: 11700150 20530654 18447604

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H3 receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inverse agonist (inhibitory) agonist (activating) antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H3 receptor inverse agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H3 receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H3 receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Histamine H3 receptor agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Histamine H3 receptor antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Novel Target Trial Name GSK-1004723

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

inverse agonist (inhibitory)

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H3 receptor inverse agonist

PMIDs:
22356925 27303254 21615387

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

n/a

PMIDs:
19515567

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histamine H3 receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name OBE101,Histalean

Novel drug target Novel Target

PMIDs:
11700150 20530654 18447604

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inverse agonist (inhibitory)

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor inverse agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Histamine H3 receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Novel Target

Trial Name GSK-1004723

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
21652606

Sources:
PharmGKB

Alternate Names:

HRH3 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Alternate Names:

HRH3 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Alternate Names:

HRH3 Display Id

HISTAMINE H3 RECEPTOR (HH3R) (G-PROTEIN COUPLED RECEPTOR 97). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9Y5N1] Description

ENSG00000101180 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Alternate Names:

ENSG00000101180 Ensembl Gene Id

HRH3 Uniprot Gene Name

HRH3_HUMAN Uniprot Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Human Readable Name G PROTEIN COUPLED RECEPTOR

Interpro Name GPCR, rhodopsin-like, 7TM

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME