Histamine H3 receptor

Function

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.

Classification

Family (Pfam)

PF00001 7tm_1

InterPro

GPCR_Rhodpsn, GPCR_Rhodpsn_7TM, Histamine_H3_rcpt

Functional cluster

Nucleic Acid Metabolism & Repair Enzymes

Experimental structures · PDB · 8

• 7F61 X-ray 2.60A
• 8YN5 EM 2.70A
• 8YN6 EM 2.77A
• 8YN7 EM 2.77A
• 8YN8 EM 2.77A
• 8YUU EM 2.70A
• 8YUV EM 3.00A
• 9JEQ EM 3.05A

A predicted model is available from AlphaFold.

Gene Ontology · 11

• GO:0030425 dendrite
• GO:0005886 plasma membrane
• GO:0098793 presynapse
• GO:0045202 synapse
• GO:0004969 histamine receptor activity
• GO:0030594 neurotransmitter receptor activity
• GO:0007189 adenylate cyclase-activating G protein-coupled receptor signaling pathway
• GO:0007197 adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway
• GO:0007268 chemical synaptic transmission
• GO:0007187 G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
• GO:0007269 neurotransmitter secretion

Drugs targeting this protein · 15

• JNJ-39220675 antagonist
• GSK-1004723 antagonist
• IRDABISANT antagonist
• BAVISANT antagonist
• CIPRALISANT MALEATE agonist
• PF-03654746 antagonist
• PF-03654764 antagonist
• BETAHISTINE antagonist
• GSK239512 antagonist
• ABT-288 antagonist
• PITOLISANT HYDROCHLORIDE inverse agonist
• SUVN-G3031 inverse agonist
• PITOLISANT inverse agonist
• MK-0249 inverse agonist
• GSK189254 antagonist

Related proteins · sequence + function similarity

• Histamine H3 receptor 1.00
• Histamine H3 receptor 1.00
• Histamine H3 receptor 1.00
• Prostaglandin E2 receptor EP1 subtype 0.81
• Prostaglandin E2 receptor EP1 subtype 0.80
• Sphingosine 1-phosphate receptor 5 0.78
• Vasopressin V2 receptor 0.77
• Sphingosine 1-phosphate receptor 5 0.77
• Sphingosine 1-phosphate receptor 5 0.77
• Gastrin/cholecystokinin type B receptor 0.77
• Gastrin/cholecystokinin type B receptor 0.76
• Muscarinic acetylcholine receptor M1 0.76

Co-cited proteins · studied together in the literature

• Histamine H3 receptor 1 shared papers
• Histamine H4 receptor 1 shared papers

Literature · 6 cited papers

• The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
• Structure of the human histamine H3 receptor gene (HRH3) and identification of naturally occurring variations. J. Neural Transm. · 2002
• The DNA sequence and comparative analysis of human chromosome 20. Nature · 2001
• Genomic organization and characterization of splice variants of the human histamine H3 receptor. Biochem. J. · 2001
• Molecular cloning and characterization of a new human histamine receptor, HH4R. Biochem. Biophys. Res. Commun. · 2000
• Cloning and functional expression of the human histamine H3 receptor. Mol. Pharmacol. · 1999