Tachykinin receptor 3

Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.^[5][6]

TACR3
Identifiers
Aliases	TACR3, HH11, NK-3R, NK3R, NKR, TAC3RL, Tachykinin receptor 3, TAC3R, NK3
External IDs	OMIM: 162332; MGI: 892968; HomoloGene: 824; GeneCards: TACR3; OMA:TACR3 - orthologs
Gene location (Human) Chr. Chromosome 4 (human)[1] Band 4q24 Start 103,586,031 bp[1] End 103,719,985 bp[1]
Gene location (Mouse) Chr. Chromosome 3 (mouse)[2] Band 3|3 G3 Start 134,534,768 bp[2] End 134,640,340 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in Hypothalamus C1 segment prefrontal cortex Amygdala urinary bladder substantia nigra ventricular zone corpus callosum Brodmann area 9 primary visual cortex Top expressed in iris ventral tegmental area substantia nigra vestibular sensory epithelium stria vascularis lumbar subsegment of spinal cord lateral hypothalamus Gonadal ridge cornea adrenal cortex More reference expression data BioGPS More reference expression data
Gene ontology Molecular function tachykinin receptor activity G protein-coupled receptor activity signal transducer activity protein binding Cellular component cytoplasm integral component of membrane membrane plasma membrane integral component of plasma membrane dendrite membrane neuronal cell body membrane nucleus sperm midpiece Biological process response to estradiol ageing hyperosmotic salinity response regulation of feeding behavior regulation of dopamine metabolic process positive regulation of heart rate response to morphine positive regulation of blood pressure signal transduction positive regulation of uterine smooth muscle contraction response to cocaine tachykinin receptor signaling pathway positive regulation of flagellated sperm motility G protein-coupled receptor signaling pathway Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 6870 21338 Ensembl ENSG00000169836 ENSMUSG00000028172 UniProt P29371 P47937 RefSeq (mRNA) NM_001059 NM_021382 RefSeq (protein) NP_001050 NP_067357 Location (UCSC) Chr 4: 103.59 – 103.72 Mb Chr 3: 134.53 – 134.64 Mb PubMed search [3] [4]
Wikidata
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Function

This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neurokinin 3, also referred to as neurokinin B.^[6]

Selective ligands

A number of selective ligands are available for NK₃. NK₃ receptor antagonists are being investigated as treatments for various indications.^[7]

Agonists

• Neurokinin B – endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK₃
• Senktide – 7-amino acid polypeptide, NK₃ selective, CAS# 106128-89-6

Antagonists

• Elinzanetant (BAY-3427080 GSK-1144814, NT-814)
• Fezolinetant (ESN-364)
• Osanetant (SR-142,801)
• Pavinetant (MLE-4901, AZD-4901, AZD-2624)
• Talnetant (SB-223,412)
• SB-222,200 – potent and selective antagonist, K_i = 4.4 nM, 3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide, CAS# 174635-69-9
• SB-218,795 – more selective than SB-222,200, K_i = 13 nM, (R)-[(2-Phenyl-4-quinolinylcarbonyl)amino]-methyl ester benzeneacetic acid, CAS# 174635-53-1

See also

• Tachykinin receptor