Tachykinin receptor 3

TACR3
Identifiers
Aliases	TACR3, HH11, NK-3R, NK3R, NKR, TAC3RL, Tachykinin receptor 3, TAC3R, NK3
External IDs	OMIM: 162332; MGI: 892968; GeneCards: TACR3
Gene location (Human)
Chr.	Chromosome 4 (human)
End	103,719,985 bp
Gene location (Mouse)
Chr.	Chromosome 3 (mouse)
End	134,640,340 bp
RNA expression pattern
	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
	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
Databases	NCBI: entry; OMA: entry
	6870
	21338
	ENSG00000169836
	ENSMUSG00000028172
	P29371
	P47937
	NM_001059
	NM_021382
	NP_001050
	NP_067357
	Wikidata
View/Edit Human	View/Edit Mouse

Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.

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.

Selective ligands

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

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

References

1 2 3 GRCh38: Ensembl release 89: ENSG00000169836 – Ensembl, May 2017
1 2 3 GRCm38: Ensembl release 89: ENSMUSG00000028172 – Ensembl, May 2017
↑ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
↑ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
↑ Huang RR, Cheung AH, Mazina KE, Strader CD, Fong TM (Apr 1992). "cDNA sequence and heterologous expression of the human neurokinin-3 receptor". Biochemical and Biophysical Research Communications. 184 (2): 966–72. doi:10.1016/0006-291X(92)90685-E. PMID 1374246.
1 2 "Entrez Gene: TACR3 tachykinin receptor 3".
↑ Quartara L, Altamura M (Aug 2006). "Tachykinin receptors antagonists: from research to clinic". Current Drug Targets. 7 (8): 975–92. doi:10.2174/138945006778019381. PMID 16918326.

External links

"Tachykinin Receptors: NK₃". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2012-05-31. Retrieved 2008-12-09.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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[refGRCh38Ensembl-1] 1 2 3 GRCh38: Ensembl release 89: ENSG00000169836 – Ensembl, May 2017

[refGRCm38Ensembl-2] 1 2 3 GRCm38: Ensembl release 89: ENSMUSG00000028172 – Ensembl, May 2017

[3] "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.

[4] "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.

[pmid1374246-5] Huang RR, Cheung AH, Mazina KE, Strader CD, Fong TM (Apr 1992). "cDNA sequence and heterologous expression of the human neurokinin-3 receptor". Biochemical and Biophysical Research Communications. 184 (2): 966–72. doi:10.1016/0006-291X(92)90685-E. PMID 1374246.

[entrez-6] 1 2 "Entrez Gene: TACR3 tachykinin receptor 3".

[pmid16918326-7] Quartara L, Altamura M (Aug 2006). "Tachykinin receptors antagonists: from research to clinic". Current Drug Targets. 7 (8): 975–92. doi:10.2174/138945006778019381. PMID 16918326.

v t e Neurokinin receptor modulators
NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Elinzanetant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant
NK₂	Agonists: Neurokinin A Antagonists: GR-159897 Ibodutant Nepadutant Saredutant Otilonium bromide
NK₃	Agonists: Neurokinin B Senktide Antagonists: Elinzanetant Fezolinetant Osanetant Pavinetant SB-218,795 SB-222,200 Talnetant