TACR2
Identifiers
Aliases	TACR2, NK2R, NKNAR, SKR, TAC2R, Tachykinin receptor 2
External IDs	OMIM: 162321 MGI: 98477 HomoloGene: 55548 GeneCards: TACR2
Gene location (Human) Chr. Chromosome 10 (human)[1] Band 10q22.1 Start 69,403,903 bp[1] End 69,416,918 bp[1]
Gene location (Mouse) Chr. Chromosome 10 (mouse)[2] Band 10|10 B4 Start 62,088,217 bp[2] End 62,101,769 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in gastric mucosa smooth muscle tissue left uterine tube transverse colon fundus myometrium urinary bladder gastrocnemius muscle rectum body of stomach Top expressed in adrenal gland right ventricle stomach colon vastus lateralis muscle duodenum upper arm triceps brachii muscle neck jejunum More reference expression data BioGPS More reference expression data
Gene ontology Molecular function tachykinin receptor activity G protein-coupled receptor activity substance K receptor activity signal transducer activity protein binding Cellular component integral component of membrane membrane integral component of plasma membrane sperm flagellum sperm head sperm midpiece plasma membrane Biological process intestine smooth muscle contraction positive regulation of acetylcholine secretion, neurotransmission excretion muscle contraction negative regulation of luteinizing hormone secretion prolactin secretion operant conditioning response to electrical stimulus regulation of uterine smooth muscle contraction positive regulation of vascular permeability positive regulation of ion transport positive regulation of smooth muscle contraction signal transduction positive regulation of uterine smooth muscle contraction tachykinin receptor signaling pathway chemical synaptic transmission positive regulation of flagellated sperm motility G protein-coupled receptor signaling pathway Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 6865 21337 Ensembl ENSG00000075073 ENSMUSG00000020081 UniProt P21452 P30549 RefSeq (mRNA) NM_001057 NM_009314 RefSeq (protein) NP_001048 NP_033340 Location (UCSC) Chr 10: 69.4 – 69.42 Mb Chr 10: 62.09 – 62.1 Mb PubMed search [3] [4]
Wikidata
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Substance-K receptor is a protein that in humans is encoded by the TACR2 gene.^[5]

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 neuropeptide substance K, also referred to as neurokinin A.^[5]

Selective Ligands

Several selective ligands for NK₂ are now available, and although most of the compounds developed so far are peptides, one small-molecule antagonist Saredutant is currently in clinical trials as an anxiolytic and antidepressant.

Agonists

• GR-64349 - potent and selective agonist, EC₅₀ 3.7nM, 7-amino acid polypeptide chain. CAS# 137593-52-3

Antagonists

• Ibodutant - failed its Phase 3 trial for IBS treatment in 2015, and abandoned by Menarini
• Saredutant - mixed but mostly negative Phase 3 trial results in 2009, and abandoned by Sanofi-Aventis
• GR-159897
• MEN-10376 - potent and selective antagonist, 7-amino acid polypeptide chain. CAS# 135306-85-3