Target intelligence / Profile preview

Tachykinin receptor 2 (NK2R) (NK2R)

Target
NK2R
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The Tachykinin receptor 2 (NK2R), encoded by the TACR2 gene, is a G protein-coupled receptor (GPCR) that selectively binds the tachykinin neuropeptide neurokinin A (NKA) (UniProt: P21452). It is highly expressed in the smooth muscle layers of the gastrointestinal (GI) tract and the respiratory system, where it mediates excitatory signals leading to muscle contraction and increased motility (IUPHAR/BPS Guide to Pharmacology). In the GI system, NK2R activation is a key driver of peristalsis and visceral sensation; consequently, its overactivity is linked to the pathophysiology of irritable bowel syndrome (IBS), particularly the diarrhea-predominant subtype (IBS-D) (PMID: 22982101). Beyond the gut, NK2R plays a role in bronchoconstriction, making it a target of interest for asthma and chronic obstructive pulmonary disease (COPD) (PMID: 15504044). Therapeutic strategies focus on selective NK2R antagonists, such as ibodutant and saredutant, which are designed to alleviate symptoms like abdominal pain and urgency by normalizing intestinal transit (PubChem CID: 11511134). While these agents have shown potential in clinical trials for GI disorders, their development has been marked by variable efficacy, leading to ongoing research into more specific patient stratification and biomarker use.

Other names
Neurokinin 2 receptorNeurokinin A receptorTACR2NK-2 receptorTachykinin receptor 2
02

Mechanism of action

Tachykinin NK2 receptor antagonism

03

Biological functions

Signal transductionSmooth muscle contractionGastrointestinal motility regulationBronchoconstriction
04

Disease associations

Irritable bowel syndromeAsthmaGastrointestinal motility disorderChronic obstructive pulmonary disease
05

Safety considerations

Gastrointestinal motility changesPotential respiratory effectsLimited clinical efficacy in broad populations
06

Interacting drugs

Ibodutant

3 more in the full profile.

07

Biomarkers

Neurokinin A levelsTACR2 gene expression

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