Substance-K receptor is a
protein that in humans is encoded by the ''TACR2''
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 neuropeptide substance K, also referred to as neurokinin A.
Selective Ligands
Several selective ligands for NK
2 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
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...
.
Agonists
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GR-64349 - potent and selective agonist, EC
50 3.7nM, 7-amino acid polypeptide chain. CAS# 137593-52-3
Antagonists
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Ibodutant
Ibodutant was a candidate drug for irritable bowel syndrome diarrhea, developed by The Menarini Group. , it underwent a multicentre double blind efficacy clinical study. Ibodutant selectively blocks the tachykinin receptor NK2, with blockade pra ...
- failed its Phase 3 trial for IBS treatment in 2015, and abandoned by Menarini
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Saredutant
Saredutant (SR-48,968) is a drug that acts as a Tachykinin receptor 2, NK2 receptor receptor antagonist, antagonist. It was under development by Sanofi-Aventis as a novel antidepressant and anxiolytic and made it to Phase III clinical trials, pha ...
- mixed but mostly negative Phase 3 trial results in 2009, and abandoned by Sanofi-Aventis
*
GR-159897
GR-159897 is a potent and selective NK2 receptor antagonist drug. It has anxiolytic effects in animal models, and also inhibits bronchoconstriction of the airways, which may potentially make it useful in the treatment of asthma.
See also
* Ib ...
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MEN-10376
Multiple endocrine neoplasia type 1 (MEN-1) is one of a group of disorders, the multiple endocrine neoplasias, that affect the endocrine system through development of neoplastic lesions in pituitary, parathyroid gland and pancreas.
It was firs ...
- potent and selective antagonist, 7-amino acid polypeptide chain. CAS# 135306-85-3
See also
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Tachykinin receptor
References
Further reading
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External links
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{{Neurokinin receptor modulators
G protein-coupled receptors