Tachykinin receptor 3, also known as TACR3, is a
protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metab ...
which in humans is encoded by the ''TACR3''
gene
In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. The molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protei ...
.
Function
This gene belongs to a family of genes that function as
receptor
Receptor may refer to:
* Sensory receptor, in physiology, any neurite structure that, on receiving environmental stimuli, produces an informative nerve impulse
*Receptor (biochemistry), in biochemistry, a protein molecule that receives and respond ...
s for
tachykinin
Tachykinin peptides are one of the largest families of neuropeptides, found from amphibians to mammals. They were so named due to their ability to rapidly induce contraction of gut tissue. The tachykinin family is characterized by a common C-termi ...
s. 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
Neurokinin B (NKB) belongs in the family of tachykinin peptides. Neurokinin B is implicated in a variety of human functions and pathways such as the secretion of gonadotropin-releasing hormone.
Additionally, NKB is associated with pregnancy in fe ...
.
Selective ligands
A number of selective ligands are available for NK
3. NK
3 receptor antagonists are being investigated as treatments for various indications.
Agonists
*
Neurokinin B
Neurokinin B (NKB) belongs in the family of tachykinin peptides. Neurokinin B is implicated in a variety of human functions and pathways such as the secretion of gonadotropin-releasing hormone.
Additionally, NKB is associated with pregnancy in fe ...
– endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK
3
*
Senktide – 7-amino acid polypeptide, NK
3 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-phenylpropyl4-quinolinecarboxamide, CAS# 174635-69-9
*
SB-218,795 – more selective than SB-222,200, K
i = 13 nM, (R)-
2-Phenyl-4-quinolinylcarbonyl)aminomethyl ester benzeneacetic acid, CAS# 174635-53-1
See also
*
Tachykinin receptor
References
Further reading
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External links
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G protein-coupled receptors
{{transmembranereceptor-stub