Neurokinin Receptor
NK receptor; Tachykinin receptor
There are three main classes of neurokinin receptors: NK1R (the substance P preferring receptor), NK2R, and NK3R. These tachykinin receptors belong to the class I (rhodopsin-like) G-protein coupled receptor (GPCR) family. The various tachykinins have different binding affinities to the neurokinin receptors: NK1R, NK2R, and NK3R. These neurokinin receptors are in the superfamily of transmembrane G-protein coupled receptors (GPCR) and contain seven transmembrane loops. Neurokinin-1 receptor interacts with the Gαq-protein and induces activation of phospholipase C followed by production of inositol triphosphate (IP3) leading to elevation of intracellular calcium as a second messenger. Further, cyclic AMP (cAMP) is stimulated by NK1R coupled to the Gαs-protein. The neurokinin receptors are expressed on many cell types and tissues.
Neurokinin Receptor Isoform Specific Products
All Product Categories
-
Neurokinin Receptor Inhibitors
(21)
View all products
-
Neurokinin Receptor Agonists
(41)
View all products
-
Neurokinin Receptor Antagonists
(156)
View all products
-
Neurokinin Receptor Activator
(1)
View all products
-
Neurokinin Receptor Modulators
(7)
View all products
-
Neurokinin Receptor Controls
(3)
View all products
-
Neurokinin Receptor Related Products (276)
Related Products (276)
-
Antibodies (4)
-
Neurokinin Receptor Isoform Comparison
-
[Sar9,Met(O2)11]-Substance P
![[Sar9,Met(O2)11]-Substance P](https://file.medchemexpress.com/product_pic/hy-p1012.gif "Click to View [Sar9,Met(O2)11]-Substance P Product Detail")
0 Images[Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
-
Rolapitant hydrochloride hydrate
0 ImagesSynonyms: SCH619734 hydrochloride hydrateRolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model.
-
L-703606 oxalate hydrate
0 ImagesCat. No.: HY-117216BPurity: 99.4%L-703606 oxalate hydrate is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.
-
Maropitant
0 ImagesMaropitant is an orally active NK1 receptor antagonist. Maropitant prevents vomiting and inhibits ulcerative dermatitis.
-
Casopitant mesylate
0 ImagesSynonyms: GW679769BCasopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of Substance P (HY-P0201). Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
-
Substance P (7-11)
0 ImagesSubstance P (7-11) is a C-terminal fragment of Substance P which can cause an increase in the intracellular calcium concentration.
-
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10)
![[Lys5,MeLeu9,Nle10]Neurokinin A(4-10)](https://file.medchemexpress.com/product_pic/hy-p3849.gif "Click to View [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) Product Detail")
0 ImagesSynonyms: LMN-NKA[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues.
-
Vofopitant dihydrochloride
0 ImagesSynonyms: GR 205171AVofopitant dihydrochloride (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant dihydrochloride blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant dihydrochloride exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant dihydrochloride improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant dihydrochloride can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting.
-
Tradipitant
0 ImagesSynonyms: VLY-686; LY686017Tradipitant (VLY-686) is a neurokinin-1 (NK-1) antagonist.
-
GR 64349
0 ImagesGR 64349 is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 selectively activates the NK-2 receptor subtype. GR 64349 activates tonic and rhythmic bladder contractions of the micturition reflex. GR 64349 acetate does not inhibit rhythmic bladder contraction activation induced by normal saline. GR 64349 induces inward currents.
-
Hemokinin 1 (mouse)
0 ImagesHemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
-
Spantide I
0 ImagesSpantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
-
Vapreotide acetate
0 ImagesSynonyms: RC-160 acetate; BMY-41606 acetateVapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
-
[bAla8]-Neurokinin A(4-10)
![[bAla8]-Neurokinin A(4-10)](https://file.medchemexpress.com/product_pic/hy-p1031.gif "Click to View [bAla8]-Neurokinin A(4-10) Product Detail")
0 ImagesCat. No.: HY-P1031CAS No.: 122063-01-8Synonyms: MEN 10210[bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist.
-
NKP608
0 ImagesNKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK1) receptor antagonist with IC50 of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK2, NK3 receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer.
-
MEN 10207
0 ImagesMEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
![[MePhe7]-Neurokinin B](https://file.medchemexpress.com/product_pic/hy-p3862.gif "Click to View [MePhe7]-Neurokinin B Product Detail")
-
RP 67580
0 ImagesRP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation.
