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
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Neurokinin Receptor Inhibitors
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Neurokinin Receptor Related Products (279)
Related Products (279)
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Antibodies (4)
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Neurokinin Receptor Isoform Comparison
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[Glp5] Substance P (5-11)
![[Glp5] Substance P (5-11)](https://file.medchemexpress.com/product_pic/hy-p3800.gif "Click to View [Glp5] Substance P (5-11) Product Detail")
0 ImagesCat. No.: HY-P3800CAS No.: 56104-22-4[Glp5] Substance P (5-11) is an octapeptide. [Glp5] Substance P (5-11) is one of the main substance P fragments in rat central nervous system (CNS). [Glp5] Substance P (5-11) locally modulates dopamine release in rat striatum.
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UK-224671
0 ImagesCat. No.: HY-19405CAS No.: 178309-91-6UK-224671 is a potent and selective NK2 receptor antagonist. UK-224671 is affected by P-gp efflux and poor intrinsic membrane permeability, resulting in low oral bioavailability.
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CP 122721
0 ImagesCat. No.: HY-10049CAS No.: 145742-28-5CP 122721 is an orally active NK1 receptor antagonist. CP 122721 attenuates cisplatin-induced vomiting in ferrets (ID50: 0.08 mg/kg). CP 122721 inhibits kainate (KA)-induced seizure activity and CA1 neuronal cell death in rats. CP 122721 is useful in the study of depression, asthma, and irritable bowel syndrome (IBS).
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L-733060
0 ImagesCat. No.: HY-14406CAS No.: 148700-85-0L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 can be used for the study of chronic orofacial pain.
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[Lys5,MeLeu9,Nle10]-NKA(4-10)
![[Lys5,MeLeu9,Nle10]-NKA(4-10)](https://file.medchemexpress.com/product_pic/hy-p1279.gif "Click to View [Lys5,MeLeu9,Nle10]-NKA(4-10) Product Detail")
0 ImagesCat. No.: HY-P1279CAS No.: 137565-28-7[Lys5,MeLeu9,Nle10]-NKA(4-10) is a highly selective and potent NK2 receptor agonist, with an IC50 of 6.1 nM.
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Ibodutant
0 ImagesCat. No.: HY-14770CAS No.: 522664-63-7Synonyms: MEN 15596Ibodutant (MEN 15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1.
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L 363851
0 ImagesCat. No.: HY-125304CAS No.: 100807-53-2L 363851 is a Neurokinin 2 receptor agonist, and induces the contractile response of tracheal smooth muscle devoid of epithelium (IC50 of 3.2 nM) and phosphoinositide hydrolysis (IC50 of 36 μM).
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Substance P (4-11)
0 ImagesCat. No.: HY-P3891CAS No.: 53749-60-3Substance P (4-11), the C-terminus fragment of Substance P (HY-P0201), is a Substance P agonist that shows highly selective for NK1 receptors.
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Lanepitant
0 ImagesCat. No.: HY-19665CAS No.: 170566-84-4Synonyms: LY303870Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis.
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[D-Pro2,D-Phe7,D-Trp9] Substance P
![[D-Pro2,D-Phe7,D-Trp9] Substance P](https://file.medchemexpress.com/product_pic/hy-p3809.gif "Click to View [D-Pro2,D-Phe7,D-Trp9] Substance P Product Detail")
0 ImagesCat. No.: HY-P3809CAS No.: 77275-70-8[D-Pro2,D-Phe7,D-Trp9] Substance P is a Substance P (HY-P0201) analogue. [D-Pro2,D-Phe7,D-Trp9] Substance P is an inhibitor of Substance P. [D-Pro2,D-Phe7,D-Trp9] Substance P contracts guinea-pig ileum (GPI) indirectly.
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C14TKL-1
0 ImagesCat. No.: HY-P1379CAS No.: 1423381-12-7C14TKL-1 is a tachykinin-like peptide and exhibits an agonistic activity for neurokinin receptor 1 (NK-1).
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TAK-637
0 ImagesCat. No.: HY-105534CAS No.: 217185-75-6TAK-637 is an orally active neurokinin-1 receptor antagonist. TAK-637 increases bladder storage capacity. TAK-637 can be used for research of functional bowel diseases such as irritable bowel syndrome.
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TKA-731
0 ImagesCat. No.: HY-19403CAS No.: 210776-01-5
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SSR 146977
0 ImagesCat. No.: HY-116822CAS No.: 264618-44-2SSR 146977 is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 inhibits the binding of radioactive neurokinin B to NK3 receptors in Chinese hamster ovary cells, with a Ki of 0.26 nM.
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Rolapitant hydrochloride
0 ImagesCat. No.: HY-14751ACAS No.: 858102-79-1Synonyms: SCH619734 hydrochlorideRolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model.
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Neurokinin Receptor (393-407), rat
0 ImagesCat. No.: HY-P3852CAS No.: 153607-26-2Synonyms: SPR393-407Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation.
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L-703606 oxalate
0 ImagesCat. No.: HY-117216ACAS No.: 351351-06-9L-703606 oxalate is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.
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Maropitant-13C,d3
0 ImagesCat. No.: HY-10053S1Maropitant-13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting.
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CP 122721 hydrochloride
0 ImagesCP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide neurokinin NK1 antagonist, with a pIC50 of 9.8 for human NK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects.
