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 Agonists
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Neurokinin Receptor Antagonists
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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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Substance P (alligator)
0 ImagesCat. No.: HY-P3885CAS No.: 113516-47-5Substance P (alligator), a Substance P (HY-P0201) extracted from alligator, is a neuropeptide. The primary structure of Substance P (alligator) is: Arg-Pro-Arg-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2.
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Dapitant
0 ImagesCat. No.: HY-17012CAS No.: 153438-49-4Synonyms: RPR 100893Dapitant (RPR 100893) is a non-peptide Substance P antagonist with high affinity for the human NK1 receptor. It belongs to the 7,7,4-trimethylperhydroisoindole class of compounds. Dapitant inhibits the binding of Substance P to NK1 receptors, thereby blocking its neurokinin-mediated effects. This novel antagonist represents a potential therapeutic option for conditions involving Substance P, such as neurogenic inflammation and pain modulation.
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FK888
0 ImagesCat. No.: HY-105215CAS No.: 138449-07-7FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration.
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[Glp5,Sar9] Substance P (5-11)
![[Glp5,Sar9] Substance P (5-11)](https://file.medchemexpress.com/product_pic/hy-p3905.gif "Click to View [Glp5,Sar9] Substance P (5-11) Product Detail")
0 ImagesCat. No.: HY-P3905CAS No.: 77128-78-0[Glp5,Sar9] Substance P (5-11) is a neuropeptide Substance P (HY-P0201) analogue specifically designed to interact with the Neurokinin-1 (NK1) receptor. [Glp5,Sar9] Substance P (5-11) modulates pain perception and inflammatory responses.
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Casopitant
0 ImagesCat. No.: HY-14405CAS No.: 414910-27-3Synonyms: GW679769Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
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SLV-317 free base
0 ImagesCat. No.: HY-19429CAS No.: 393101-98-9SLV-317 (free base) is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 (free base) can effective antagonist of substance P-induced effects.
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MEDI-1912
0 ImagesCat. No.: HY-P991323MEDI-1912 is a human monoclonal antibody (mAb) targeting NGF/bNGF. MEDI-1912 inhibits signaling through TrkA and p75 receptors. MEDI-1912 can be used in chronic pain research.
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[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10)
![[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10)](https://file.medchemexpress.com/product_pic/hy-p11075.gif "Click to View [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) Product Detail")
0 ImagesCat. No.: HY-P11075CAS No.: 2770688-04-3[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) is a selective NK2R agonist with an EC50 of 3.7 nM for hNK2R. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) significantly inhibits weight loss in diet-induced obese (DIO) mice model and improves Loperamide (HY-156131)-induced dysfunctional voiding in wild-type mice. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) can be used for neurokinin receptor mediated disorders, such as obesity, insulin resistance and type 2 diabetes research.
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(R)-Casopitant
0 ImagesSynonyms: (R)-GW679769(R)-Casopitant ((R)-GW679769) is the isomer of Casopitant (HY-14405). Casopitant is a NK(1)-receptor antagonist. Casopitant can be used for the research of chemotherapy-induced nausea and vomiting.
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Substance P, Free Acid
0 ImagesSubstance P, Free Acid is a native substance P analog, but shows no biological activity of substance P.
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SR140333B
0 ImagesCat. No.: HY-161835CAS No.: 155418-06-7SR140333B is a selective NK1 receptor inhibitor that can reduce LPS-induced fever and mitigate LPS (HY-D1056)-induced changes in brain tissue in rats.
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Benzomalvin A
0 ImagesCat. No.: HY-118463CAS No.: 157047-96-6Synonyms: (-)-Benzomalvin ABenzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively.
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Leucyl-phenylalanine amide
0 ImagesCat. No.: HY-137462CAS No.: 38678-60-3Synonyms: L-Leucyl-L-phenylalaninamideLeucyl-phenylalanine amide (L-Leucyl-L-phenylalaninamide) is a dipeptide analog. Leucyl-phenylalanine amide is a ligand of SP1-7 with a Ki value of 10.2 nM. Leucyl-phenylalanine amide shows no binding activity to human NK-1 or NK-3 receptors.
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Maropitant citrate hydrate
0 ImagesMaropitant citrate hydrate is the citrate hydrate of Maropitant (HY-10053). Maropitant is an orally active NK1 receptor antagonist. Maropitant prevents vomiting and inhibits ulcerative dermatitis.
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[MePhe8,Sar9] Substance P
![[MePhe8,Sar9] Substance P](https://file.medchemexpress.com/product_pic/hy-p3927.gif "Click to View [MePhe8,Sar9] Substance P Product Detail")
0 ImagesCat. No.: HY-P3927CAS No.: 77128-76-8Synonyms: [MePhe8-MeGly9] Substance P[MePhe8,Sar9] Substance P ([MePhe8-MeGly9] Substance P) is an analog of Substance P (HY-P0201). Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
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S 16474
0 ImagesCat. No.: HY-120928CAS No.: 149250-10-2S 16474 is a cyclic peptide with antagonistic effects on NK1 and NK2 receptors. S 16474 can be used in the study of neurogenic inflammation.
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Acetylaszonalenin
0 ImagesCat. No.: HY-119552CAS No.: 42230-55-7Synonyms: LL-S490βAcetylaszonalenin, a prenylated indole derivative, is a fungal metabolite.Acetylaszonalenin is a potent neurokinin-1 (NK1) receptor antagonist. Acetylaszonalenin shows inhibition of [3H]-SP binding to human astrocytoma cells with a Ki of 170 μM.
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Substance P (2-11)
0 ImagesCat. No.: HY-P3896CAS No.: 53749-61-4Substance P (2-11) is a substance P (SP) fragment peptide. Substance P (2-11) has contracting activities on guinea pig ileum. Substance P (2-11) inhibits the permeation of 3H SP in BBMEC monolayers.
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Fezolinetant-d4
0 ImagesCat. No.: HY-19632SSynonyms: ESN-364-d4Fezolinetant-d4 (ESN-364-d4) is the deuterium labeled Fezolinetant (HY-19632). Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
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GSK256471
0 ImagesCat. No.: HY-116268CAS No.: 1133706-08-7GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia.
