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 Activator
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Neurokinin Receptor Modulators
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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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NK3R-IN-2
0 ImagesCat. No.: HY-176546NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM for human NK3R. NK3R-IN-2 can pass through the blood-brain barrier. NK3R-IN-2 has excellent NK3R binding affinity (IC50 = 87.31 nM) in CHO-K1 cells. NK3R-IN-2 effectively inhibits the level of luteinizing hormone (LH). NK3R-IN-2 can be used for research on hormone related conditions.
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AWL 60
0 ImagesCat. No.: HY-P2052CAS No.: 140716-14-9AWL 60 is a compound with SP antagonist and weak opioid agonist properties, which can antagonize SP-agonists in vitro and attenuate the decrease in blood pressure caused by SP-agonists in vivo.
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Senktide TFA
0 ImagesCat. No.: HY-W755425Senktide TFA is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50=0.5-3 nM). Senktide TFA less potently agonizes the NK1 receptor (EC50=35 µM). Senktide TFA is promising for research of neurological disease.
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Maropitant-d3
0 ImagesCat. No.: HY-10053SMaropitant-d3 is the 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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[Tyr6,D-Phe7,D-His9]-Substance P (6-11)
![[Tyr6,D-Phe7,D-His9]-Substance P (6-11)](https://file.medchemexpress.com/product_pic/hy-p10619.gif "Click to View [Tyr6,D-Phe7,D-His9]-Substance P (6-11) Product Detail")
0 ImagesCat. No.: HY-P10619CAS No.: 145194-26-9
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[DAla4] Substance P (4-11)
![[DAla4] Substance P (4-11)](https://file.medchemexpress.com/product_pic/hy-p3883.gif "Click to View [DAla4] Substance P (4-11) Product Detail")
0 ImagesCat. No.: HY-P3883CAS No.: 81381-50-2[DAla4] Substance P (4-11) is an analog of Substance P (HY-P0201) that inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (HY-P0006) (IC50 of 0.5 μM) and 125I-Bolton Hunter-conjugated Substance P (IC50 of 0.15 μM) to rat brain cortex membranes.
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MEN 10207 acetate
0 ImagesCat. No.: HY-151413AMEN 10207 (acetate) is a selective antagonist of the NK-2 tachykinin receptor. MEN 10207 (acetate) induces tachykinin-induced contractions in rat bladder and guinea pig airways in vivo. MEN 10207 (acetate) inhibits [β-Ala 8 ]-NKA (4-10)-induced enhancement of bladder motility in anesthetized rats and [β-Ala 8 ]-NKA (4-10)-induced enhancement of bronchoconstriction in anesthetized guinea pigs.
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SB 414240
0 ImagesCat. No.: HY-122286CAS No.: 272104-60-6SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with Kis of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease.
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Men 10376
0 ImagesCat. No.: HY-P1276CAS No.: 135306-85-3Synonyms: Neurokinin-2 receptor antagonistMen 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
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Phyllomedusin
0 ImagesCat. No.: HY-P3092CAS No.: 26145-48-2Phyllomedusin, an tachykinin decapeptide, is a NK1 receptor agonist. Phyllomedusin has vasodilating activity and provokes the contraction of the pylorus.
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Lanepitant dihydrochloride
0 ImagesCat. No.: HY-105137CAS No.: 170508-05-1Synonyms: LY303870 dihydrochlorideLanepitant dihydrochloride (LY303870 dihydrochloride) is a non-peptide neurokinin-1 receptor antagonist. Lanepitant dihydrochloride has analgesic and anti-inflammatory activities.
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[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11)
![[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11)](https://file.medchemexpress.com/product_pic/hy-p3805.gif "Click to View [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) Product Detail")
0 ImagesCat. No.: HY-P3805CAS No.: 89430-34-2[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) is a potent neurokinin NK1 antagonist. [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) inhibits the effects of gold-protein-substance P (GPSP) and substance P (SP).
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Neuropeptide K (human, porcine, rat)
0 ImagesCat. No.: HY-P10268CAS No.: 96827-05-3Neuropeptide K, human, porcine, rat exhibits bioactivity in gallbladder contraction, protein extravasation, hypotension and brcnchial smooth muscle spasm. Neuropeptide K, human, porcine, rat is concentrated in brain and acts as tachykinin neuromessenger.
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Fosaprepitant-d4 dimeglumine
0 ImagesCat. No.: HY-14407ASSynonyms: MK-0517-d4; L785298-d4Fosaprepitant-d4 (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
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GR203040
0 ImagesCat. No.: HY-10051CAS No.: 168398-02-5GR203040 is an orally active NK1 receptor antagonist with a pKi of 10.3. GR203040 shows potent antiemetic activity.
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NK1 receptor antagonist 2
0 ImagesCat. No.: HY-145250CAS No.: 579475-17-5NK1 receptor antagonist 2 is a neurokinin 1 (NK1) receptor antagonist. NK1 receptor antagonist 2 is applicable to research related to tinnitus and hearing loss.
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GR 64349 TFA
0 ImagesCat. No.: HY-P1278AGR 64349 TFA is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 TFA selectively activates the NK-2 receptor subtype. GR 64349 TFA activates tonic and rhythmic bladder contractions of the micturition reflex. GR 64349 TFA does not inhibit rhythmic bladder contraction activation induced by normal saline. GR 64349 TFA induces inward currents.
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Imnopitant
0 ImagesCat. No.: HY-109147CAS No.: 290297-57-3Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .
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L-741671
0 ImagesCat. No.: HY-119095CAS No.: 187724-85-2L-741671 is a selective and brain-permeable antagonist of neurokininl (hNKI) receptor, with K
