Neurokinin 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.
Targets for Neurokinin Receptor
Products for Neurokinin Receptor
- Cat.No. Product Name Information
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GC69805
(R)-Casopitant
(R)-GW679769
(R)-Casopitant ((R)-GW679769) is an isomer of Casopitant. Casopitant is an NK(1) receptor antagonist that can be used in the research of chemotherapy-induced nausea and vomiting.
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GC15200
Aprepitant
Emend, L754,030, MK-869, ONO7436
Aprepitant is a novel and highly selective Neurokinin-1 (NK-1) receptor antagonist.
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GC33724
Befetupitant (Ro67-5930)
Ro67-5930
Befetupitant (Ro67-5930) is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.
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GA20847
Biotinyl-Substance P
Biotinyl-Substance P is the biotin tagged Substance P.
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GC62888
Casopitant mesylate
GW679769B
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist.
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GC50042
CP 122721 hydrochloride
High affinity NK1 antagonist
-
GC35751
CS-003 Free base
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively.
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GC62951
Elinzanetant
NT-814; BAY3427080
Elinzanetant is a neurokinin receptors antagonist used for the research of Schizophrenia.
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GC15591
Eprazinone 2HCl
NSC 317935
Eprazinone 2HCl is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties.
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GC30104
Fezolinetant (ESN-364)
Fezolinetant (ESN-364) is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
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GC16246
Fosaprepitant
Neurokinin-1 antagonist
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GC10659
Fosaprepitant dimeglumine salt
MK 0517
Fosaprepitant dimeglumine salt (MK-0517) is a prodrug of Aprepitant.
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GC64711
Fosnetupitant
Fosnetupitant (Pronetupitant) a methylene phosphate prodrug of Netupitant.
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GC16408
GR 159897
neurokinin NK2 receptor antagonist,orally active
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GC50069
GR 203040
Potent and selective NK1 antagonist
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GC18080
GR 73632
Potent and selective tachykinin NK1 receptor agonist
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GC13239
Hemokinin 1 (mouse)
agonist at the tachykinin NK1 receptor
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GC31199
Ibodutant (MEN 15596)
MEN 15596
Ibodutant (MEN 15596) (MEN 15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1.
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GC31145
Kassinin
Kassinin is a peptide derived from the Kassina frog.
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GC72876
L-703606 oxalate hydrate
L-703606 oxalate drate is a potent, selective antagonist of NK1 receptor.
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GC18128
L-732,138
tachykinin NK1 receptor antagonist
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GC36543
Maropitant
CJ-11,972
Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist.
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GC25618
Maropitant citrate
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GC71154
MEN 10207
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist.
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GC17547
MEN 10376
DYWVWWK-NH2, Asp-Tyr-Trp-Val-Trp-Trp-Lys-NH2
NK2 receptor antagonist
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GC36582
Men 10376 TFA
Neurokinin-2 receptor antagonist TFA
Men 10376 TFA 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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GC31300
MEN11467
MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK1 receptor antagonist.
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GC34408
Monohydroxy Netupitant D6
Monohydroxy Netupitant D6 is the deuterium labeled Monohydroxy Netupitant, which is a metabolite of Netupitant.
-
GC17596
Netupitant
Ro 6731898/000
neurokinin 1 (NK1) receptor antagonist
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GC34418
Netupitant D6 (CID-6451149 D6)
-
GC33559
Netupitant metabolite Monohydroxy Netupitant (Monohydroxy Netupitant)
Monohydroxy Netupitant is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist.
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GC45824
Netupitant-d6
An internal standard for the quantification of netupitant
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GC11738
Neurokinin A (porcine)
Neurokinin A (porcine) (Substance K), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor.
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GC61486
Neurokinin A TFA
Substance K TFA; Neurokinin α TFA; Neuromedin L TFA
Neurokinin A TFA is an endogenous tachykinin neuropeptide and a potent selective agonist of the neurokinin 2 receptor (NK2R).
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GC36725
Neurokinin A(4-10)
Neurokinin A (4-10) is a tachykinin NK2 receptor agonist.
-
GC34683
Neurokinin A(4-10) TFA
Neurokinin A (4-10) TFA is a tachykinin NK2 receptor agonist.
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GC32020
Neurokinin antagonist 1
Neurokinin antagonist 1 is a Neurokinin antagonist extracted from patent WO1998045262A1.
-
GC11801
Neurokinin B (human, porcine)
Neurokinin B (human, porcine) belongs to the tachykinin family of peptides.
-
GC34684
Neurokinin B TFA
Neurokinin B TFA belongs to the tachykinin family of peptides.
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GC30347
NK-1 Antagonist 1
NK-1 Antagonist 1 (NK-1 Antagonist 1) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression.
-
GC69568
NK1 receptor antagonist 2
NK1 receptor antagonist 2 is an NK1 receptor antagonist. It can be used for research on tinnitus and hearing loss.
-
GC36749
NKP608
NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.
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GC63131
Orvepitant maleate
GW823296 maleate
Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor.
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GC38829
Osanetant
Osanetant (SR142801) is a selective NK3 receptor antagonist.
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GC30861
Pavinetant (MLE-4901)
AZD 2624, AZD 4901
Pavinetant (MLE-4901) (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
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GC31156
Physalaemin
Physalaemin, a non-mammalian tachykinin, binds selectively to neurokinin-1 (NK1) receptor with high affinity.
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GC15449
Rolapitant
Orally active neurokinin NK1 receptor antagonist.
-
GC31143
Saredutant (SR 48968)
SR 48968; SR 48968C
Saredutant (SR 48968) is a selective (Neurokinin 2) NK2 receptor antagonist with an IC50 value of 0.13nM.
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GC10107
SB-222200
An NK3 receptor antagonist
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GC31198
Scyliorhinin II
Scyliorhinin II is a selective neurokinin-3 receptor agonist, with a Ki of 2.5 nM for neurokinin-3 receptor in rat cerebral cortex.
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GC14839
Senktide
NK3 tachykinin receptor agonist
-
GC33691
Serlopitant (VPD-737)
Serlopitant (VPD-737) is a selective Neurokinin-1 (NK-1) receptor antagonist.
-
GC69933
Spantide I TFA
Spantide I TFA is an analogue of substance P and a selective antagonist of the neurokinin-1 receptor (NK1 receptor), with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptors, respectively. Spantide I can reduce type 1 cytokines in infected corneas and enhance type 2 cytokine IL-10, thereby significantly reducing corneal perforation.
-
GC37680
SSR-241586
SSR-241586 is an antagonist of neurokinin receptors.
-
GC15649
Substance P
Substance P, an important neuropeptide neurotransmitter, stimulates phosphatidylinositol turnover with an EC50 value of 0.36nM.
-
GC37695
Substance P (1-7)(TFA)
-
GC72212
Substance P (5-11) (TFA)
Substance P (5-11) TFA TFA, the C-terminal heptapeptide of Substance P (Substance P ), is a neuropeptide.
-
GC37696
Substance P 1-7
Substance P 1-7 is a fragment of the neuropeptide, substance P (SP).
-
GC37697
Substance P 1-9
Substance P 1-9 is nonapeptide, which decreases the inactivation of substance P by the guinea-pig ileum and urinary bladder.
-
GC37698
Substance P 7-11
Substance P 7-11 is a C-terminal fragment of Substance P which can cause an increase in the intracellular calcium concentration.
-
GC39509
Substance P TFA
Neurokinin P TFA
Substance P TFA (Neurokinin P TFA) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
-
GC31221
Tachykinin angatonist 1
Tachykinin angatonist 1 is a neurokinin receptor antagonist extracted from patent US5968923, compound example 32.
-
GC16026
Talnetant
SB-223412
A nonpeptide NK3 antagonist
-
GC37730
Talnetant hydrochloride
SB 223412 hydrochloride; SB 223412-A
Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells.
-
GC33735
Tradipitant (VLY-686)
VLY-686; LY686017
Tradipitant (VLY-686) (VLY-686) is a neurokinin-1 (NK-1) antagonist.
-
GC33747
Vofopitant (GR 205171)
GR 205171
Vofopitant (GR 205171) is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.
-
GC37918
Vofopitant dihydrochloride
GR 205171A
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent.
-
GC30945
Y1 receptor antagonist 1
H 409-22 isomer
Y1 receptor antagonist 1 (H 409-22 isomer) is a neuropeptide Y1 receptor antagonist.
-
GC72766
Y1 receptor antagonist 1 formic
H 409-22 isomer formic
Y1 receptor antagonist 1 formic (H 409-22 isomer formic) is the formic salt form of Y1 receptor antagonist 1.
-
GC15122
[bAla8]-Neurokinin A(4-10)
MEN 10210
NK2 receptor agonist
-
GC72115
[D-Pro2] Spantide I TFA
[D-Pro2] Spantide I TFA is a Spantide analog.
-
GC35019
[Nle11]-Substance P
[Nle11]-Substance P is a substance P analog that avoids methionine oxidation problems.
-
GC13610
[Sar9,Met(O2)11]-Substance P
NK1 tachykinin receptor agonist
-
GC38013
[Sar9,Met(O2)11]-Substance P TFA
[Sar9,Met(O2)11]-Substance P TFA is a tachykinin NK1 receptor selective agonist.
-
GC35027
[Sar9] Substance P
[Sar9] Substance P is a potent and selective neurokinin (NK)-1 receptor agonist.