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)-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.
- GC15200 Aprepitant Substance P (SP) inhibitor
- GC33724 Befetupitant (Ro67-5930) Befetupitant (Ro67-5930) is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) 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.
- GC30104 Fezolinetant (ESN-364) Fezolinetant (ESN-364) is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
- GC16246 Fosaprepitant Neurokinin-1 antagonist
- GC10659 Fosaprepitant dimeglumine salt Fosaprepitant dimeglumine salt (MK-0517) is a prodrug of Aprepitant.
- GC64711 Fosnetupitant Fosnetupitant (Pronetupitant) a methylene phosphate prodrug of Netupitant.
- GC16408 GR 159897 neurokinin NK2 receptor antagonist,orally active
- GC18080 GR 73632 Potent and selective tachykinin NK1 receptor agonist
-
GC13239
Hemokinin 1 (mouse)
agonist at the tachykinin NK1 receptor
- GC31199 Ibodutant (MEN 15596) Ibodutant (MEN 15596) (MEN 15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1.
- GC31145 Kassinin Kassinin is a peptide derived from the Kassina frog.
- GC18128 L-732,138 tachykinin NK1 receptor antagonist
- GC36543 Maropitant Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist.
- GC25618 Maropitant citrate
- GC17547 MEN 10376 NK2 receptor antagonist
- GC36582 Men 10376 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.
- GC31300 MEN11467 MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK1 receptor antagonist.
- GC34408 Monohydroxy Netupitant D6 Monohydroxy Netupitant D6 is the deuterium labeled Monohydroxy Netupitant, which is a metabolite of Netupitant.
- GC17596 Netupitant neurokinin 1 (NK1) receptor antagonist
- 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.
- GC11738 Neurokinin A (porcine) Neurokinin A (porcine) (Substance K), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor.
- 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.
- 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.
- GC38829 Osanetant Osanetant (SR142801) is a selective NK3 receptor antagonist.
- GC30861 Pavinetant (MLE-4901) Pavinetant (MLE-4901) (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
-
GC31156
Physalaemin
Physalaemin, a non-mammalian tachykinin, binds selectively to neurokinin-1 (NK1) receptor with high affinity.
- GC15449 Rolapitant Orally active neurokinin NK1 receptor antagonist.
- GC31143 Saredutant (SR 48968) Saredutant (SR 48968) is a selective NK2 receptor antagonist.
- 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.
- 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 Sensory neuropeptide and inflammatory mediator
- GC37695 Substance P (1-7)(TFA)
- 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.
- GC31221 Tachykinin angatonist 1 Tachykinin angatonist 1 is a neurokinin receptor antagonist extracted from patent US5968923, compound example 32.
- GC37730 Talnetant hydrochloride 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) Tradipitant (VLY-686) (VLY-686) is a neurokinin-1 (NK-1) antagonist.
- GC33747 Vofopitant (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 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
Y1 receptor antagonist 1 (H 409-22 isomer) is a neuropeptide Y1 receptor antagonist.
- GC15122 [bAla8]-Neurokinin A(4-10) NK2 receptor agonist
- 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.