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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

  1. Cat.No. Product Name Information
  2. 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.

    (R)-Casopitant  Chemical Structure
  3. GC15200 Aprepitant Substance P (SP) inhibitor Aprepitant  Chemical Structure
  4. GC33724 Befetupitant (Ro67-5930) Befetupitant (Ro67-5930) is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist. Befetupitant (Ro67-5930)  Chemical Structure
  5. 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. CS-003 Free base  Chemical Structure
  6. GC30104 Fezolinetant (ESN-364) Fezolinetant (ESN-364) is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes. Fezolinetant (ESN-364)  Chemical Structure
  7. GC16246 Fosaprepitant Neurokinin-1 antagonist Fosaprepitant  Chemical Structure
  8. GC10659 Fosaprepitant dimeglumine salt Fosaprepitant dimeglumine salt (MK-0517) is a prodrug of Aprepitant. Fosaprepitant dimeglumine salt  Chemical Structure
  9. GC64711 Fosnetupitant Fosnetupitant (Pronetupitant) a methylene phosphate prodrug of Netupitant. Fosnetupitant  Chemical Structure
  10. GC16408 GR 159897 neurokinin NK2 receptor antagonist,orally active GR 159897  Chemical Structure
  11. GC18080 GR 73632 Potent and selective tachykinin NK1 receptor agonist GR 73632  Chemical Structure
  12. GC13239 Hemokinin 1 (mouse)

    agonist at the tachykinin NK1 receptor

    Hemokinin 1 (mouse)  Chemical Structure
  13. GC31199 Ibodutant (MEN 15596) Ibodutant (MEN 15596) (MEN 15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1. Ibodutant (MEN 15596)  Chemical Structure
  14. GC31145 Kassinin Kassinin is a peptide derived from the Kassina frog. Kassinin  Chemical Structure
  15. GC18128 L-732,138 tachykinin NK1 receptor antagonist L-732,138  Chemical Structure
  16. GC36543 Maropitant Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant  Chemical Structure
  17. GC25618 Maropitant citrate Maropitant citrate  Chemical Structure
  18. GC17547 MEN 10376 NK2 receptor antagonist MEN 10376  Chemical Structure
  19. 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. Men 10376 TFA  Chemical Structure
  20. GC31300 MEN11467 MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK1 receptor antagonist. MEN11467  Chemical Structure
  21. GC34408 Monohydroxy Netupitant D6 Monohydroxy Netupitant D6 is the deuterium labeled Monohydroxy Netupitant, which is a metabolite of Netupitant. Monohydroxy Netupitant D6  Chemical Structure
  22. GC17596 Netupitant neurokinin 1 (NK1) receptor antagonist Netupitant  Chemical Structure
  23. GC34418 Netupitant D6 (CID-6451149 D6) Netupitant D6 (CID-6451149 D6)  Chemical Structure
  24. GC33559 Netupitant metabolite Monohydroxy Netupitant (Monohydroxy Netupitant) Monohydroxy Netupitant is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist. Netupitant metabolite Monohydroxy Netupitant (Monohydroxy Netupitant)  Chemical Structure
  25. GC11738 Neurokinin A (porcine) Neurokinin A (porcine) (Substance K), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor. Neurokinin A (porcine)  Chemical Structure
  26. GC36725 Neurokinin A(4-10) Neurokinin A (4-10) is a tachykinin NK2 receptor agonist. Neurokinin A(4-10)  Chemical Structure
  27. GC34683 Neurokinin A(4-10) TFA Neurokinin A (4-10) TFA is a tachykinin NK2 receptor agonist. Neurokinin A(4-10) TFA  Chemical Structure
  28. GC32020 Neurokinin antagonist 1

    Neurokinin antagonist 1 is a Neurokinin antagonist extracted from patent WO1998045262A1.

    Neurokinin antagonist 1  Chemical Structure
  29. GC11801 Neurokinin B (human, porcine) Neurokinin B (human, porcine) belongs to the tachykinin family of peptides. Neurokinin B (human, porcine)  Chemical Structure
  30. GC34684 Neurokinin B TFA Neurokinin B TFA belongs to the tachykinin family of peptides. Neurokinin B TFA  Chemical Structure
  31. 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. NK-1 Antagonist 1  Chemical Structure
  32. 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.

    NK1 receptor antagonist 2  Chemical Structure
  33. 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. NKP608  Chemical Structure
  34. GC38829 Osanetant Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant  Chemical Structure
  35. GC30861 Pavinetant (MLE-4901) Pavinetant (MLE-4901) (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist. Pavinetant (MLE-4901)  Chemical Structure
  36. GC31156 Physalaemin

    Physalaemin, a non-mammalian tachykinin, binds selectively to neurokinin-1 (NK1) receptor with high affinity.

    Physalaemin  Chemical Structure
  37. GC15449 Rolapitant Orally active neurokinin NK1 receptor antagonist. Rolapitant  Chemical Structure
  38. GC31143 Saredutant (SR 48968) Saredutant (SR 48968) is a selective NK2 receptor antagonist. Saredutant (SR 48968)  Chemical Structure
  39. 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. Scyliorhinin II  Chemical Structure
  40. GC14839 Senktide NK3 tachykinin receptor agonist Senktide  Chemical Structure
  41. GC33691 Serlopitant (VPD-737) Serlopitant (VPD-737) is a selective Neurokinin-1 (NK-1) receptor antagonist. Serlopitant (VPD-737)  Chemical Structure
  42. 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.

    Spantide I TFA  Chemical Structure
  43. GC37680 SSR-241586 SSR-241586 is an antagonist of neurokinin receptors. SSR-241586  Chemical Structure
  44. GC15649 Substance P Sensory neuropeptide and inflammatory mediator Substance P  Chemical Structure
  45. GC37695 Substance P (1-7)(TFA) Substance P (1-7)(TFA)  Chemical Structure
  46. GC37696 Substance P 1-7 Substance P 1-7 is a fragment of the neuropeptide, substance P (SP). Substance P 1-7  Chemical Structure
  47. 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. Substance P 1-9  Chemical Structure
  48. 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. Substance P 7-11  Chemical Structure
  49. GC31221 Tachykinin angatonist 1 Tachykinin angatonist 1 is a neurokinin receptor antagonist extracted from patent US5968923, compound example 32. Tachykinin angatonist 1  Chemical Structure
  50. 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. Talnetant hydrochloride  Chemical Structure
  51. GC33735 Tradipitant (VLY-686) Tradipitant (VLY-686) (VLY-686) is a neurokinin-1 (NK-1) antagonist. Tradipitant (VLY-686)  Chemical Structure
  52. 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. Vofopitant (GR 205171)  Chemical Structure
  53. 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. Vofopitant dihydrochloride  Chemical Structure
  54. GC30945 Y1 receptor antagonist 1

    Y1 receptor antagonist 1 (H 409-22 isomer) is a neuropeptide Y1 receptor antagonist.

    Y1 receptor antagonist 1  Chemical Structure
  55. GC15122 [bAla8]-Neurokinin A(4-10) NK2 receptor agonist [bAla8]-Neurokinin A(4-10)  Chemical Structure
  56. GC35019 [Nle11]-Substance P [Nle11]-Substance P is a substance P analog that avoids methionine oxidation problems. [Nle11]-Substance P  Chemical Structure
  57. GC13610 [Sar9,Met(O2)11]-Substance P

    NK1 tachykinin receptor agonist

    [Sar9,Met(O2)11]-Substance P  Chemical Structure
  58. GC38013 [Sar9,Met(O2)11]-Substance P TFA [Sar9,Met(O2)11]-Substance P TFA is a tachykinin NK1 receptor selective agonist. [Sar9,Met(O2)11]-Substance P TFA  Chemical Structure
  59. GC35027 [Sar9] Substance P [Sar9] Substance P is a potent and selective neurokinin (NK)-1 receptor agonist. [Sar9] Substance P  Chemical Structure

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