2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Neurokinin Receptor

Neurokinin Receptor

NK receptor; Tachykinin receptor

Neurokinin Receptor

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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:

Neurokinin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P10599
    Scyliorhinin I
    		Agonist
    Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guinea pig ileum.
    Scyliorhinin I
  • HY-P1278B
    GR 64349 acetate
    		Agonist
    GR 64349 acetate is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 acetate selectively activates the NK-2 receptor subtype. GR 64349 acetate activates tonic and rhythmic bladder contractions of the micturition reflex. GR 64349 acetate does not inhibit rhythmic bladder contraction activation induced by normal saline. GR 64349 acetate induces inward currents.
    GR 64349 acetate
  • HY-W755425
    Senktide TFA
    		Agonist
    Senktide 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.
    Senktide TFA
  • HY-P3092
    Phyllomedusin
    		Agonist
    Phyllomedusin, an tachykinin decapeptide, is a NK1 receptor agonist. Phyllomedusin has vasodilating activity and provokes the contraction of the pylorus.
    Phyllomedusin
  • HY-P1278A
    GR 64349 TFA
    		Agonist
    GR 64349 is a potent and highly selective NK2 receptor peptide agonist, with an EC50 of 3.7 nM in rat colon. GR 64349 exhibits selectivity >1000 and >300-fold with respect to NK1 and NK3 receptors, respectively.
    GR 64349 TFA
  • HY-P2793
    Uperolein
    		Agonist
    Uperolein is a physalaemin-like endecapeptide, produced in the skin of Uperoleia rugosa and Uperoleia marmorata. Uperolein has a spasmodic effect on both the gastrointestinal tract and longitudinal muscles.
    Uperolein
  • HY-P1506
    [Nle11]-Substance P
    		Agonist
    [Nle11]-Substance P is a substance P analog that avoids methionine oxidation problems.
    [Nle11]-Substance P
  • HY-P1588
    Scyliorhinin II
    		Agonist
    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
  • HY-P1279
    [Lys5,MeLeu9,Nle10]-NKA(4-10)
    		Agonist
    [Lys5,MeLeu9,Nle10]-NKA(4-10) is a highly selective and potent NK2 receptor agonist, with an IC50 of 6.1 nM.
    [Lys5,MeLeu9,Nle10]-NKA(4-10)
  • HY-125304
    L 363851
    		Agonist
    L 363851 is a Neurokinin 2 receptor agonist, and induces the contractile response of tracheal smooth muscle devoid of epithelium (IC50 of 3.2 nM) and phosphoinositide hydrolysis (IC50 of 36 μM).
    L 363851
  • HY-P1379
    C14TKL-1
    		Agonist
    C14TKL-1 is a tachykinin-like peptide and exhibits an agonistic activity for neurokinin receptor 1 (NK-1).
    C14TKL-1
  • HY-P1379A
    C14TKL-1 acetate
    		Agonist
    C14TKL-1 acetate is the acetate salt form of C14TKL-1 (HY-P1379). C14TKL-1 acetate is a tachykinin-like peptide and exhibits an agonistic activity for neurokinin receptor 1 (NK-1).
    C14TKL-1 acetate
  • HY-P11075
    [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10)
    		Agonist
    [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.
    [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10)
  • HY-P2475
    [Pro9]-Substance P
    		Agonist
    [Pro9]-Substance P is a potent, reversible and selective agonist of NK-1 tachykinin receptors with an EC50 of 0.93 nM.
    [Pro9]-Substance P
  • HY-P1279A
    [Lys5,MeLeu9,Nle10]-NKA(4-10) TFA
    		Agonist
    [Lys5,MeLeu9,Nle10]-NKA(4-10) TFA is a highly selective and potent NK2 receptor agonist, with an IC50 of 6.1 nM.
    [Lys5,MeLeu9,Nle10]-NKA(4-10) TFA
  • HY-P11429
    [Asp5,6,Me-Phe8] Substance P (5-11)
    		Agonist
    [Asp5,6,Me-Phe8] Substance P (5-11) is a tachykinin NK-3 receptor agonist. [Asp5,6,Me-Phe8] Substance P (5-11) reduces alcohol intake in genetically selected alcohol-preferring rats.
    [Asp5,6,Me-Phe8] Substance P (5-11)
  • HY-P3848
    Tyr0-Neurokinin A
    		Agonist
    Tyr0-Neurokinin A is a neuropeptide belongs to tachykinin peptide family. Tyr0-Neurokinin A is an agonist of Tacr2. Tyr0-Neurokinin A can be used in the research of insulin resistance, obesity, diabetes.
    Tyr0-Neurokinin A
  • HY-B1392A
    Esmolol
    		Agonist
    Esmolol is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol attenuates post resuscitation myocardial dysfunction. Esmolol improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.
    Esmolol
  • HY-G0012S
    Monohydroxy Netupitant-d6
    		Agonist
    Monohydroxy Netupitant-d6 is the deuterium labeled Monohydroxy Netupitant, which is a metabolite of Netupitant.
    Monohydroxy Netupitant-d<sub>6</sub>
  • HY-G0012
    Netupitant metabolite Monohydroxy Netupitant
    		Agonist
    Monohydroxy Netupitant is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist.
    Netupitant metabolite Monohydroxy Netupitant
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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