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

Neurokinin Receptor

NK receptor; Tachykinin receptor

Neurokinin Receptor

Related Products

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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-P3849
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10)
    		Agonist 99.83%
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues.
    [Lys5,MeLeu9,Nle10]Neurokinin A(4-10)
  • HY-108479
    Nolpitantium
    		Antagonist
    Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation.
    Nolpitantium
  • HY-P3801
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11)
    		Modulator 99.01%
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats.
    [Glp5,(Me)Phe8,Sar9] Substance P (5-11)
  • HY-P1278
    GR 64349
    		Antagonist 99.45%
    GR 64349 is a potent and highly selective NK2 receptor peptide antagonist, 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
  • HY-P2000
    Septide
    		Agonist 98.97%
    Septide ((Pyr6,Pro9)-Substance P) is a potent NK1 receptor agonist with a Kd value of 0.55 nM.
    Septide
  • HY-12114
    Serlopitant
    		Antagonist
    Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.
    Serlopitant
  • HY-P0242
    Neurokinin B
    		Agonist
    Neurokinin B belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs-including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect.
    Neurokinin B
  • HY-P3862
    [MePhe7]-Neurokinin B
    		Inhibitor 98.87%
    [MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC50 value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R).
    [MePhe7]-Neurokinin B
  • HY-16436
    Rolapitant hydrochloride hydrate
    		Antagonist 98.25%
    Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model.
    Rolapitant hydrochloride hydrate
  • HY-12142
    Vofopitant
    		Antagonist 99.82%
    Vofopitant 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
  • HY-14407
    Fosaprepitant
    		Antagonist
    Fosaprepitant (L-785298) is a proagent of Aprepitant (HY-10052). Fosaprepitant is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
    Fosaprepitant
  • HY-P3889
    Substance P (6-11)
    Substance P (6-11) is the C-terminal hexapeptideamide of Substance P (Substance P (HY-P0201)). Substance P (6-11) binds to NK-1 tachykinin receptor. Substance P (6-11) shows depolarization of motoneurons and a hypotensive effect.
    Substance P (6-11)
  • HY-P3861
    Biotin-NeurokininA
    Biotin-NeurokininA is a biotinylated NeurokininA (HY-P0197). Neurokinin A (Substance K), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor. Neurokinin A acts as a major mediator in human airway and gastrointestinal tissues.
    Biotin-NeurokininA
  • HY-108480
    SDZ NKT 343
    		Antagonist
    SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity.
    SDZ NKT 343
  • HY-P1186
    Eledoisin Related Peptide
    		Activator 98.96%
    Eledoisin Related Peptide is a Substance P analog that excites neurons and triggers behavioral responses. Eledoisin Related Peptide is also a tachykinin receptor ligand.
    Eledoisin Related Peptide
  • HY-P1198A
    Hemokinin 1, human TFA
    		Agonist
    Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia.
    Hemokinin 1, human TFA
  • HY-19633
    CS-003 Free base
    		Antagonist
    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 (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.
    CS-003 Free base
  • HY-P4709
    (Trp7,β-Ala8)-Neurokinin A (4-10)
    		Antagonist
    (Trp7,β-Ala8)-Neurokinin A (4-10) is a potent neurokinin-3 (NK3) antagonist.
    (Trp7,β-Ala8)-Neurokinin A (4-10)
  • HY-114673
    Benzomalvin B
    		Inhibitor
    Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P.
    Benzomalvin B
  • HY-106659
    SCH 900978
    		Antagonist
    SCH 900978 (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.
    SCH 900978
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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