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

Neurokinin Receptor

NK receptor; Tachykinin receptor

Neurokinin Receptor

Related Products

PDF 1.25 MB

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-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-10052R
    Aprepitant (Standard)
    		Inhibitor
    Aprepitant (Standard) is the analytical standard of Aprepitant. This product is intended for research and analytical applications. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant (Standard)
  • HY-P3069
    γ-Neuropeptide (rabbit)
    		Agonist 99.99%
    γ-Neuropeptide (rabbit) can be isolated from rabbit intestine. γ-Neuropeptide is an endogenous neurokinin peptide that acts as a neurokinin 2 (NK2) receptor agonist. γ-Neuropeptide mediates hypothalamic-pituitary-adrenal (HPA) axis, as well as reproductive hormone release.
    γ-Neuropeptide (rabbit)
  • 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-108481
    L-760735
    		Antagonist 99.9%
    L-760735 is a high affinity, selective and orally active NK1 receptor antagonist with an IC50 of 0.19 nM for human NK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects.
    L-760735
  • HY-P1277
    GR 94800
    		Antagonist 99.42%
    GR 94800 is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively.
    GR 94800
  • HY-107692
    SB 218795
    		Antagonist 99.86%
    SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit.
    SB 218795
  • HY-U00382
    Substance P Receptor Antagonist 1
    		Antagonist 99.42%
    Substance P Receptor Antagonist 1 has the potential function in central nervous system disorders, respiratory, inflammatory diseases and gastrointestinal disorders.
    Substance P Receptor Antagonist 1
  • HY-117380
    SB 235375
    		Antagonist 98.13%
    SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models.
    SB 235375
  • HY-P3925
    [His11]Substance P
    		98.97%
    [His11]Substance P is an analog of Substance P (HY-P0201). Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
    [His11]Substance P
  • HY-101704A
    Y1 receptor antagonist 1 formic
    		Antagonist 99.84%
    Y1 receptor antagonist 1 (H 409-22 isomer) formic (Example 4) is a neuropeptide Y1 receptor antagonist. Y1 receptor antagonist 1 can be used for the study of cardiovascular diseases, such as vasoconstriction.
    Y1 receptor antagonist 1 formic
  • HY-P3851
    (β-Ala8)-Neurokinin A (4-10)
    		Agonist
    (β-Ala8)-Neurokinin A (4-10), a neuropeptide, is a potent and selective NK-2 tachykinin receptor (Neurokinin Receptor) agonist.
    (β-Ala8)-Neurokinin A (4-10)
  • HY-105346
    WIN 51708
    		Antagonist 99.70%
    WIN 51708 is a nonpeptide antagonist of neurokinin (NK)-1 receptor. WIN 51708 has a higher affinity for the rat NK-1 receptor compared to the human NK-1 receptor.
    WIN 51708
  • HY-122347
    Orvepitant
    		Antagonist
    Orvepitant (GW823296) 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. Orvepitant can across the blood-brain barrier. Orvepitant has the potential for depressive disorder and chronic refractory cough (CRC) treatment.
    Orvepitant
  • HY-178269
    SCH-720881
    		Antagonist
    SCH-720881 is the active metabolite of Rolapitant (HY-14751). Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model.
    SCH-720881
  • HY-P3889
    Substance P (6-11)
    Substance P (6-11) is the C-terminal hexapeptideamide of 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-W011978S
    N-Acetyl-L-tryptophan-d3
    N-Acetyl-L-tryptophan-d3 is the deuterium labeled N-Acetyl-L-tryptophan (HY-W011978). N-Acetyl-L-tryptophan is an antagonist of the neurokinin-1 receptor (NK-1R), disrupting the binding of substance P (SP) to NK-1R. This action provides neuroprotective effects, improving memory deficits and motor impairments. N-Acetyl-L-tryptophan is also an inhibitor of cytochrome c (Cytochrome c), and it exerts antioxidant and anti-inflammatory effects by inhibiting the expression of IL-1β and the activation of caspase-1. N-Acetyl-L-tryptophan holds promise for research in neurodegenerative and inflammatory diseases.
    N-Acetyl-L-tryptophan-d<sub>3</sub>
  • HY-P3861
    Biotin-Neurokinin A
    Biotin-Neurokinin A is a biotinylated Neurokinin A (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-Neurokinin A
  • HY-P3598
    Substance P(1-4)
    		Antagonist
    Substance P(1-4) is a potent neurokinin receptors (NK-R) antagonist. Substance P(1-4) has regulation of normal hematopoiesis and inhibits endogenous erythroid colony (EEC) formation.
    Substance P(1-4)
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.