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-120167
    YM-44778
    		Antagonist
    YM-44778 is a neurokinin receptor antagonist. The pKi values for NK1, NK2 and NK3 are 8.08, 8.55 and 8.24, respectively. YM-44778 inhibits the increase of bladder pressure induced by substance [Sar9,Met(O2)11] -P (HY-P1012) in anestheticized rats.
    YM-44778
  • HY-P3880
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P
    		Antagonist
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P is a neuropeptide Substance P (HY-P0201) antagonist.
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P
  • HY-P3808
    [D-Pro2,D-Trp7,9] Substance P
    		Antagonist
    [D-Pro2,D-Trp7,9] Substance P, a Substance P (HY-P0201) analogue, is a weak agonist and a potent, specific, competitive Substance P antagonist.
    [D-Pro2,D-Trp7,9] Substance P
  • HY-W370556
    (Rac)-LM11A-31
    		Control
    (Rac)-LM11A-31 is a racemate of LM11A-31. LM11A-31 is a non-peptide modulator of p75NTR (neurotrophin receptor p75) and is an orally effective proNGF antagonist.
    (Rac)-LM11A-31
  • 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-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-W777166
    Aprepitant-13C2,d2 (Major)
    		Inhibitor
    Aprepitant-13C2,d2 (Major) (MK-0869-13C2,d2) is 13C labeled Aprepitant. Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
    Aprepitant-<sup>13</sup>C<sub>2</sub>,d<sub>2</sub> (Major)
  • HY-109171R
    Elinzanetant (Standard)
    		Antagonist
    Elinzanetant (Standard) is the analytical standard of Elinzanetant. This product is intended for research and analytical applications. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women.
    Elinzanetant (Standard)
  • HY-105346
    WIN 51708
    		Antagonist
    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-177079S
    Dazodeunetant
    		Inhibitor
    Dazodeunetant (Example 56) is a nitrogen-containing fused ring derivative. Dazodeunetant is an inhibitor of neurokinin (NK). Dazodeunetant has an IC50 0f 75.99 nM against NK3R in HEK293-NK3 (IP1). Dazodeunetant can be studied in research for menopausal hot flashes.
    Dazodeunetant
  • HY-172514
    (1R,2S,3R)-Aprepitant
    		Antagonist
    (1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive human neurokinin-1 (NK-1) receptor antagonist. (1R,2S,3R)-Aprepitant is promising for research of cancers and postoperative nausea and vomiting.
    (1R,2S,3R)-Aprepitant
  • HY-10053B
    Maropitant citrate
    		Antagonist
    Maropitant citrate is an orally active NK1 receptor antagonist. Maropitant citrate prevents vomiting and inhibits ulcerative dermatitis.
    Maropitant citrate
  • HY-119005A
    YM-49598 iodide
    		Antagonist
    YM-49598 iodide is a tachykinin NK-1 receptor antagonist. YM-49598 iodide can inhibit drug-induced bladder contraction in rats, with IC50 of 11 μg/kg.
    YM-49598 iodide
  • HY-14551C
    Osanetant monohydrochloride
    		Antagonist
    Osanetant (SR142801) monohydrochloride is a selective NK3 receptor antagonist. Osanetant monohydrochloride produces anxiolytic- and antidepressant-like effects.
    Osanetant monohydrochloride
  • HY-N7574
    WS9326A
    		Antagonist
    WS9326A is a tachykinin receptor antagonist that can be isolated from Streptomyces violaceus.
    WS9326A
  • HY-19429A
    SLV-317
    		Antagonist
    SLV-317 is an antagonist of the neurokinin-1 receptor with oral activity. SLV-317 can effective antagonist of substance P-induced effects.
    SLV-317
  • HY-10053R
    Maropitant (Standard)
    		Antagonist
    Maropitant (Standard) is the analytical standard of Maropitant. This product is intended for research and analytical applications. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting.
    Maropitant (Standard)
  • HY-14432R
    Pavinetant (Standard)
    		Antagonist
    Pavinetant (Standard) is the analytical standard of Pavinetant. This product is intended for research and analytical applications. Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
    Pavinetant (Standard)
  • HY-109171S
    Elinzanetant-d3
    		Antagonist
    Elinzanetant-d3 (NT-814-d3) is deuterium labeled Elinzanetant. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women.
    Elinzanetant-d<sub>3</sub>
  • HY-107693
    SSR 146977 hydrochloride
    		Antagonist
    SSR 146977 hydrochloride is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 hydrochloride can be used in the study of psychiatric disorders and airway inflammation.
    SSR 146977 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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