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-P3932
    [Sar4] Substance P (4-11)
    [Sar4] Substance P (4-11) is an analog of Substance P (4-11). Substance P (4-11), the C-terminus fragment of Substance P (Substance P (HY-P0201)), is a Substance P agonist.
    [Sar4] Substance P (4-11)
  • HY-116620
    Benzomalvin C
    Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg/mL in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It is isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.
    Benzomalvin C
  • HY-P3853
    GR 87389
    		Inhibitor
    GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra.
    GR 87389
  • 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-12142S
    rac-Vofopitant-d3
    		Antagonist
    rac-Vofopitant-d3 (rac-GR 205171-d3) is the deuterium labeled Vofopitant (HY-12142). 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.
    rac-Vofopitant-d<sub>3</sub>
  • 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-169511
    Anthrotainin
    		Inhibitor
    Anthrotainin, a tetracyclic compound, is a substance P binding inhibitor with an IC50 of 3 μM.
    Anthrotainin
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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