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-117952
    L 743310
    		Antagonist
    L 743310 is a non-peptide, selective antagonist of the human neurokinin hNK1 receptor, with high affinity for primate and cloned human hNK1 receptors and lower affinity for rodent NK1 receptors. L 743310 inhibits resiniferatoxin-induced plasma protein extravasation in guinea pig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis.
    L 743310
  • HY-P3847
    Tyr0-Neurokinin B
    Tyr0-Neurokinin B (Tyr-NKB) is an analogue of Neurokinin B. Tyr0-Neurokinin B can exerts contractions in bladder.
    Tyr0-Neurokinin B
  • 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-P1193
    GR 82334
    		Antagonist
    GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist. GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats.
    GR 82334
  • HY-P3806
    [D-Pro4,D-Trp7,9,10] Substance P (4-11)
    		Antagonist
    [D-Pro4,D-Trp7,9,10] Substance P (4-11) is a potent tachykinin antagonist.
    [D-Pro4,D-Trp7,9,10] Substance P (4-11)
  • HY-P2439
    MEN 10208
    		Antagonist
    MEN 10208 is a neurokinin A antagonist prepared by solid phase synthesis. The Fmoc strategy has more advantages than the Boc strategy in its preparation, and can obtain products with higher yield and purity.
    MEN 10208
  • HY-P3803
    [D-Pro4,D-Trp7,9] Substance P (4-11)
    		Antagonist
    [D-Pro4,D-Trp7,9] Substance P (4-11) is a potent antagonist of Substance P (HY-P0201). [D-Pro4,D-Trp7,9] Substance P (4-11) decreases plasma aldosterone (ALDO) concentration.
    [D-Pro4,D-Trp7,9] Substance P (4-11)
  • HY-P3933
    [Tyr8,Nle11] Substance P
    		Modulator
    [Tyr8,Nle11] Substance P is a Substance P (HY-P0201) analog. Substance P is a peptide mainly secreted by neurons and is involved in many biological processes, including nociception and inflammation.
    [Tyr8,Nle11] Substance P
  • HY-P3800
    [Glp5] Substance P (5-11)
    [Glp5] Substance P (5-11) is an octapeptide. [Glp5] Substance P (5-11) is one of the main substance P fragments in rat central nervous system (CNS). [Glp5] Substance P (5-11) locally modulates dopamine release in rat striatum.
    [Glp5] Substance P (5-11)
  • HY-108483
    RP 67580
    		Antagonist
    RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation.
    RP 67580
  • 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-14770
    Ibodutant
    		Antagonist
    Ibodutant (MEN 15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1.
    Ibodutant
  • 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-P3891
    Substance P (4-11)
    Substance P (4-11), the C-terminus fragment of Substance P (Substance P (HY-P0201)), is a Substance P agonist that shows highly selective for NK1 receptors.
    Substance P (4-11)
  • HY-19665
    Lanepitant
    		Antagonist
    Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis.
    Lanepitant
  • HY-P3809
    [D-Pro2,D-Phe7,D-Trp9] Substance P
    [D-Pro2,D-Phe7,D-Trp9] Substance P is a Substance P (HY-P0201) analogue. [D-Pro2,D-Phe7,D-Trp9] Substance P is an inhibitor of Substance P. [D-Pro2,D-Phe7,D-Trp9] Substance P contracts guinea-pig ileum (GPI) indirectly.
    [D-Pro2,D-Phe7,D-Trp9] Substance P
  • 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-105534
    TAK-637
    		Antagonist
    TAK-637 is an orally active neurokinin-1 receptor antagonist. TAK-637 increases bladder storage capacity. TAK-637 can be used for research of functional bowel diseases such as irritable bowel syndrome.
    TAK-637
  • HY-116822
    SSR 146977
    		Antagonist
    SSR 146977 is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 inhibits the binding of radioactive neurokinin B to NK3 receptors in Chinese hamster ovary cells, with a Ki of 0.26 nM.
    SSR 146977
  • HY-14751A
    Rolapitant hydrochloride
    		Antagonist
    Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model.
    Rolapitant hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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