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-P1278A
    GR 64349 TFA
    		Antagonist
    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 TFA
  • HY-109147
    Imnopitant
    		Antagonist
    Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .
    Imnopitant
  • HY-119095
    L-741671
    		Antagonist
    L-741671 is a selective and brain-permeable antagonist of neurokininl (hNKI) receptor, with Kis of 64 nM, 0.03 nM and 0.7 nM in rat, human and ferret, respectively.
    L-741671
  • HY-106982
    Ezlopitant
    		Antagonist
    Ezlopitant (CJ-11,974) is a selective, non-peptidic neurokinin-1 (NK-1)-receptor antagonist. Ezlopitant inhibits both acute and delayed emetic reactions induced by Cisplatin (HY-17394) in ferrets via acting on NK1 receptors in the central nervous system. Ezlopitant has the potential for pain, chemotherapy-induced emesis and irritable bowel syndrome research.
    Ezlopitant
  • HY-P3890
    Substance P (5-11)
    Substance P (5-11), the C-terminal heptapeptide of Substance P (HY-P0201), is a neuropeptide. Substance P (5-11) binds to NK-1 tachykinin receptor.
    Substance P (5-11)
  • HY-149358
    NK3R-IN-1
    		Inhibitor
    NK3R-IN-1 (compound 16x), a imidazolepiperazine derivative, is an orally active Neurokinin Receptor NK3R inhibitor. NK3R-IN-1 decreases blood luteinizing hormone levels in ovariectomy (OVX) model.
    NK3R-IN-1
  • HY-122347
    Orvepitant
    		Antagonist
    Orvepitant (GW823296) is a compound with the ability to inhibit pruritus induced by cancer epidermal growth factor receptor inhibitor (EGFRI) and is a neurokinin-1 receptor antagonist.
    Orvepitant
  • HY-P3854
    GR 83074
    		Antagonist
    GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity.
    GR 83074
  • HY-10050
    CJ-17493
    		Antagonist
    CJ-17493 is a neurokinin-1 (NK1) receptor antagonist, with a Ki of 0.2 nM. CJ-17493 shows moderate affinity for the verapamil-binding site of L-type Ca2+ channels (IC50 = 164 nM) and site 2 of sodium channels (IC50 = 48 nM). CJ-17493 can be used for the study of neurological diseases.
    CJ-17493
  • HY-P3820
    [Dehydro-Pro4] Substance P (4-11)
    [Dehydro-Pro4] Substance P (4-11) is a peptide fragment of Substance P. Substance P is a peptide mainly secreted by neurons. Substance P takes part in many biological processes, including nociception, inflammation and immunity.
    [Dehydro-Pro4] Substance P (4-11)
  • HY-P2793
    Uperolein
    		Agonist
    Uperolein is a physalaemin-like endecapeptide, produced in the skin of Uperoleia rugosa and Uperoleia marmorata. Uperolein has a spasmodic effect on both the gastrointestinal tract and longitudinal muscles.
    Uperolein
  • HY-P1506
    [Nle11]-Substance P
    		Agonist
    [Nle11]-Substance P is a substance P analog that avoids methionine oxidation problems.
    [Nle11]-Substance P
  • HY-P3887
    MLGFFQQPKPR-NH2
    MLGFFQQPKPR-NH2 is a reversed Substance P peptide. Substance P is a neuropeptide.
    MLGFFQQPKPR-NH2
  • HY-P10588
    WIN 66306
    		Antagonist
    WIN 66306 is a cyclic heptapeptide that can be isolated from an Aspergillus species. WIN 66306 is a neurokinin antagonist with antagonistic effects on both NK1 and NK2 receptors.
    WIN 66306
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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