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-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-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-182423
    RO5328673
    		Antagonist
    RO5328673 is an orally active, blood-brain barrier permeable neurokinin receptor antagonist that effectively targets human NK3 receptors (Ki=0.4 nM, Ka=0.1 nM), human NK2 receptors (Ki=1.1 nM, Ka=0.9 nM), and guinea pig NK3 receptors (Ka=0.1 nM and 0.13 nM). RO5328673 acts as an insurmountable antagonist of NK3 receptors with a slow dissociation rate, while it shows rapid association and dissociation rates at human NK2 receptors. RO5328673 potently inhibits senktide (HY-P0187)-induced enhancement of spontaneous activity in dopaminergic neurons and reverses senktide-induced changes in motor activity of gerbils. RO5328673 is widely applicable to research related to schizophrenia.
    RO5328673
  • 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-129448
    RO4583298
    		Antagonist
    RO4583298 is a potent, orally active dual antagonist of NK1 (human and gerbil)/NK3 (human, cynomolgus monkey, gerbil and guinea-pig). RO4583298 inhibits senktide-induced potentiation of spontaneous activity of dopaminergic neurons. RO4583298 can block gerbil foot tapping response and inhibits mouse tail whips.
    RO4583298
  • 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-19405
    UK-224671
    		Antagonist
    UK-224671 is a potent and selective NK2 receptor antagonist. UK-224671 is affected by P-gp efflux and poor intrinsic membrane permeability, resulting in low oral bioavailability.
    UK-224671
  • HY-10049
    CP 122721
    		Antagonist
    CP 122721 is an orally active NK1 receptor antagonist. CP 122721 attenuates cisplatin-induced vomiting in ferrets (ID50: 0.08 mg/kg). CP 122721 inhibits kainate (KA)-induced seizure activity and CA1 neuronal cell death in rats. CP 122721 is useful in the study of depression, asthma, and irritable bowel syndrome (IBS).
    CP 122721
  • HY-14406
    L-733060
    		Inhibitor
    L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 can be used for the study of chronic orofacial pain.
    L-733060
Cat. No. Product Name / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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