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  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. Nombre del producto Efecto Pureza Chemical Structure
  • 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-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
Cat. No. Nombre del producto / Synonyms Application Reactivity
Neurokinin Receptor Isoform Comparison

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