Neurokinin Receptor
NK receptor; Tachykinin receptor
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
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Neurokinin Receptor Inhibitors
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Neurokinin Receptor Agonists
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Neurokinin Receptor Antagonists
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Neurokinin Receptor Activator
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Neurokinin Receptor Modulators
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Neurokinin Receptor Related Products (279)
Related Products (279)
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Antibodies (4)
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Neurokinin Receptor Isoform Comparison
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Substance P-Gly-Lys-Arg
0 ImagesCat. No.: HY-P3886CAS No.: 123148-51-6Substance P-Gly-Lys-Arg, also known as β-Preprotachykinin (58-71), is an analog of Substance P (HY-P0201).
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(D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P
0 ImagesCat. No.: HY-P3881CAS No.: 115760-58-2(D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P is a selective NK1 receptor antagonist.
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PD-161182
0 ImagesCat. No.: HY-117670CAS No.: 168570-35-2PD-161182 is a non-peptide NK-3 antagonist. PD-161182 can be studied in NK-3-related central nervous system disturbances, pain, inflammation, pulmonary and skin diseases.
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ASN-1377642
0 ImagesCat. No.: HY-131463CAS No.: 337505-63-2ASN-1377642 is a NK1 receptor antagonist with a Ki value of 251 nM. ASN-1377642 shows antitumor action in breast cancer cells with NK1R-Tr high expression.
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L-659877
0 ImagesCat. No.: HY-120522CAS No.: 125989-12-0Synonyms: Cyclo(Gln-Trp-Phe-Gly-Leu-Met)L-659877 (Cyclo(Gln-Trp-Phe-Gly-Leu-Met)) is a compound used to study the chemical properties of peptide fragments in collision-induced dissociation. A series of experiments were conducted to study the structural changes of b-fragment ions of different lengths in collision-induced dissociation.
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SCH 60057
0 ImagesCat. No.: HY-157743CAS No.: 203061-35-2SCH 60057 (Compound 7) is a neurokinin (NK) receptor inhibitor that can be isolated from Acremonium sp., with IC50 values of 6 μM and 12 μM for NK1 and NK2, respectively.
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FR 113680
0 ImagesCat. No.: HY-105436CAS No.: 126088-92-4FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.
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(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P acetate
0 ImagesCat. No.: HY-P3225CAS No.: 143077-65-0(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P (acetate) is an antagonist for Substance P (HY-P0201) and Bombesin (HY-P0195) that has effects on ocular inflammatory responses to antidromic trigeminal nerve stimulation.
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(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B
0 ImagesCat. No.: HY-P3850CAS No.: 109212-72-8(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B (Neurokinin Receptor) with a pA2 of 5.5. (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B shows no influence on Substance P or Neurokinin A.
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Substance P (3-11)
0 ImagesCat. No.: HY-P3895CAS No.: 51165-11-8Substance P (3-11) is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) has contracting activities on guinea pig ileum. Substance P (3-11) also promotes human monocyte chemotaxis .
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[Pro9]-Substance P
![[Pro9]-Substance P](https://file.medchemexpress.com/product_pic/hy-p2475.gif "Click to View [Pro9]-Substance P Product Detail")
0 ImagesCat. No.: HY-P2475CAS No.: 104486-69-3[Pro9]-Substance P is a potent, reversible and selective agonist of NK-1 tachykinin receptors with an EC50 of 0.93 nM.
![[Lys5,MeLeu9,Nle10]-NKA(4-10) TFA](https://file.medchemexpress.com/product_pic/hy-p1279a.gif "Click to View [Lys5,MeLeu9,Nle10]-NKA(4-10) TFA Product Detail")
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[Glp6] Substance P (6-11)
![[Glp6] Substance P (6-11)](https://file.medchemexpress.com/product_pic/hy-p3799.gif "Click to View [Glp6] Substance P (6-11) Product Detail")
0 ImagesCat. No.: HY-P3799CAS No.: 61123-13-5[Glp6] Substance P (6-11) is an analogue of substance P (6-11). Substance P (6-11) stimulates [3H]-inositol monophosphate ([3H]-IP1) formation in rat urinary bladder by acting on the 'septide-sensitive' tachykinin receptors.
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Imnopitant dihydrochloride
0 ImagesCat. No.: HY-109147ACAS No.: 290296-52-5Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist.
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[Gly11] Substance P
![[Gly11] Substance P](https://file.medchemexpress.com/product_pic/hy-p3922.gif "Click to View [Gly11] Substance P Product Detail")
0 ImagesCat. No.: HY-P3922[Gly11] Substance P is an analog of Substance P (HY-P0201). Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS.
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CP-99994
0 ImagesCat. No.: HY-12144CAS No.: 136982-36-0CP-99994 is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity.
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[Sar4] Substance P (4-11)
![[Sar4] Substance P (4-11)](https://file.medchemexpress.com/product_pic/hy-p3932.gif "Click to View [Sar4] Substance P (4-11) Product Detail")
0 ImagesCat. No.: HY-P3932[Sar4] Substance P (4-11) is an analog of Substance P (4-11). Substance P (4-11), the C-terminus fragment of Substance P (HY-P0201), is a Substance P agonist.
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Zalsenertant tetraxetan
0 ImagesCat. No.: HY-153709CAS No.: 1613265-38-5Synonyms: IPN-01087Zalsenertant tetraxetan (IPN-01087) is a DOTA-conjugated antagonist of the neurohypophyseal hormone receptor subtype 1 (NTSR1). Zalsenertant tetraxetan is labeled with the radioactive isotope Lu-177 (177Lu), which can be used for molecular imaging to identify potential responders. Zalsenertant tetraxetan can be used in the radiotherapy research of solid tumors.
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Benzomalvin C
0 ImagesCat. No.: HY-116620CAS No.: 157047-98-8Benzomalvin 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.
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CGP-49823
0 ImagesCat. No.: HY-19203CAS No.: 150705-88-7CGP-49823 is an orally active and highly selective antagonist of the neurokinin 1 receptor (NK1 receptor). CGP-49823‘s potency is significantly higher in isolated spinal cords of hamsters than in those of rats. CGP 49823 exhibits a significant anti-anxiety effect in social interaction experiments of rats, and its tolerance develops slowly, without causing anxiety-like withdrawal reactions after discontinuation. CGP-49823 can be used in anxiety and depression research.
