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 Controls
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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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SDZ NKT 343
0 ImagesCat. No.: HY-108480CAS No.: 180046-99-5SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity.
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Ranakinin
0 ImagesCat. No.: HY-P2139CAS No.: 139446-71-2Ranakinin is a NK1R agonist. Ranakinin inhibits the binding of selective NK1 radioligands to NK1 receptors. Ranakinin activates phospholipase C (Phospholipase C), thereby enhancing polyphosphoinositide hydrolysis. Ranakinin stimulates inositol phosphate production and reduces membrane polyphosphoinositide levels. Ranakinin stimulates corticosterone and aldosterone secretion.
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CS-003 Free base
0 ImagesCat. No.: HY-19633CAS No.: 191672-52-3CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.
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(Trp7,β-Ala8)-Neurokinin A (4-10)
0 ImagesCat. No.: HY-P4709CAS No.: 132041-95-3(Trp7,β-Ala8)-Neurokinin A (4-10) is a potent neurokinin-3 (NK3) antagonist.
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Scyliorhinin I
0 ImagesCat. No.: HY-P10599CAS No.: 103425-21-4Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guinea pig ileum.
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Benzomalvin B
0 ImagesCat. No.: HY-114673CAS No.: 157047-97-7Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P.
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SCH 900978
0 ImagesCat. No.: HY-106659CAS No.: 873947-10-5Synonyms: NK-1 Antagonist 1SCH 900978 (NK-1 Antagonist 1) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression.
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MDL 105212A
0 ImagesCat. No.: HY-105462CAS No.: 167261-60-1MDL 105212A is a potent and orally active nonpeptide neurokinin receptor (NK-1/NK-2) tachykinin receptor antagonist. MDL 105212A can be used for the researches of inflammation, immunology and neurological disease, such as asthma.
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[D-Trp2,7,9] Substance P
![[D-Trp2,7,9] Substance P](https://file.medchemexpress.com/product_pic/hy-p3802.gif "Click to View [D-Trp2,7,9] Substance P Product Detail")
0 ImagesCat. No.: HY-P3802CAS No.: 100930-11-8[D-Trp2,7,9] Substance P is a tachykinin (Neurokinin Receptor) antagonist with Ki values of 1 μM, 1.3 μM, and ~9 μM for NK-1, NK-2,and NK-3 receptor, respectively.
![[S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10)](https://file.medchemexpress.com/product_pic/hy-p11312.gif "Click to View [S5K, F6Y, L9mL, M10Mox] neurokinin A (4-10) Product Detail")
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SSR-241586
0 ImagesCat. No.: HY-19456CAS No.: 1239279-30-1SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).
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Eprazinone
0 ImagesCat. No.: HY-B2078CAS No.: 10402-90-1Eprazinone can enhance lung function and arterial oxygen levels and can be used in the study of chronic bronchitis. Higher doses of eprazinone increased phospholipid levels and decreased neutral lipid content in bronchoalveolar lavage (BAL) fluid, but had no effect on protein and cell levels in BAL. Eprazinone dose-dependently reduced short-circuit current (Isc), primarily by reducing chloride secretion at lower concentrations and affecting sodium and chloride transport at higher doses. Eprazinone may exert its anti-inflammatory effects by regulating BAL lipid composition and airway ion transport.
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CP-99994 hydrochloride
0 ImagesCat. No.: HY-12145CAS No.: 145148-39-6CP-99994 hydrochloride is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 hydrochloride prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 hydrochloride 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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Grexenetant
0 ImagesCat. No.: HY-187871CAS No.: 2854332-29-7Grexenetant (compound I) is a NK-3 receptor antagonist. Grexenetant can be used in the research of diseases mediated by NK-3 receptors, such as depression, anxiety, psychosis, schizophrenia, psychotic disorders, bipolar disorder, cognitive impairment, Parkinson's disease, Alzheimer's disease, attention deficit hyperactivity disorder, pain, convulsions, obesity, inflammatory diseases, vomiting, preeclampsia, airway-related diseases, reproductive disorders, sex hormone-dependent diseases, gynecological diseases, and menopausal syndrome.
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Rolapitant-d4
0 ImagesCat. No.: HY-14751SSynonyms: SCH619734-d4Rolapitant-d4 (SCH619734-d4) is the deuterated-labeled Rolapitant (HY-14751). Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model.
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Fosnetupitant-d6 dihydrochloride
0 ImagesCat. No.: HY-W758677ASynonyms: Pronetupitant-d6 dihydrochlorideFosnetupitant-d6 dihydrochloride (Pronetupitant-d6 dihydrochloride) is the deuterium labeled Fosnetupitant dihydrochloride (HY-W758677A). Fosnetupitant (Pronetupitant) a methylene phosphate proagent of Netupitant. Fosnetupitant (Pronetupitant) exhibits a pKi of 9.5 for human NK1 receptor.
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MDL 29913
0 ImagesCat. No.: HY-P1017CAS No.: 135721-56-1MDL 29913, a cyclic pseudopeptide, is a competitive NK2 tachykinin receptor selective antagonist, with a pA2 of 8.66.
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GR 64349 acetate
0 ImagesCat. No.: HY-P1278BGR 64349 acetate is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 acetate selectively activates the NK-2 receptor subtype. GR 64349 acetate activates tonic and rhythmic bladder contractions of the micturition reflex. GR 64349 acetate does not inhibit rhythmic bladder contraction activation induced by normal saline. GR 64349 acetate induces inward currents.
