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
All Product Categories
-
Neurokinin Receptor Inhibitors
(21)
View all products
-
Neurokinin Receptor Agonists
(41)
View all products
-
Neurokinin Receptor Antagonists
(156)
View all products
-
Neurokinin Receptor Activator
(1)
View all products
-
Neurokinin Receptor Modulators
(7)
View all products
-
Neurokinin Receptor Controls
(3)
View all products
-
Neurokinin Receptor Related Products (276)
Related Products (276)
-
Antibodies (4)
-
Neurokinin Receptor Isoform Comparison
-
(1R,2S,3R)-Aprepitant
0 ImagesCat. No.: HY-172514CAS No.: 1185502-97-9(1R,2S,3R)-Aprepitant (Compound ent-4) is a competitive human neurokinin-1 (NK-1) receptor antagonist. (1R,2S,3R)-Aprepitant is promising for research of cancers and postoperative nausea and vomiting.
-
Maropitant citrate
0 ImagesCat. No.: HY-10053BCAS No.: 862543-54-2Maropitant citrate is an orally active NK1 receptor antagonist. Maropitant citrate prevents vomiting and inhibits ulcerative dermatitis.
-
YM-49598 iodide
0 ImagesCat. No.: HY-119005ACAS No.: 476494-44-7YM-49598 iodide is a tachykinin NK-1 receptor antagonist. YM-49598 iodide can inhibit drug-induced bladder contraction in rats, with IC50 of 11 μg/kg.
-
Osanetant monohydrochloride
0 ImagesCat. No.: HY-14551CCAS No.: 173050-51-6Synonyms: SR142801 monohydrochlorideOsanetant (SR142801) monohydrochloride is a selective NK3 receptor antagonist. Osanetant monohydrochloride produces anxiolytic- and antidepressant-like effects.
-
WS9326A
0 ImagesCat. No.: HY-N7574CAS No.: 125774-71-2WS9326A is a tachykinin receptor antagonist that can be isolated from Streptomyces violaceus.
-
Maropitant (Standard)
0 ImagesMaropitant (Standard) is the analytical standard of Maropitant. This product is intended for research and analytical applications. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting.
-
Pavinetant (Standard)
0 ImagesCat. No.: HY-14432RCAS No.: 941690-55-7Synonyms: MLE-4901 (Standard); AZD2624 (Standard); AZD4901 (Standard)Pavinetant (Standard) is the analytical standard of Pavinetant. This product is intended for research and analytical applications. Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
-
Elinzanetant-d3
0 ImagesCat. No.: HY-109171SSynonyms: NT-814-d3; BAY3427080-d3Elinzanetant-d3 (NT-814-d3) is deuterium labeled Elinzanetant. Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women.
-
SSR 146977 hydrochloride
0 ImagesCat. No.: HY-107693CAS No.: 264618-38-4SSR 146977 hydrochloride is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 hydrochloride can be used in the study of psychiatric disorders and airway inflammation.
-
(R)-Nolpitantium
0 ImagesCat. No.: HY-120308CAS No.: 154728-59-3Synonyms: SR140603(R)-Nolpitantium is the R-enantiomer of Nolpitantium (HY-108479). Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK1 receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation.
-
Vestipitant
0 ImagesCat. No.: HY-12140CAS No.: 334476-46-9Synonyms: GW597599Vestipitant (GW597599) is a neurokinin-1 receptor antagonist (pKi: 9.4, hNK1) with hypnotic effects and the ability to suppress primary insomnia. Vestipitant can effectively block substance P-mediated extracellular regulated kinase phosphorylation and relieve anxiety and possible depression induced by the agonist GR73632 (HY-P1192) in gerbils. Vestipitant can also improve functional dyspnea, anxiety, insomnia, irritable bowel disease, gastroesophageal reflux disease, tinnitus and antiemetic effects.
-
WIN 62577
0 ImagesCat. No.: HY-169501CAS No.: 138091-43-7WIN 62577 is a species-selective tachykinin NK1 receptor antagonist. WIN 62577 is also an allosteric enhancer with micromolar potency at M3 receptors. WIN 62577 exhibits potent antiviral activity against SARS-CoV-2.
-
Rolapitant (Standard)
0 ImagesSynonyms: SCH619734 (Standard)Rolapitant (Standard) is the analytical standard of Rolapitant. This product is intended for research and analytical applications. 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.
-
SB 218795 (Standard)
0 ImagesCat. No.: HY-107692RCAS No.: 174635-53-1SB 218795 (Standard) is the analytical standard of SB 218795 (HY-107692). This product is intended for research and analytical applications. SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit.
-
ZM 253270
0 ImagesCat. No.: HY-117053CAS No.: 169340-04-9ZM 253270 is a species-selective non-peptide NK-2 receptor (NK-2R) antagonist. ZM 253270 competitively inhibits the binding of [3H]NKA to native or cloned NK-2R from hamster bladder (Ki=2 nM), but has a weaker inhibitory effect (48-fold) on the binding of [3H]NKA to cloned human NK-2R.
-
L-732138 (Standard)
0 ImagesL-732138 (Standard) is the analytical standard of L-732138 (HY-101249). This product is intended for research and analytical applications. L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action.
-
ZD6021
0 ImagesCat. No.: HY-118378CAS No.: 255049-08-2ZD6021 is an orally active Neurokinin 1 Receptor antagonist, with Ki values of 0.12 nM for NK1 and 0.62 nM for NK2. At a concentration of 100 nM, ZD6021 has a pKB value of 8.9 for human pulmonary artery NK1 receptors, and a pKB value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasma protein extravasation in guinea pigs, with an ED50 of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED50 of 13 mg/kg.
-
Esmolol
0 ImagesCat. No.: HY-B1392ACAS No.: 81147-92-4Esmolol is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol attenuates post resuscitation myocardial dysfunction. Esmolol improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.
-
Netupitant (Standard)
0 ImagesCat. No.: HY-16346RCAS No.: 290297-26-6Synonyms: CID 6451149 (Standard)Netupitant (Standard) is the analytical standard of Netupitant. This product is intended for research and analytical applications. Netupitant (CID-6451149) is a highly potent, selective and orally active neurokinin-1 (NK1) receptor antagonist with a Ki of 0.95 nM for hNK1 in CHO cells. Netupitant has antiemetic affect.
-
SCH 206272
0 ImagesCat. No.: HY-116958CAS No.: 226915-43-1SCH 206272 is a selective antagonist of the tachykinin (NK) receptor. SCH 206272 inhibits binding at human tachykinin NK(1), NK(2), and NK(3) receptors (Ki = 1.3, 0.4, and 0.3 nM, respectively). SCH 206272 has an orally active.
