NK2R
Neurokinin receptor NK2R, encoded by TACR2, is a tachykinin G protein-coupled receptor cloned from human tracheal and gastric tissues and primarily activated by neurokinin A[1]. Mechanistically, NK2R signaling supports smooth muscle contractility, epithelial secretion, inflammation, and nociception within gastrointestinal, respiratory, urogenital, immune, and nervous systems[2]. In human colon models, NK2 tachykinin receptors play a dominant role in circular muscle contraction and modulate motor responses in colonic muscle strips[3][4]. In airway models, NK2 receptors mediate airway smooth muscle contraction, especially in human bronchi, and contribute to antigen- or PAF-associated bronchospasm and airway hyperresponsiveness[5][6]. Compared with related isoforms, NK1R preferentially responds to substance P, NK2R to neurokinin A, and NK3R to neurokinin B, which supports isoform-specific ligand selection in receptor studies[2]. For experimental applications, NK2R antagonists such as MEN10,627 and nepadutant provide selective tools for testing NK2R-dependent gastrointestinal motility and bronchoconstriction mechanisms[6][7].
References:
- [1]. Gerard NP, et al. The human neurokinin A (substance K) receptor: molecular cloning of the gene, chromosome localization, and isolation of cDNA from tracheal and gastric tissues. J Biol Chem. 1990;265(33):20455-20462.
- [2]. Steinhoff MS, et al. Tachykinins and their receptors: contributions to physiological control and the mechanisms of disease. Physiol Rev. 2014 Jan;94(1):265-301. [Content Brief]
- [3]. Giuliani S, et al. NK2 tachykinin receptors and contraction of circular muscle of the human colon: characterization of the NK2 receptor subtype. Eur J Pharmacol. 1991;203(3):365-70. [Content Brief]
- [4]. Croci T, et al. In vitro characterization of tachykinin NK2-receptors modulating motor responses of human colonic muscle strips. Br J Pharmacol. 1998 Jul;124(6):1321-7. [Content Brief]
- [5]. Advenier C. Tachykinin NK2 receptors further characterized in the lung with nonpeptide receptor antagonists. Can J Physiol Pharmacol. 1995 Jul;73(7):878-84. doi: 10.1139/y95-121. PMID: 8846425. et al. Tachykinin NK2 receptors further characterized in the lung with nonpeptide receptor antagonists. Can J Physiol Pharmacol. 1995 Jul;73(7):878-84. [Content Brief]
- [6]. Perretti F, et al. Antibronchospastic activity of MEN10,627, a novel tachykinin NK2 receptor antagonist, in guinea-pig airways. Eur J Pharmacol. 1995 Jan 24;273(1-2):129-35. [Content Brief]
- [7]. Catalioto RM, et al. MEN 11420 (Nepadutant), a novel glycosylated bicyclic peptide tachykinin NK2 receptor antagonist. Br J Pharmacol. 1998 Jan;123(1):81-91. [Content Brief]
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NK2R Related Products (32)
Related Products (32)
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EB1002
0 ImagesEB1002 is a highly selective, long-acting NK2R agonist. EB1002 exerts central appetite suppression, increases peripheral energy expenditure and enhances insulin sensitivity, which effectively reduces body weight, improves glucose and lipid metabolism, with favorable safety profiles. EB1002 can be used for research on diseases such as obesity and type 2 diabetes.
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Fmoc-Dap(Boc)-OH
0 ImagesFmoc-Dap (Boc)-OH is an amino acid derivative bearing the Fmoc protecting group. Fmoc-Dap (Boc)-OH supports Fmoc-based solid-phase peptide synthesis for the preparation of bicyclic tachykinin NK2 receptor antagonists.
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Saredutant
0 ImagesSynonyms: SR 48968; SR 48968CSaredutant is a selective NK2 receptor antagonist.
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GR 159897
0 ImagesGR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
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L-659874
0 ImagesCat. No.: HY-P2593CAS No.: 125989-15-3L-659874 is a selective NK2 receptor antagonist with an IC50 value of 0.49 μM in hamsters. L-659874 inhibits NK2 receptor-mediated hydrolysis of inositol phospholipids. L-659874 could be used for research on the correlation between pain signal transduction and smooth muscle responses.
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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.
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RO5328673
0 ImagesCat. No.: HY-182423CAS No.: 1310817-94-7RO5328673 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.
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[Lys5,MeLeu9,Nle10]Neurokinin A(4-10)
![[Lys5,MeLeu9,Nle10]Neurokinin A(4-10)](https://file.medchemexpress.com/product_pic/hy-p3849.gif "Click to View [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) Product Detail")
0 ImagesSynonyms: LMN-NKA[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues.
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GR 64349
0 ImagesGR 64349 is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 selectively activates the NK-2 receptor subtype. GR 64349 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 induces inward currents.
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Spantide I
0 ImagesSpantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
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MEN 10207
0 ImagesMEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
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Hemokinin 1, human
0 ImagesHemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia.
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γ-Neuropeptide (rabbit)
0 Imagesγ-Neuropeptide (rabbit) can be isolated from rabbit intestine. γ-Neuropeptide is an endogenous neurokinin peptide that acts as a neurokinin 2 (NK2) receptor agonist. γ-Neuropeptide mediates hypothalamic-pituitary-adrenal (HPA) axis, as well as reproductive hormone release.
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SB 218795
0 ImagesSB 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.
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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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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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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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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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