NK3R
NK3R (neurokinin-3 receptor), encoded by TACR3, is a class A G protein-coupled receptor of the tachykinin receptor family that preferentially binds the endogenous neuropeptide neurokinin B (NKB) and mediates neuroendocrine signaling in the central nervous system and hypothalamus[1][2]. Mechanistically, NKB-NK3R signaling contributes to the regulation of gonadotropin-releasing hormone (GnRH) secretion and reproductive axis activity, establishing NK3R as a key component of central reproductive control pathways[3][4]. Studies of patients carrying loss-of-function TAC3 or TACR3 mutations demonstrated that disruption of this pathway causes normosmic congenital hypogonadotropic hypogonadism and revealed an essential physiological role for NK3R in pubertal development and gonadotropin regulation[3][5]. In disease-associated neuroendocrine phenotypes, impaired NK3R signaling is linked to reduced GnRH pulse frequency, altered luteinizing hormone secretion, and elevated FSH/LH ratios, providing clinically relevant experimental markers for pathway dysfunction[5]. Compared with the related tachykinin receptors NK1R and NK2R, NK3R exhibits the highest affinity for NKB and therefore mediates distinct biological functions within tachykinin signaling networks[1][2]. For experimental applications, selective NK3R agonists such as senktide and selective antagonists including talnetant, osanetant, pavinetant, and fezolinetant have been widely used to investigate receptor pharmacology, neuroendocrine regulation, and therapeutic modulation of NKB-dependent signaling pathways[1][6].
References:
- [1]. Sun W, et al. Structural insights into neurokinin 3 receptor activation by endogenous and analogue peptide agonists. Cell Discov. 2023 Jun 30;9(1):66. [Content Brief]
- [2]. Zhang WW, et al. Tacr3/NK3R: Beyond Their Roles in Reproduction. ACS Chem Neurosci. 2020 Oct 7;11(19):2935-2943. [Content Brief]
- [3]. Topaloglu AK, et al. TAC3 and TACR3 mutations in familial hypogonadotropic hypogonadism reveal a key role for Neurokinin B in the central control of reproduction. Nat Genet. 2009 Mar;41(3):354-358. [Content Brief]
- [4]. Zhang C, et al. 17 β-estradiol rapidly increases ATP-sensitive potassium channel activity in gonadotropin-releasing hormone neurons [corrected] via a protein kinase signaling pathway. Endocrinology. 2010 Sep;151(9):4477-84. [Content Brief]
- [5]. Francou B, et al. Normosmic congenital hypogonadotropic hypogonadism due to TAC3/TACR3 mutations: characterization of neuroendocrine phenotypes and novel mutations. PLoS One. 2011;6(10):e25614. [Content Brief]
- [6]. Wikipedia.
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NK3R Related Products (32)
Related Products (32)
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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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[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.
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NK3R-IN-2
0 ImagesCat. No.: HY-176546NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM for human NK3R. NK3R-IN-2 can pass through the blood-brain barrier. NK3R-IN-2 has excellent NK3R binding affinity (IC50 = 87.31 nM) in CHO-K1 cells. NK3R-IN-2 effectively inhibits the level of luteinizing hormone (LH). NK3R-IN-2 can be used for research on hormone related conditions.
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Senktide TFA
0 ImagesCat. No.: HY-W755425Senktide TFA is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50=0.5-3 nM). Senktide TFA less potently agonizes the NK1 receptor (EC50=35 µM). Senktide TFA is promising for research of neurological disease.
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SB 414240
0 ImagesCat. No.: HY-122286CAS No.: 272104-60-6SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with Kis of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease.
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SSR 146977
0 ImagesCat. No.: HY-116822CAS No.: 264618-44-2SSR 146977 is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 inhibits the binding of radioactive neurokinin B to NK3 receptors in Chinese hamster ovary cells, with a Ki of 0.26 nM.
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[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10)
![[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10)](https://file.medchemexpress.com/product_pic/hy-p11075.gif "Click to View [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) Product Detail")
0 ImagesCat. No.: HY-P11075CAS No.: 2770688-04-3[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) is a selective NK2R agonist with an EC50 of 3.7 nM for hNK2R. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) significantly inhibits weight loss in diet-induced obese (DIO) mice model and improves Loperamide (HY-156131)-induced dysfunctional voiding in wild-type mice. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) can be used for neurokinin receptor mediated disorders, such as obesity, insulin resistance and type 2 diabetes research.
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GSK256471
0 ImagesCat. No.: HY-116268CAS No.: 1133706-08-7GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB) (HY-P0242)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia.
![[Asp5,6,Me-Phe8] Substance P (5-11)](https://file.medchemexpress.com/product_pic/hy-p11429.gif "Click to View [Asp5,6,Me-Phe8] Substance P (5-11) Product Detail")
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GSK172981
0 ImagesCat. No.: HY-121164CAS No.: 1133705-99-3GSK172981 is a brain-penetrant tachykinin NK3 receptor antagonist with pKi values of 7.7 and 7.8 for human and native guinea pig NK3 receptors, respectively. GSK172981 can be used for the study of schizophrenia.
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WIN-64821
0 ImagesCat. No.: HY-N9554CAS No.: 150881-27-9WIN-64821 is a secondary metabolite produced by Aspergillus species, and acts as a Neurokinin Receptor antagonist. The Ki values of WIN-64821 for NK1, NK2 and NK3 receptors are 0.24 (human astrocytoma cells), 0.26 (rat duodenum) and 15.2 (guinea pig forebrain) μM, respectively. WIN-64821 inhibits apamin-induced contraction of rat vas deferens, blocks substance P-induced contraction of guinea pig ileum and Ca2+ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research.
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Talnetant hydrochloride
0 ImagesCat. No.: HY-14552ACAS No.: 204519-66-4Synonyms: SB 223412 hydrochloride; SB 223412-ATalnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies.
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