2. シグナル伝達
  3. GPCR/G Protein
    Neuronal Signaling
  4. Neurokinin Receptor
  5. NK3R Isoform

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].

NK3R 関連製品 (29):

製品番号 製品名 製品効果 純度
  • HY-P0187
    Senktide Agonist 99.91%
    Senktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50=0.5-3 nM). Senktide less potently agonizes the NK1 receptor (EC50=35 µM). Senktide is promising for research of neurological disease.
  • HY-19632
    Fezolinetant Antagonist 99.19%
    Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
  • HY-15722
    SB-222200 Antagonist 99.85%
    SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders.
  • HY-14552
    Talnetant Antagonist 99.38%
    Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies.
  • HY-14432
    Pavinetant Antagonist 99.63%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
  • HY-181682
    NK3R antagonist-1 Antagonist
    NK3R antagonist-1 is an orally active neurokinin-3 receptor (NK3R) antagonist with an IC50 of 53.61 nM. NK3R antagonist-1 reduces plasma luteinizing hormone (LH) levels in ovariectomized rat models. NK3R antagonist-1 is applicable to research related to menopausal hot flushes.
  • HY-182423
    RO5328673 Antagonist
    RO5328673 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.
  • HY-14551
    Osanetant Antagonist 98.19%
    Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia.
  • HY-P0006
    Eledoisin 99.06%
    Eledoisin (Eledone peptide) is a specific agonist of NK2 and NK3 receptors.
  • HY-151413
    MEN 10207 Antagonist 99.80%
    MEN 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.
  • HY-P3862
    [MePhe7]-Neurokinin B Inhibitor 98.76%
    [MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC50 value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R).
  • HY-133206A
    Fosnetupitant chloride monohydrochloride Antagonist 99.70%
    Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pKi values of 9.5, 6.1 for human NK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant.
  • HY-P1198
    Hemokinin 1, human Agonist 98.11%
    Hemokinin 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.
  • HY-107692
    SB 218795 Antagonist 99.86%
    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.
  • HY-108480
    SDZ NKT 343 Antagonist
    SDZ 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.
  • HY-P1198A
    Hemokinin 1, human TFA Agonist
    Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia.
  • HY-19633
    CS-003 Free base Antagonist
    CS-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.
  • HY-P4709
    (Trp7,β-Ala8)-Neurokinin A (4-10) Antagonist
    (Trp7,β-Ala8)-Neurokinin A (4-10) is a potent neurokinin-3 (NK3) antagonist.
  • HY-P3802
    [D-Trp2,7,9] Substance P Antagonist
    [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.
  • HY-176546
    NK3R-IN-2 Inhibitor
    NK3R-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.