2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Neurokinin Receptor
  5. Neurokinin Receptor Antagonist

Neurokinin Receptor Antagonist

Neurokinin Receptor Isoform Comparison

Neurokinin Receptor Antagonists (154):

Cat. No. Product Name Effect Purity
  • 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-14407A
    Fosaprepitant dimeglumine
    		Antagonist 98.42%
    Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).
  • HY-16346
    Netupitant
    		Antagonist 99.90%
    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.
  • HY-14751
    Rolapitant
    		Antagonist 99.89%
    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.
  • HY-106910
    Saredutant
    		Antagonist 98.09%
    Saredutant is a selective NK2 receptor antagonist.
  • HY-109171
    Elinzanetant
    		Antagonist 99.82%
    Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause.
  • 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-14406A
    L-733060 hydrochloride
    		Antagonist 99.9%
    L-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 hydrochloride mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 hydrochloride blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 hydrochloride reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 hydrochloride can be used for the study of chronic orofacial pain.
  • HY-135108
    QWF Peptide
    		Antagonist 98.06%
    QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC50 of 4.7 μM.
  • HY-101249
    L-732138
    		Antagonist 99.9%
    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.
  • HY-14432
    Pavinetant
    		Antagonist 99.63%
    Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
  • 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-122347A
    Orvepitant maleate
    		Antagonist 99.99%
    Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment.
  • 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-107691
    GR 159897
    		Antagonist 99.60%
    GR 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.
  • HY-P0061
    Vapreotide
    		Antagonist 99.72%
    Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
  • HY-P1722
    Spantide II
    		Antagonist 99.47%
    Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis.
  • HY-117216B
    L-703606 oxalate hydrate
    		Antagonist 99.4%
    L-703606 oxalate hydrate is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.
  • HY-14405A
    Casopitant mesylate
    		Antagonist 99.83%
    Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of Substance P (HY-P0201). Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
  • HY-P1194
    Spantide I
    		Antagonist 99.64%
    Spantide 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.