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

Neurokinin Receptor Antagonist

Neurokinin Receptor Antagonists (83):

Cat. No. Product Name Effect Purity
  • HY-14770
    Ibodutant
    Antagonist
    Ibodutant (MEN 15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1.
  • HY-19665
    Lanepitant
    Antagonist
    Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis.
  • HY-105534
    TAK-637
    Antagonist
    TAK-637 is an orally active neurokinin-1 receptor antagonist. TAK-637 increases bladder storage capacity. TAK-637 can be used for research of functional bowel diseases such as irritable bowel syndrome.
  • HY-117216A
    L-703606 oxalate
    Antagonist
    L-703606 oxalate is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.
  • HY-10053S1
    Maropitant-13C,d3
    Antagonist
    Maropitant-13C,d3 is the 13C- and deuterium labeled Maropitant. 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[1][2].
  • HY-105215
    FK888
    Antagonist
    FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration.
  • HY-14405
    Casopitant
    Antagonist
    Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
  • HY-P1277
    GR 94800
    Antagonist
    GR 94800 is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively.
  • HY-120928
    S 16474
    Antagonist
    S 16474 is a cyclic peptide with antagonistic effects on NK1 and NK2 receptors. S 16474 can be used in the study of neurogenic inflammation.
  • HY-120522
    L-659877
    Antagonist
    L-659877 (Cyclo(Gln-Trp-Phe-Gly-Leu-Met)) is a compound used to study the chemical properties of peptide fragments in collision-induced dissociation. A series of experiments were conducted to study the structural changes of b-fragment ions of different lengths in collision-induced dissociation.
  • HY-105436
    FR 113680
    Antagonist
    FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.
  • HY-P3225
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P acetate
    Antagonist
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P (acetate) is an antagonist for Substance P (HY-P0201) and Bombesin (HY-P0195) that has effects on ocular inflammatory responses to antidromic trigeminal nerve stimulation.
  • HY-P3850
    (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B
    Antagonist
    (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B (Neurokinin Receptor) with a pA2 of 5.5. (D-Pro2,D-Trp6,8,Nle10)-Neurokinin B shows no influence on Substance P or Neurokinin A.
  • HY-109147A
    Imnopitant dihydrochloride
    Antagonist
    Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist.
  • HY-117380
    SB 235375
    Antagonist
    SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models.
  • HY-101704A
    Y1 receptor antagonist 1 formic
    Antagonist 99.84%
    Y1 receptor antagonist 1 formic (H 409-22 isomer formic) is the formic salt form of Y1 receptor antagonist 1 (HY-101704). Y1 receptor antagonist 1 formic is a neuropeptide Y1 receptor antagonist.
  • HY-12142S
    rac-Vofopitant-d3
    Antagonist
    rac-Vofopitant-d3 (rac-GR 205171-d3) is the deuterium labeled Vofopitant (HY-12142). Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.
  • HY-120167
    YM-44778
    Antagonist
    YM-44778 is a neurokinin receptor antagonist. The pKi values for NK1, NK2 and NK3 are 8.08, 8.55 and 8.24, respectively. YM-44778 inhibits the increase of bladder pressure induced by substance [Sar9,Met(O2)11] -P (HY-P1012) in anestheticized rats.
  • HY-P3880
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P
    Antagonist
    (D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P is a neuropeptide Substance P (HY-P0201) antagonist.
  • HY-P3808
    [D-Pro2,D-Trp7,9] Substance P
    Antagonist
    [D-Pro2,D-Trp7,9] Substance P, a Substance P (HY-P0201) analogue, is a weak agonist and a potent, specific, competitive Substance P antagonist.