Neurokinin Receptor Antagonist

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).

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.

QWF Peptide is a substance P (SP) antagonist. QWF Peptide inhibits SP-induced biological responses and also suppresses SP-induced contraction of isolated guinea pig tracheal strips. QWF Peptide can be used for asthma-related research.

L-703606 oxalate hydrate is a potent, selective antagonist of NK1 receptor. L-703606 can be used for study of gastric acid secretion.

Tradipitant (VLY-686) is a neurokinin-1 (NK-1) antagonist.

Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a K_i of 4.4 μM for rat small intestine NK-2 receptor.

RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a K_i value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation.

Octahydroisoindole (Perhydroisoindole) is a substance P antagonist that can cross the blood-brain barrier and is useful for the study of movement disorders associated with central nervous system diseases.

Fosaprepitant (L-785298) is a proagent of Aprepitant (HY-10052). Fosaprepitant is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).

Y1 receptor antagonist 1 (H 409-22 isomer) (Example 4) is a neuropeptide Y1 receptor antagonist. Y1 receptor antagonist 1 can be used for the study of cardiovascular diseases, such as vasoconstriction.

Netupitant-d₆ is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist.

Spantide I TFA, a substance P analog, is a selective NK₁ receptor antagonist, with K_i 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.

WIN 66306 is a cyclic heptapeptide that can be isolated from an Aspergillus species. WIN 66306 is a neurokinin antagonist with antagonistic effects on both NK1 and NK2 receptors.

GR 94800 is a potent and selective NK₂ receptor peptide antagonist, with pK_B values of 9.6, 6.4 and 6.0 for NK₂, NK₁ and NK₃ receptors, respectively.

Substance P Receptor Antagonist 1 has the potential function in central nervous system disorders, respiratory, inflammatory diseases and gastrointestinal disorders.

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.

Y1 receptor antagonist 1 (H 409-22 isomer) formic (Example 4) is a neuropeptide Y1 receptor antagonist. Y1 receptor antagonist 1 can be used for the study of cardiovascular diseases, such as vasoconstriction.

WIN 51708 is a nonpeptide antagonist of neurokinin (NK)-1 receptor. WIN 51708 has a higher affinity for the rat NK-1 receptor compared to the human NK-1 receptor.

Orvepitant (GW823296) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pK_i of 10.2 for human neurokinin-1 receptor. Orvepitant can across the blood-brain barrier. Orvepitant has the potential for depressive disorder and chronic refractory cough (CRC) treatment.

Substance P(1-4) is a potent neurokinin receptors (NK-R) antagonist. Substance P(1-4) has regulation of normal hematopoiesis and inhibits endogenous erythroid colony (EEC) formation.