tachykinin receptor

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.

Senktide is an agonist of tachykinin NK3 receptor.

Substance P (Neurokinin P) (SP) is an undecapeptide (a peptide composed of a chain of 11 amino acid residues) member of the tachykinin neuropeptide family.

MEN11467 is a novel, orally available, potent and selective peptidomimetic tachykinin NK 1 receptor antagonist for the study of acute colon cancer.

Vofopitant dihydrochloride (GR 205171A) is an orally available, selective tachykinin NK1 receptor antagonist that inhibits [3H]SP binding to NK1 with pKi values of 9.5 and 10.6, respectively. It is a potential compound for the treatment of pathological vomiting.

Befetupitant (Ro67-5930) is a potent and selective tachykinin 1 receptor (NK1R) antagonist for the study of corneal neovascularization.

Burapitant (SSR 240600) is a novel non-peptide tachykinin neurokinin 1 (NK) receptor antagonist with anti-coke oven and antidepressant activity.

Aprepitant is a Substance P Neurokinin-1 Receptor Antagonist. The mechanism of action of aprepitant is as a Neurokinin 1 Antagonist, and Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 2C9 Inducer, and Cytochrome P450 3A4 Inducer.

Netupitant (CID 6451149) is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM).

Maropitant is a selective neurokinin (NK1) receptor antagonist.

Fezolinetant (ESN-364) is a neurokinin-3 receptor antagonist that is being investigated for menopausal hot flashes.

gamma-preprotachykinin amide (72-92) acetate is a 21 amino acid peptide belonging to the tachykinin (TK) family and including neurokinin A (NKA) in its C-terminal sequence. gamma-preprotachykinin amide (72-92) acetate possesses higher affinity than NKA for central NK-2 receptors; it shows lower affinity for NK-1 receptors, however, it potently stimulates salivary secretion, which is mediated by NK-1 receptor activation.

Tachykinin antagonist 1 is an antagonist of neurokinin receptors.

CS-003 free base (CS-003) is a triple tachykinin receptor antagonist with high affinity for human (neurokinin) NK1, NK2 and NK3 receptors, with Ki values of 2.3 nM and 0.54 nM, respectively And 0.74 nM. CS-003 free base (CS-003) has therapeutic effects on

Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).

Men 10376 is a selective antagonist of tachykinin NK-2 receptor. It has a Ki of 4.4 μM for rat small intestine NK-2 receptor.

Ibodutant is an effective and selective tachykinin NK2 receptor antagonist (pKi: 10.1).

SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).

Tradipitant (VLY-686) is an antagonist of neurokinin-1.

Physalaemin acetate is a non-mammalian tachykinin with high affinity when binding selectively to neurokinin-1 (NK1) receptor.

YM-49598 iodide is a tachykinin NK-1 receptor antagonist. It inhibits drug-induced bladder contractions in rats with an IC50 of 11 μg kg.

L 659,877 is an antagonist of the Tachykinin and neurokinin-2 receptor.

Spantide antagonizes both bombesin & substance P. It is also tachykinin receptor antagonist.

WIN 62577 is a species-selective tachykinin NK1 receptor antagonist and also serves as an allosteric enhancer with micromolar potency at M3 receptors. Additionally, WIN 62577 demonstrates potent antiviral activity against SARS-CoV-2.