nk receptor

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.

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

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.

Rolapitant (SCH619734) Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life.

Elinzanetant is a dual antagonist of neurokinin (NK) receptors 1 and 3 and modulates reproductive hormone secretion.

Substance P (7-11) (Substance P 7-11(TFA)) is a C-terminal fragment of Substance P .

Senktide is an agonist of tachykinin NK3 receptor.

L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM)

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.

Highy selective and potent NK2 receptor agonist (IC50 = 6.1 nM). Induces contraction of the rat fundus and bladder (EC50 values are 117 and 10 nM respectively).

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

Bisaramil hydrochloride (Bisaramil) is a novel diazabicyclononane antiarrhythmic compound that inhibits the generation of free radicals.Bisaramil hydrochloride blocks sodium currents and inhibits the slow Ca(2+) action potential induced by isoproterenol in K(+)-depolarized muscle.

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

NKP608 is a selective and highly effective neurokinin-1 (NK-1) receptor antagonist with anticancer and antianxiety activities, inhibiting the proliferation of human colorectal cancer cells through the Wnt signaling pathway.

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.

Toremifene (GTx 006) is a selective estrogen-receptor modulator (SERM).

NK-1 Antagonist 1 is a NK-1 receptor antagonist.

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.

Orvepitant maleate is an effective, selective, and well-tolerated neurokinin-1 receptor (NK-1) antagonist (pKi: 10.2 for human neurokinin-1 receptor). Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatmen

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.