Tachykinin 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.

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

Maropitant is a selective neurokinin (NK1) receptor antagonist.

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

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

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.

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.

SB 218795 is an effective and selective antagonist of NK3 with a Ki 13 nM for hNK3 which is about 90-fold and 7000-fold selectivity over hNK2 and hNK1.

Eprazinone dihydrochloride (NSC 317935) is a mucolytic with antitussive and mucolytic effect.

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(1-7) (Substance P 1-7) is the major bioactive metabolite formed after proteolytic degradation of the tachykinin substance P (SP),with anti-inflammatory, anti-nociceptive and anti-hyperalgesic effects

Talnetant (SB 223412) is a selective, competitive NK3 receptor antagonist that penetrates the brain and modulates mesolimbic and mesocortical dopaminergic neurotransmission.

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

Neurokinin A(4-10)(TFA) is an agonist of tachykinin NK2 receptor .

Eledoisin Related Peptide (Eledoisin RP) is a tachykinin receptor ligand.

Senktide is an agonist of tachykinin NK3 receptor.

[Sar9,Met(O2)11]-Substance P (NA) is an NK1 receptor agonist.

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

Neurokinin A (NKA), formerly known as Substance K, is a neurologically active peptide translated from the pre-protachykinin gene.

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.

Potent and selective tachykinin NK1 receptor agonist (EC50 = 2 nM in guinea pig vas deferens).

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).