tachykinin nk1 receptor

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.

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

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.

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.

Maropitant is a selective neurokinin (NK1) receptor antagonist.

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

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

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

[Sar9,Met(O2)11]-Substance P acetate is a tachykinin NK1 receptor selective agonist. [Sar9,Met(O2)11]-Substance P acetate is a selective tachykinin NK1 receptor agonist.[Sar9,Met(O2)11]-Substance P acetate and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissimilar time-course. Both agonists increase dose-dependently face washing and sniffing while [Sar9,Met(O2)11]-Substance P acetate is the sole to produce grooming.

tachykinin NK1 receptor antagonist

Potent and selective tachykinin NK2 receptor agonist (EC50 = 3.7 nM in rat colon). Displays > 1000- and > 300-fold selectivity over NK1 and NK3 receptors respectively. Active in vivo.

[Tyr6,D-Phe7,D-His9]-Substance P (6-11) is a tachykinin NK1 receptor antagonist that can counteract histamine-induced hyperalgesia.

TAK-637 is a tachykinin 1 (NK1) receptor antagonist.

Hemokinin 1, human TFA acts as a selective full agonist at the tachykinin neurokinin 1 (NK1) receptor, while also being a full agonist at NK2 and NK3 receptors. It is capable of inducing opioid-independent analgesia [1] [2].

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

Endogenous substance P homolog that is a selective agonist at the tachykinin NK1 receptor (IC50 values are 1.8, 370 and 480 nM for NK1, NK3 and NK2 receptors respectively). Has proliferative and antiapoptotic actions on B-cells in vitro and is antihyperte

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

CAM 4515 is a nonpeptide tachykinin NK1 receptor antagonist.

human tachykinin NK1 receptor antagonist

MEN 10207 is an antagonist of tachykinin.

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.

Tachykinin NK1 receptor antagonist.

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

Hemokinin 1 (human) acetate is an endogenous substance P homolog that is a selective agonist at the tachykinin NK1 receptor (IC50 values are 1.8, 370 and 480 nM for NK1, NK3 and NK2 receptors respectively). Has proliferative and antiapoptotic actions on B