human nk1 receptor

Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

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.

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.

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.

N-Acetyl-L-tryptophan (N-acetyltryptophan) is an inhibitor of neurokinin 1 receptor (NK1-receptor, NK1R).

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

Fosnetupitant is a methylene phosphate prodrug of Netupitant. It has a pKi of 9.5 for the human NK1 receptor.

human tachykinin NK1 receptor antagonist

L-703,606 is a potent, selective human 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].

Fosnetupitant chloride monohydrochloride (Pro-netupitant chloride monohydrochloride) is a selective NK1 antagonist exhibiting high affinity for the human NK1 receptor with a pK i value of 9.5, and a lower affinity for the NK3 receptor with a pK i of 6.1. It serves as a methylene phosphate prodrug of Netupitant [1].

CP 122721 hydrochloride is a potent and selective non-peptide (nonpeptide) neurokinin NK1 antagonist, demonstrating a pIC50 of 9.8 against the human NK1 receptor in IM-9 cells. It exhibits anxiolytic and antidepressant-like effects, as evidenced in studies [1] [2].

Fosaprepitant-d4 Dimeglumine is a deuterated compound of Fosaprepitant Dimeglumine. Fosaprepitant Dimeglumine has a CAS number of 265121-04-8. Fosaprepitant Dimeglumine is the dimeglumine salt form of fosaprepitant, the water-soluble, N-phosphorylated prodrug of aprepitant, with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent binds selectively to the human substance P neurokinin 1 (NK1) receptors in the central nervous system (CNS). This inhibits receptor binding of the endogenous substance P and prevents substance P-induced emesis.

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.

Hemokinin 1 (mouse) is a selective excitogen 1 receptor agonist with Ki values of 0.175 nM for the human NK1 receptor and 560 nM for the human NK2 receptor.

Hemokinin 1 (mouse) acetate is a selective excitogen 1 receptor agonist with a Ki value of 0.175 nM for the human NK1 receptor and 560 nM for the human NK2 receptor.

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