nk1 antagonist 1

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

Ezlopitant (CJ-11974) is a small molecule neurokinin-1-receptor (NK1) antagonist used to treat nausea, vomiting and pain.

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

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting, and orally active neurokinin 1 (NK1) receptor antagonist with a K_i of 0.66 nM, which does not interact with CYP3A4 and demonstrates potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].

Casopitant mesylate (GW679769B) is a selective, brain-permeable, and orally active antagonist of the neurokinin 1 (NK1) receptor, and it is the second in its class of antiemetics.

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

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

Fosrolapitant is an antagonist of the neurokinin 1 (NK1) receptor.

Casopitant (GW679769) is an orally active neurokinin-1 (NK1) receptor antagonist, researched for its potential use in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).

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

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.

Benzomalvin B is a fungal metabolite originally isolated from Penicillium. It acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P by 24% in vitro when used at a concentration of 100 μg/ml.

Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor, inhibiting binding of substance P by 46% at 100 μg ml in vitro, and a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. Isolated from Penicillium, it contains an epoxide group at C-19 and C-20, absent in benzomalvins A, B, or E.

Rolapitant Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity.

Rolapitant, also known as SCH-619734, is 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.

Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extrava......

Acetylaszonalenin is a fungal metabolite that has been found in A. flavipes.1 It acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P with a Ki value of 170 μM.

WIN 66306 is a cyclic heptapeptide antagonist of neurokinin-1 (NK1) and NK2 receptors originally isolated from A. flavipes. It binds to NK1 and NK2 receptors and inhibits contractions induced by substance P in isolated guinea pig ileum in a concentration-dependent manner.

Imnopitant dihydrochloride, a neurokinin NK1 receptor antagonist [1].

Spantide I TFA, a selective NK1 receptor antagonist and a substance P analog, exhibits K(i) values of 230 nM for NK1 and 8150 nM for NK2 receptors, respectively. It offers a method to decrease type 1 while increasing type 2 cytokine IL-10 in the infected cornea, significantly reducing corneal perforation [1] [2] [3].

GR 94800 TFA is a potent, selective antagonist of the NK 2 receptor peptide, demonstrating pK B values of 9.6 for NK 2, 6.4 for NK 1, and 6.0 for NK 3 receptors, respectively [1] [2].

GR 64349 is a potent and highly selective NK2 receptor peptide antagonist with an EC50 of 3.7 nM in rat colon, exhibiting over 1000-fold selectivity against NK1 receptors and over 300-fold selectivity against NK3 receptors, ensuring targeted action [1] [2].

[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) is a potent neurokinin NK1 antagonist that effectively inhibits the actions of gold-protein-substance P (GPSP) and substance P (SP), demonstrating its efficacy in neutralizing their effects [1].

(D-Arg1, D-Pro2, D-Phe7, D-His9)-Substance P is a selective NK1 receptor antagonist [1].