nk-1 receptor

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

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.

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

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.

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

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

Tradipitant (VLY-686) is an antagonist of neurokinin-1.

YM-49598 iodide is a tachykinin NK-1 receptor antagonist. It inhibits drug-induced bladder contractions in rats with an IC50 of 11 μg kg.

SCH 206272 is a potent, orally active antagonist of tachykinin NK(1), NK(2), and NK(3) receptor.

YM44781 is a non-peptide tachykinin receptor antagonist. YM44781 exhibits high binding affinities at NK(1) (pK(i) = 9.09 + - 0.02) and NK(2) (pK(i) = 9.94 + - 0.03) receptors, respectively.

YM49598 is a tachykinin receptor antagonist. YM49598 exhibited high binding affinities at NK(1) (pK(i) = 9.09 +/- 0.02) and NK(2) (pK(i) = 9.94 +/- 0.03) receptors, respectively. YM49598 was almost inactive but produced a potent inhibition (IC(50) = 11 +/

D-Lysine lactam is a chiral building block.1,2It has been used in the synthesis of a chiral antibiotic synthetic intermediate, as well as in the stereoselective synthesis of neurokinin (NK) receptor antagonists. 1.Kumar, A., Bhashkar, B., Bhavsar, J., et al.Catalytic reduction: Efficient synthesis of chiral key intermediate of besifloxacin hydrochlorideDer Pharma Chemica7(9)297-3000(2015) 2.Gerspacher, M., Lewis, C., Ball, H.A., et al.Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonistJ. Med. Chem.46(16)3508-3513(2003)

Ganglioside GM1 asialo is a component of cellular lipid rafts and can be formed by the cleavage of the sialic acid residue from ganglioside GM1 by neuraminidase. Ganglioside GM1 asialo is a glycolipid receptor for P. aeruginosa flagellin and stimulates defensive responses in host cells, including extracellular ATP release, calcium mobilization, and ERK1/2 phosphorylation when stimulated by flagellin and an anti-ganglioside GM1 asialo antibody. The percentage of ganglioside GM1 asialo-positive natural killer (NK) and CD8+ T cells in lung is increased in a mouse model of respiratory syncytial virus (RSV) infection compared with healthy animals. Depletion of ganglioside GM1 asialo-positive NK and T cells reduces IFN-γ levels in the lung, reduces weight loss, and increases lung viral load in RSV-infected mice. Ganglioside GM1 asialo mixture contains ganglioside GM1 asialo molecular species with C18:1 and C20:1 sphingoid backbones.

Serlopitant is a selective antagonist of Neurokinin-1 (NK-1) receptor.

Vestipitant mesylate is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia.

Vestipitant, also known as GW597599, is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia.

MDL-105212A HCl is a nonpeptide NK-1 and NK-2 receptor antagonist.

(R)-Casopitant ((R)-GW679769), an isomer of Casopitant, functions as an NK(1)-receptor antagonist and is used in the study of chemotherapy-induced nausea and vomiting [1] [2].

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

Neurokinin A TFA (Substance K TFA), a peptide neurotransmitter of the tachykinin family, functions via the NK-2 receptor and acts as a key mediator in human airway and gastrointestinal tissues [1].

Neurokinin A (4-10) TFA is a tachykinin NK2 receptor agonist [1].

[Sar9,Met(O2)11]-Substance P TFA is a tachykinin NK 1 receptor selective agonist.

Men 10376 TFA is a selective antagonist of the tachykinin NK-2 receptor, exhibiting a K_i value of 4.4 μM for the NK-2 receptor in rat small intestine [1].