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
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.
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.