|Related Categories||A-AM, Antagonist, Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology,|
|Gene Information||human ... TACR1(6869)|
Competitive substance P receptor antagonist. It is approximately 1000-fold more potent at cloned human NK-1 receptors than at cloned human NK-2 and NK-3 receptors; and approximately 200-fold more potent at human NK-1 receptors than at rat NK-1 receptors. The IC50 for the human NK-1 receptor expressed in CHO cells is approximately 2 nM.
The substance P/neurokinin-1 receptor system in lung cancer: focus on the antitumor action of neurokinin-1 receptor antagonists. Muñoz M, González-Ortega A, Rosso M, et al. Peptides 38(2), 318-25, (2012)
Role of tachykinins and neurokinin receptor subtypes in the regulation of motility of the forestomach and abomasum in conscious sheep. Oh-ishi T, Shimoda T, Hayashi H, et al. Neuropeptides 47(1), 9-18, (2013)
Tachykinin NK₁ receptor antagonist co-administration attenuates opioid withdrawal-mediated spinal microglia and astrocyte activation. Tumati S, Largent-Milnes TM, Keresztes AI, et al. Eur. J. Pharmacol. 684(1-3), 64-70, (2012)
The NK-1 receptor is expressed in human leukemia and is involved in the antitumor action of aprepitant and other NK-1 receptor antagonists on acute lymphoblastic leukemia cell lines. Muñoz, M., et al. Invest. New Drugs 30, 529-40, (2012)
Spinal cord mechanisms mediating behavioral hyperalgesia induced by neurokinin-1 tachykinin receptor activation in the rostral ventromedial medulla. Lagraize SC, Guo W, Yang K, et al. Neuroscience 171(4), 1341-56, (2010)
NK-1 receptor antagonists induce apoptosis and counteract substance P-related mitogenesis in human laryngeal cancer cell line HEp-2. Muñoz M, Rosso M, Aguilar FJ, et al. Invest. New Drugs 26(2), 111-8, (2008)
Neurokinin-1 receptors located in human retinoblastoma cell lines: antitumor action of its antagonist, L-732,138. Muñoz M, Rosso M, Coveñas R, et al. Invest. Ophthalmol. Vis. Sci. 48(6), 2775-81, (2007)
Vanilloid receptor-1 (TRPV1)-dependent activation of inhibitory neurotransmission in spinal substantia gelatinosa neurons of mouse. Ferrini F, Salio C, Vergnano AM, et al. Pain 129(1-2), 195-209, (2007)
Paradoxical effect of salbutamol in a model of acute organophosphates intoxication in guinea pigs: role of substance P release. Chávez J, Segura P, Vargas MH, et al. Am. J. Physiol. Lung Cell. Mol. Physiol. 292(4), L915-23, (2007)
Involvement of TRPV1-dependent and -independent components in the regulation of vagally induced contractions in the mouse esophagus. Boudaka A, Wörl J, Shiina T, et al. Eur. J. Pharmacol. 556(1-3), 157-65, (2007)
Effects of KP-496, a novel dual antagonist for leukotriene D4 and thromboxane A2 receptors, on contractions induced by various agonists in the guinea pig trachea. Ishimura M, Kataoka S, Suda M, et al. Allergol. Int. 55(4), 403-10, (2006)
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