SB 218795
Chemical Name: (R)-[[2-Phenyl-4-quinolinyl)carbonyl]amino]-methyl ester benzeneacetic acid
Purity: ≥99%
Biological Activity
SB 218795 is a potent, selective and competitive non-peptide NK3 receptor antagonist (Ki = 13 nM at hNK3). Displays 90-fold and 7000-fold selectivity over hNK2 and hNK1 receptors respectively. Active in vivo, inhibiting agonist-induced pupillary constriction.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.
Giardina et al.
J.Med.Chem., 1997;40:1794 -
In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists.
Medhurst et al.
Br.J.Pharmacol., 1997;122:469
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Citations for SB 218795
The citations listed below are publications that use Tocris products. Selected citations for SB 218795 include:
4 Citations: Showing 1 - 4
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Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X?, P2X?, P2X? channels, P2Y and A? metabotropic receptors in neurotransmission.
Authors: Liñán-Rico Et al.
Neuropharmacology 2015;95:83
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Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine.
Authors: Wang Et al.
Am J Physiol Gastrointest Liver Physiol 2014;307:G719
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Contractile effect of tachykinins on rabbit small intestine.
Authors: Valero Et al.
Acta Pharmacol Sin 2011;32:487
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The tachykinins substance P and hemokinin-1 favor the generation of human memory Th17 cells by inducing IL-1β, IL-23, and TNF-like 1A expression by monocytes.
Authors: Cunin Et al.
J Immunol 2011;186:4175
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