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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.
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|Storage||Store at RT|
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.
|Solubility||Soluble to 100 mM in DMSO and to 5 mM in ethanol|
References are publications that support the biological activity of the product.
Giardina et al (1997) Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. J.Med.Chem. 40 1794 PMID: 9191956
Medhurst et al (1997) In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists. Br.J.Pharmacol. 122 469 PMID: 9351503
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Keywords: SB 218795, SB 218795 supplier, Potent, selective, non-peptide, NK3, antagonists, Tachykinin, Receptors, Neurokinin, SB218795, Receptor, 1376, Tocris Bioscience
4 Citations for SB 218795
Citations are publications that use Tocris products. Selected citations for SB 218795 include:
Liñán-Rico et al (2015) Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X?, P2X?, P2X? channels, P2Y and A? metabotropic receptors in neurotransmission. Neuropharmacology 95 83 PMID: 25724083
Valero et al (2011) Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol Sin 32 487 PMID: 21441943
Cunin et al (2011) 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. J Immunol 186 4175 PMID: 21368235
Wang et al (2014) Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine. Am J Physiol Gastrointest Liver Physiol 307 G719 PMID: 25147231
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