Cat. No. 1408
Chemical Name: (R)-N-[2,3-Dihydro-1-[2-(2-methylph
Biological ActivityExtremely potent and highly selective non-peptide CCK2 silent antagonist (Ki values are 68 pM and 63 nM at CCK2 and CCK1 receptors respectively). Acts in vivo to potently inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation with a long duration of action.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Kitano et al (2000) Long-lasting cholecystokinin2 receptor blockade after a single subcutaneous injection of YF476 or YM022. Br.J.Pharmacol. 130 699. PMID: 10821801.
Beinborn et al (1998) Small synthetic ligands of the cholecystokinin-B/gastrin receptor can mimic the function of endogenous peptide hormones. Yale J.Biol.Med. 71 337. PMID: 10461364.
Nishida et al (1994) Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo. J.Pharmacol.Exp.Ther. 269 725. PMID: 7910212.
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Citations are publications that use Tocris products. Selected citations for YM 022 include:
Saia et al (2014) Cholecystokinin inhibits inducible nitric oxide synthase expression by lipopolysaccharide-stimulated peritoneal macrophages. Mediators Inflamm 2014 896029. PMID: 25125801.
Wagner et al (2013) The dorsomedial hypothalamus mediates stress-induced hyperalgesia and is the source of the pronociceptive peptide cholecystokinin in the rostral ventromedial medulla. Neuropharmacology 238 29. PMID: 23415792.
Marshall et al (2012) Activation of descending pain-facilitatory pathways from the rostral ventromedial medulla by cholecystokinin elicits release of prostaglandin-E2 in the spinal cord. Pain 153 86. PMID: 22030324.
Karson et al (2008) Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others. Br J Pharmacol 54 117. PMID: 17689570.
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Keywords: YM 022, supplier, potent, selective, non-peptide, CCK2, antagonists, Cholecystokinin2, Receptors, YM022, Tocris Bioscience, CCK2 Receptor Antagonist products