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Category:
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7TM Receptors Peptides (Gastrointestinal) CCK Receptors
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Cat.No.
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Product Name
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1408 |
YM 022
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Price and Availability
Click here for full price details of
YM 022
Other Information:
Not
for sale in Japan
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Chemical Name:
(R)-N-[2,3-Dihydro-1-[2-(2-methylphenyl)-2-oxoethyl]-2-
oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphe
nyl)-urea |
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Biological Activity:
Extremely
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.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
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. 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. Kitano et al
(2000) Long-lasting cholecystokinin2
receptor blockade after a single subcutaneous injection of YF476 or YM022.
Br.J.Pharmacol. 130 699.
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or by Research Area
Keywords: YM 022, Peptides (Gastrointestinal), Highly Potent, Selective Non-peptide CCK2 Antagonist, YM022, Tocris Bioscience
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