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YM022

CAS No. : 145084-28-2

MCE 站：YM022

产品活性：YM022 是一种高效，选择性和口服活性胃泌素/胆囊收缩素(CCK)-B 受体 (CCK-BR) 拮抗剂。 YM022 显示CCK-B 和 CCK-A 受体的 K_i 值分别为 68 pM 和 63 nM。 YM022 在体内可以抑制胃泌素诱导的胃酸分泌和组氨酸脱羧酶的活化。

研究领域：GPCR/G Protein  |  Immunology/Inflammation

作用靶点：CCR

In Vitro: YM022 inhibits binding to canine pancreas CCK-A receptor in a dose-dependent manner, with an IC₅₀ value for [³H]devazepide binding of 136 nM.
YM022 inhibits the binding of [¹²⁵I]CCK-8 to canine cloned gastrin/CCK-B receptor in a dose-dependent manner, with an IC₅₀ value for [¹²⁵I]CCK-8 binding of 0.73 nM.
Selectivity [ratio of (IC₅₀ for gastrin/CCK-B receptor)/(IC₅₀for CCK-A receptor)] of YM022 is 186.

In Vivo: YM022 (intravenous injection; 0.01-1 μM/kg) dose-dependently inhibits pentagastrin- and peptone meal-induced acid secretion with ED₅₀ values of 0.0261 and 0.0654 μmol/kg, respectively, without affecting histamine- or methacholine-induced acid secretion.
YM022 (subcutaneous injection; 300 μmol/kg; single dose) lowers the oxyntic mucosal HDC activity and raises the serum gastrin concentration in a dose-dependent manner (measured 24 h after dosage). Maximum enzyme inhibition is achieved at a dose of 300 μmol/kg ?for YM022 and the inhibition of HDC lasts for 4 weeks. At sacrifice, drug residues can be seen at the injection site for as long as 4 (YM022) weeks after injection in rat.
YM022 is suspended in 2% Methocel for oral ingestion and in PEG300 for subcutaneous injection.

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