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Lintitript

CAS No. : 136381-85-6

MCE 站：Lintitript

产品活性：Lintitript (SR 27897) 是一种高效，选择性，口服活性，竞争性和非肽类 CCK1 受体拮抗剂，EC₅₀ 为 6 nM，K_i 为 0.2 nM。Lintitript 对 CCK1 的选择性比对 CCK2 受体的选择性高 33 倍以上 (EC₅₀值为 200 nM)。Lintitript 增加瘦素的血浆浓度和食物摄入以及胰岛素的血浆浓度。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Cholecystokinin Receptor

In Vitro: In vitro, Lintitript (SR 27897) is a competitive antagonist of cholecystokinin (CCK)-stimulated amylase release in isolated rat pancreatic acini (pA₂ = 7.50) and of CCK-induced guinea pig gall bladder contractions (pA₂ = 9.57).
Lintitript produces concentration dependent inhibition of [¹²⁵I]CCK binding to CCK1 receptor sites in the rat pancreas (IC₅₀ value of 0.58 nM) and also to CCK 2 sites in the guinea pig cortex (IC₂ value of 479 nM). Lintitript inhibits [¹²⁵I]gastrin binding to gastrin receptors. Lintitript (0.5 nM) increases the dissociation constant of CCK for the CCK A receptor (K_d = 1.8 to 7.2 nM) without modifying the maximum number of receptors (B_max = 1800 to 1770 fmol/mg).

In Vivo: Lintitript (SR 27897; 1 mg/kg, i.v.) completely reverses the CCK-induced amylase secretion. Lintitript also inhibits CCK-induced gastric and gallbladder emptying in mice (ED₅₀s = 3 and 72 μg/kg, respectively). Lintitript is also very active (ED₅₀ = 27 μg/kg p.o.) in the gall bladder emptying protocol with egg yolk as an inducer of endogenous CCK release.

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