L-365260 hemihydrate

Name: L-365260 hemihydrate
Brand: TargetMol
SKU: T62039
Rating: 4.5 (1 reviews)

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产品编号 T62039

L-365260 hemihydrate 是选择性的、具有口服活性的非肽胃泌素和脑胆囊收缩素受体 (CCK-B) 拮抗剂，Kis 值分别为 1.9 nM 和 2.0 nM。L-365260 hemihydrate 以竞争性方式与豚鼠胃泌素和脑 CCK 受体相互作用。

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产品编号 T62039

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产品介绍

生物活性

产品描述	L-365260 hemihydrate is a selective, orally active non-peptide gastrin and brain cholecystokinin receptor (CCK-B) antagonist, demonstrating competitive interaction with guinea pig stomach gastrin and brain CCK receptors and exhibiting inhibition constants (Kis) of 1.9 nM and 2.0 nM, respectively.
体外活性	L-365260 hemihydrate exhibits a similar high affinity for brain CCK-B receptors of rats, mice and man, and a lower affinity for gastrin and brain CCK-B (IC 50 =20-40 nM) receptors in dog tissues [1]. L-365260 (1 μM) hemihydrate strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron [2].
体内活性	L-365260 hemihydrate (0.1-30 mg/kg; p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED 50 =0.03 mg/kg), rats (ED 50 =0.9 mg/kg) and guinea pigs (ED 50 =5.1 mg/kg) [1]. L-365260 hemihydrate (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats [3]. L-365260 hemihydrate (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats [3]. Animal Model: Male Sprague-Dawley rats (300-350 g; Morphine- injected) [3]. Dosage: 0.01, 0.05, 0.1, 0.2, 0.75, 1.0, 10.0 mg/kg Administration: S.c. 10 min prior to i.p. injection of 4 mg/kg Morphine Result: Enhanced morphine analgesia.