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L-365260 hemihydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L-365260 hemihydrate图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
L-365260 hemihydrate 是一种口服有效的和选择性的非肽胃泌素和脑胆囊收缩素受体 (CCK-B) 拮抗剂,其Kis 值分别为 1.9 nM 和 2.0 nM。L-365260 hemihydrate 以立体选择性和竞争性方式与豚鼠胃胃泌素和脑CCK受体相互作用。L-365260 hemihydrate 可增强 Morphine 缓解疼痛的活性,并防止 Morphine 耐受。
生物活性

L-365260 hemihydrate is an orally active and selective antagonist of non-peptidegastrinandbraincholecystokinin receptor(CCK-B), withKis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brainCCK receptors. L-365260 hemihydrate can enhance Morphine analgesia and prevents Morphine tolerance[1][2][3].

IC50& Target

Ki: 1.9 nM (gastrin); 2.0 nM (CCK-B)[1].

体外研究
(In Vitro)

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 (IC50=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].

体内研究
(In Vivo)

L-365260 hemihydrate (0.1-30 mg/kg; p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED50=0.03 mg/kg), rats (ED50=0.9 mg/kg) and guinea pigs (ED50=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.
分子量

407.47

性状

Solid

Formula

C24H24N4O3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month