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L-365260
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图片
CAS NO:118101-09-0
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
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200mg电议

产品介绍
L-365260 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 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 可增强 Morphine 缓解疼痛的活性，并防止 Morphine 耐受。
生物活性

L-365260 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 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brainCCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance[1][2][3].

IC50& Target

CCKBR

 

体外研究
(In Vitro)

L-365260 (1 μM) strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron[2].
L-365260 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].

体内研究
(In Vivo)

L-365260 (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats[3].
L-365260 (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats[3].
L-365260 (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].

Animal Model:Male Sprague-Dawley rats (300-350 g) were injected with Morphine[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

398.46

性状

Solid

Formula

C24H22N4O2

CAS 号

118101-09-0

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