产品
编 号：F058105
分子式：C24H22N4O2
分子量：398.46
分子式：C24H22N4O2
分子量：398.46
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 118101-09-0
产品详情
生物活性：
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance.
体内研究：
L-365260 (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats.L-365260 (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats.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).Animal Model:Male Sprague-Dawley rats (300-350 g) were injected with Morphine
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.
体外研究：
L-365260 (1 μM) strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron.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.
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance.
体内研究：
L-365260 (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats.L-365260 (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats.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).Animal Model:Male Sprague-Dawley rats (300-350 g) were injected with Morphine
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.
体外研究：
L-365260 (1 μM) strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron.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.
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