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 | |
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 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
