L-365260

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的胆囊收缩素受体 2 (CCK2) 拮抗剂，IC50 为 2 nM。

A potent, selective, orally active cholecystokinin receptor 2 (CCK2) antagonist with IC50 of 2 nM; displays >100-fold selecitvity over CCK1; antagonizes gastrin-stimulated acid secretion in mice (ED50 = 0.03 mg/kg), does not affect basal acid secretion and did not antagonize histamine- or carbachol-stimulated acid secretion.Anxiety Discontinued.

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 (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 MorphineResult:Enhanced morphine analgesia.

L 365260 | L365260

GPCR/G Protein

Cholecystokinin Receptor

Cholecystokinin Receptor

Neurological Disease

Anxiety

118101-09-0

398.46

C24H22N4O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (250.97 mM)

O=C(NC1=CC=CC(C)=C1)N[C@H]2C(N(C)C3=CC=CC=C3C(C4=CC=CC=C4)=N2)=O

N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)urea

(-20℃)

With Ice Pack

≥ 2 years