Identification | Back Directory | [Name]
L 365260 | [CAS]
118101-09-0 | [Synonyms]
260 L-365 L 365260 MSD-365260 L-365260
(L 365260 (3R)-1-Methyl-3-[3-(3-methylphenyl)ureido]-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one 1-[[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin]-3-yl]-3-(3-methylphenyl)urea Urea, N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)- (+)-1-[[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin]-3-yl]-3-(3-methylphenyl)urea (+)-N-[[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin]-3-yl]-N'-(3-methylphenyl)urea | [Molecular Formula]
C24H22N4O2 | [MDL Number]
MFCD00869756 | [MOL File]
118101-09-0.mol | [Molecular Weight]
398.46 |
Hazard Information | Back Directory | [Uses]
L-365,260 is a non-peptide competitive CCK-BR antagonist. | [Definition]
ChEBI: L-365260 is a benzodiazepine. | [Biological Activity]
Selective cholecystokinin receptor 2 (CCK 2 ) antagonist (IC 50 values are 2 and 280 nM at CCK 2 and CCK 1 receptors respectively) that is inactive at a range of other receptors including opiate, muscarinic acetylcholine, α - and β adrenergic, histamine, angiotensin and bradykinin receptors. | [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. |
| [IC 50]
CCKBR | [storage]
Store at +4°C |
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