ChemicalBook--->CAS DataBase List--->118101-09-0

118101-09-0

118101-09-0 Structure

118101-09-0 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[storage temp. ]

Store at +4°C
[solubility ]

DMSO: >20mg/mL
[form ]

solid
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]


GHS06,GHS09
[Signal word ]

Danger
[Hazard statements ]

H301-H400
[Precautionary statements ]

P273-P301+P310
[Hazard Codes ]

T,N
[Risk Statements ]

25-50/53
[Safety Statements ]

45-60-61
[RIDADR ]

UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all
Hazard InformationBack 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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