L 365260
L 365260 Basic information
- Product Name:
- L 365260
- Synonyms:
-
- L 365260
- (+)-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
- (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
- MSD-365260
- L-365260 (L 365260
- Urea, N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)-
- CAS:
- 118101-09-0
- MF:
- C24H22N4O2
- MW:
- 398.46
- Mol File:
- 118101-09-0.mol
L 365260 Chemical Properties
- storage temp.
- Store at +4°C
- solubility
- DMSO: >20mg/mL
- form
- solid
- color
- White to off-white
L 365260 Usage And Synthesis
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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