Name | N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N′-(3-methylphenyl)-urea |
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Synonyms |
L-365,260,N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)urea
L-365260 |
Description | L-365260 is a potent and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance[1][2][3]. |
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Related Catalog | |
Target |
Ki: 1.9 nM (gastrin); 2.0 nM (CCK-B)[1] |
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]. |
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. |
References |
Density | 1.23g/cm3 |
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Boiling Point | 611.5ºC at 760 mmHg |
Molecular Formula | C24H22N4O2 |
Molecular Weight | 398.45700 |
Flash Point | 323.6ºC |
Exact Mass | 398.17400 |
PSA | 73.80000 |
LogP | 3.92110 |
Vapour Pressure | 6.85E-15mmHg at 25°C |
Index of Refraction | 1.648 |
Storage condition | 2-8°C |
Symbol |
GHS06, GHS09 |
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Signal Word | Danger |
Hazard Statements | H301-H400 |
Precautionary Statements | P273-P301 + P310 |
RIDADR | UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all |