118101-09-0

118101-09-0 structure

Name: L-365,260
Chemical Name: N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N′-(3-methylphenyl)-urea
CAS Number: 118101-09-0
Molecular Formula: C₂₄H₂₂N₄O₂
Molecular Weight: 398.45700
Catalog: Signaling Pathways GPCR/G Protein Cholecystokinin Receptor
Create Date: 2017-04-01 10:25:33
Modify Date: 2025-08-25 23:19:48
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].

Name	N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N′-(3-methylphenyl)-urea
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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Cholecystokinin Receptor Research Areas >> Metabolic Disease Research Areas >> Neurological Disease
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	[1]. Lotti VJ, et, al. A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260. Eur J Pharmacol. 1989 Mar 21;162(2):273-80. [2]. Chung L, et, al. Cholecystokinin action on layer 6b neurons in somatosensory cortex. Brain Res. 2009 Jul 28;1282:10-9. [3]. Dourish CT, et, al. The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat. Eur J Pharmacol. 1990 Jan 25;176(1):35-44.

Density	1.23g/cm3
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
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

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