| Bioactivity | L-365260 is an orally active 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]. | ||||||||||||
| Invitro | 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: | ||||||||||||
| Name | L-365260 | ||||||||||||
| CAS | 118101-09-0 | ||||||||||||
| Formula | C24H22N4O2 | ||||||||||||
| Molar Mass | 398.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |