L-365260 hemihydrate |
| رقم الكتالوجGC70264 |
يعتبر L-365260 hemihydrate مناهضًا انتقائيًا نشطًا عن طريق الفم لمستقبلات غاسترين غير الببتيدية ومستقبلات كوليستوكينين في الدماغ (CCK-B)، حيث يبلغ Kis 1.9 نانومتر و 2.0 نانومتر على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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L-365260 hemihydrate 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].
L-365260 (1 μM) hemihydrate strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron[2].
L-365260 hemihydrate (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].
L-365260 hemihydrate (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats[3].
L-365260 hemihydrate (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats[3].
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]. 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.
[3]. 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.
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