L-365,260是胃泌素和脑胆囊收缩素受体B亚型（CCKB）的选择性拮抗剂，Ki值分别为1.9nM和2.0nM。
Cas No.:118101-09-0
Sample solution is provided at 25 µL, 10mM.
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L-365,260 is a selective antagonist of gastrin and brain type B cholecystokinin receptor (CCKB), with Ki values of 1.9nM and 2.0nM, respectively. L-365,260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365,260 represents a potentially powerful new tool for investigating gastrin and brain CCKB receptors, and possibly their role in physiology and disease[1][2].
In vitro, pretreatment with 100nM L-365,260 for 1 hour completely blocked CCK-8S-induced calcium signal enhancement in the rat C6 glioma cells[3]. L-365,260 also inhibited the binding of 125I-BH-CCK-8S to rat C6 glioma cells with an IC50 of 9.9nM[3]. Administering 2.5μM L-365,260 for 5 days reduced the baseline growth of two human colon cancer cell lines, LoVo and C146, to 44% and 64% of the control group, respectively[4].
In vivo, in male albino Wistar rats, intraperitoneal administration of L-365,260 (0, 0.1, 1 and 10mg/kg) 15 minutes before testing decreased the startle amplitude on light+noise trials in a dose-dependent manner, while producing no effect on the average of the five baseline habituation (noise-alone) startle amplitudes[5]. In nude mice bearing AR42J xenografts, L-365,260 (5mg/kg/d) administered by oral gavage twice daily for 3-4 weeks inhibited the growth of AR42J tumors[4].
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] Kaufmann R, Lindschau C, Schöneberg T, et al. Type B cholecystokinin receptors on rat glioma C6 cells. Binding studies and measurement of intracellular calcium mobilization. Brain Res. 1994;639(1):109-114.
[4] Watson S, Durrant L, Elston P, Morris D. Inhibitory effects of the gastrin receptor antagonist (L-365,260) on gastrointestinal tumor cells. Cancer. 1991;68(6):1255-1260.
[5] Josselyn SA, Frankland PW, Petrisano S, Bush DE, Yeomans JS, Vaccarino FJ. The CCKB antagonist, L-365,260, attenuates fear-potentiated startle. Peptides. 1995;16(7):1313-1315.
L-365,260是胃泌素和脑胆囊收缩素受体B亚型（CCKB）的选择性拮抗剂，Ki值分别为1.9nM和2.0nM。L-365,260以立体选择性和竞争性的方式与豚鼠胃泌素和脑CCK受体相互作用。L-365,260为研究胃泌素和脑CCKB受体及其在生理和疾病中的作用提供了潜在的强大新工具。
体外实验中，用100nM L-365,260预处理1小时可完全阻断CCK-8S在大鼠C6胶质瘤细胞中诱导的钙信号增强。此外，L-365,260还能抑制125I-BH-CCK-8S与大鼠C6胶质瘤细胞的结合，其IC₅₀值为9.9nM[3]。2.5μM L-365,260给药5天，降低了两种人类结肠癌细胞LoVo和C146的基线生长，分别降至对照组的44%和64%[4]。
体内实验中，在雄性白化Wistar大鼠中，于实验前15分钟腹腔注射L-365,260（0、0.1、1和10mg/kg）可剂量依赖性地降低光+噪声试验中的惊跳幅度，但对五次基线习惯化（仅噪声）试验的平均惊跳幅度没有影响[5]。在移植了AR42J的裸鼠中，每日两次灌胃给予L-365,260（5mg/kg/天），持续3-4周，抑制了AR42J肿瘤的生长[4]。
| Cell experiment [1]: | |
Cell lines | Rat C6 glioma cells |
Preparation Method | Pretreatment with 100nM L-365,260 for 1 hour, followed by the addition of 1.0nM CCK-8S, and intracellular free calcium levels were detected using fluo-3. |
Reaction Conditions | 100nM; 1h |
Applications | Pretreatment with 100nM L-365,260 for 1 hour completely blocked CCK-8S-induced calcium signal enhancement in the rat C6 glioma cells. |
| Animal experiment [2]: | |
Animal models | Male albino Wistar rats |
Preparation Method | L-365,260 was homogeneously suspended in saline containing Tween 80 (0.1%). Rats received 10 pairings of the conditioning stimulus (CS) with the unconditioned stimulus (US) in the operant cage for 3 days. Four to six days following the completion of conditioning, each rat was pretreated (15min) with L365,260 (0, 0.1, 1, or 10mg/kg) before being placed in the startle testing cage. Fifteen minutes later, five noise bursts (119dB with 60s intertrial interval) were presented to produce some short-term habituation and reduce response levels before testing for fear potentiation. Forty noise bursts, half of which were presented alone (noise-alone trials) and half in conjunction with the CS (light+noise trials), were then presented. |
Dosage form | 0, 0.1, 1 and 10mg/kg; i.p. |
Applications | L-365,260 decreased the startle amplitude on light+noise trials in a doserelated manner. In contrast, the baseline (noise-alone) trials did not appear to be altered in any systematic way by L-365,260. |
References: | |
| Cas No. | 118101-09-0 | SDF | |
| 化学名 | (R)-1-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-3-(m-tolyl)urea | ||
| Canonical SMILES | O=C1N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N[C@H]1NC(NC4=CC=CC(C)=C4)=O | ||
| 分子式 | C24H22N4O2 | 分子量 | 398.46 |
| 溶解度 | <39.85mg/ml in DMSO; <39.85mg/ml in ethanol | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5097 mL | 12.5483 mL | 25.0966 mL |
| 5 mM | 501.9 μL | 2.5097 mL | 5.0193 mL |
| 10 mM | 251 μL | 1.2548 mL | 2.5097 mL |
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