Eptapirone (F 11440)
(Synonyms: F 11440) 目录号 : GC30939
A potent and selective 5-HT1A receptor agonist
Cas No.:179756-58-2
Sample solution is provided at 25 µL, 10mM.
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Eptapirone is a potent agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 4.8 nM in a radioligand binding assay).1 It is selective for 5-HT1A over other 5-HT receptor subtypes, dopamine D2 receptors, α1-adrenergic receptors, and histamine H1 receptors (Kis = <10,000, 1,770, 691.8, and <10,000 nM, respectively). Eptapirone inhibits cAMP stimulation induced by forskolin in HA7 cells transfected with human 5-HT1A receptors (EC50 = 158 nM). In vivo, eptapirone increases extracellular 5-HT in the ventral hippocampus of rats (ED50 = 0.049 mg/kg) and serum corticosterone levels when administered p.o. or i.p. (ED50s = 0.16 and 0.057 mg/kg, respectively). It decreases immobility in rats in a forced swim test and increases punished responding in a pigeon conflict procedure, demonstrating antidepressant-like and anxiolytic activity. Eptapirone (2.5 mg/kg, p.o.) also attenuates hypertension and tachycardia induced by sibutramine in rats with no effect on sibutramine-induced hypophagia.2
1.Koek, W., Patoiseau, J.-F., Assie, M.-B., et al.F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potentialJ.Pharmacol. Exp. Ther.287(1)266-283(1998) 2.Thomas, G.H., Babbs, A.J., Chatfield, R.E., et al.5-HT1A activation counteracts cardiovascular but not hypophagic effects of sibutramine in ratsObesity (Silver Spring)17(3)467-473(2009)
Cell experiment: | Eptapirone (F11440) is dissolved in DMSO. The HeLa cell line permanently transfected with the human 5-HT1A receptor gene and permanently expressing the 5-HT1A receptor protein (HA7). In subsequent experiments, the maximum effect of Eptapirone (F11440) is compared with those of other compounds by repeated testing (n=9) at a concentration of 10-5 M (i.e., a concentration at which the reference compounds used here appeared to attain their maximal effects) in a first series of experiments and at 10-4 M in a second series. Data from each series were analyzed statistically by means of a one-way analysis of variance followed by sequential paired comparisons by means of Newman-Keuls tests[1]. |
Animal experiment: | Rats[1]For in vivo studies, F 11440 was suspended in distilled water by adding Tween 80 (2 drops/10 ml). When injected i.v., F 11440 was dissolved in a mixture of 60% PEG and 40% physiological saline. Doses are expressed as the weight of the free base. Twenty-four hours before use in the experiments, rats were housed individually in a restricted area (accessible only to the experimenter) and received 15 g standard laboratory food (water continued to be available freely). Experiments, consisting of drug treatments after which animals were decapitated and trunk blood was collected, were conducted between 8:00 a.m. and 10:30 a.m. F 11440 (or vehicle) was administered 60 min before decapitation when given p.o., and 30 min before decapitation when given i.p.[1]. |
References: [1]. Koek W, et al. F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. J Pharmacol Exp Ther. 1998 Oct;287(1):266-83. | |
| Cas No. | 179756-58-2 | SDF | |
| 别名 | F 11440 | ||
| Canonical SMILES | O=C(N1C)N(CCCCN2CCN(C3=NC=CC=N3)CC2)N=CC1=O | ||
| 分子式 | C16H23N7O2 | 分子量 | 345.4 |
| 溶解度 | DMSO : 6 mg/mL (17.37 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8952 mL | 14.476 mL | 28.9519 mL |
| 5 mM | 0.579 mL | 2.8952 mL | 5.7904 mL |
| 10 mM | 0.2895 mL | 1.4476 mL | 2.8952 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet