Befiradol hydrochloride (NLX-112 (hydrochloride))
目录号 : GC34304
Befiradolhydrochloride(NLX-112hydrochloride)是选择性的5-羟色胺1A(5-HT)1A受体激动剂。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats[1]Male albino Wistar rats (230-300 g) are used throughout the study. Rats are anaesthetized with chloral hydrate (400-500 mg/kg, i.p.) or isoflurane. For the experiment with systemic administration of the compounds, saline or (±)WAY100635 are injected s.c., followed, 40 min later, by i.p. administration of saline or Befiradol. For the experiments with local perfusion, saline is injected s.c. and 40 min later, Befiradol (F13640; NLX-112) is added to the perfusion medium for the concentration-response experiment. For the antagonism, (±)WAY100635 (or aCSF) is delivered through the dialysis probe and 40 min later, Befiradol is added to the perfusion medium. Samples are collected for 140 min after administration or beginning of the perfusion of the agonist[1]. |
References: [1]. Lladó-Pelfort L, et al. In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat. Psychopharmacology (Berl). 2012 May;221(2):261-72. | |
Befiradol hydrochloride (NLX-112 hydrochloride) is a selective 5-HT1A receptor agonist.
Befiradol (F13640; NLX-112) reduces the activity of dorsal raphe serotonergic neurons at 0.2-18.2 μg/kg, i.v. (cumulative doses; ED50=0.69 μg/kg, i.v.) and increases the discharge rate of 80% of mPFC pyramidal neurons in the same dose range (ED50=0.62 μg/kg, i.v.). Both effects are reversed by the subsequent administration of the 5-HT1A receptor antagonist (±)WAY100635. In microdialysis studies, Befiradol (F13640; NLX-112) (0.04-0.63 mg/kg, i.p.) dose-dependently decreases extracellular 5-HT in the hippocampus and mPFC. Likewise, Befiradol (F13640; NLX-112) (0.01-2.5 mg/kg, i.p.) dose-dependently increases extracellular DA in mPFC, an effect dependent on the activation of postsynaptic 5-HT1A receptors in mPFC. Local perfusion of Befiradol in mPFC (1-1,000 μM) also increases extracellular DA in a concentration-dependent manner. Both the systemic and local effects of Befiradol are prevented by prior (±)WAY100635 administration[1].
[1]. Lladó-Pelfort L, et al. In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat. Psychopharmacology (Berl). 2012 May;221(2):261-72.
| Cas No. | SDF | ||
| Canonical SMILES | O=C(C1=CC=C(F)C(Cl)=C1)N2CCC(CNCC3=NC=C(C)C=C3)(F)CC2.Cl | ||
| 分子式 | C20H23Cl2F2N3O | 分子量 | 430.32 |
| 溶解度 | DMSO : 125 mg/mL (290.48 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 | 2.3239 mL | 11.6193 mL | 23.2385 mL |
| 5 mM | 0.4648 mL | 2.3239 mL | 4.6477 mL |
| 10 mM | 0.2324 mL | 1.1619 mL | 2.3239 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。
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