Guanfacine hydrochloride
(Synonyms: 盐酸胍法辛) 目录号 : GC12132
An α2-adrenergic receptor agonist
Cas No.:29110-48-3
Sample solution is provided at 25 µL, 10mM.
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Guanfacine, an anti-hypertensive agent, is a selective agonist of α2A-adrenoceptor (α2AR) with a Kd value of 31 nM, displaying 60-fold selectivity over α2B-adrenoceptors.
In 5-choice serial reaction-time task (5-CSRTT), guanfacine treated at a low dose has been shown to increase attention in NK1R knockout mice, but not in WT mice. Guanfacine treated at a high dose reduced impulsivity in both NK1R-/- and WT mice [1].
Guanfacine has been demonstrated to reduce alcohol intake in high alcohol-consuming rats. Guanfacine treatment has been revealed to decrease the alcohol deprivation effect (ADE) and reduce the alcohol seeking and cue/priming-mediated reinstatement of alcohol seeking in rats [2].
Guanfacine has shown to reduce C-fiber-evoked field potentials in a rat model induced by spinal nerve ligation, the effect of which was reduced by treatment of receptors of the delta (DOR) antagonist naltrindole, but not by treatment of receptors of the mu (MOR) antagonist CTOP. On the contrary, DOR agonist deltorphin II, but not MOR agonist DAMGO-mediated depression of C-fiber-evoked spinal field potentials was increased by guanfacine. Additionally, co-administration of guanfacine at a low dose with deltorphin II could enhance the effect of deltorphin II mediated production of stable thermal and mechanical antinociception in nerve-ligated rats [3].
References:
1.Pillidge K1, Porter AJ, Dudley JA, Tsai YC, Heal DJ, Stanford SC. The behavioural response of mice lacking NK₁ receptors to guanfacine resembles its clinical profile in treatment of ADHD. Br J Pharmacol. 2014 Oct;171(20):4785-96. doi: 10.1111/bph.12860.
2.Fredriksson I1, Jayaram-Lindström N1, Wirf M1, Nylander E1, Nyström E1, Jardemark K2, Steensland P1.Evaluation of Guanfacine as a Potential Medication for Alcohol Use Disorder in Long-Term Drinking Rats: Behavioral and Electrophysiological Findings. Neuropsychopharmacology. 2014 Oct 31. doi: 10.1038/npp.2014.294. [Epub ahead of print]
3.Aira Z1, Barrenetxea T1, Buesa I1, Azkue JJ2. Plasticity of α2-adrenergic spinal antinociception following nerve injury: Selective, bidirectional interaction with the delta opioid receptor. Brain Res. 2015 Jan 12;1594:190-203. doi: 10.1016/j.brainres.2014.11.009.
| Cas No. | 29110-48-3 | SDF | |
| 别名 | 盐酸胍法辛 | ||
| 化学名 | N-(diaminomethylidene)-2-(2,6-dichlorophenyl)acetamide;hydrochloride | ||
| Canonical SMILES | C1=CC(=C(C(=C1)Cl)CC(=O)N=C(N)N)Cl.Cl | ||
| 分子式 | C9H10Cl3N3O | 分子量 | 282.55 |
| 溶解度 | ≥ 14.1 mg/mL in DMSO, ≥ 17.17 mg/mL in EtOH with ultrasonic and warming, ≥ 50.6 mg/mL in Water with gentle warming | 储存条件 | Store at -20°C,sealed storage, away from moisture |
| 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 | 3.5392 mL | 17.696 mL | 35.392 mL |
| 5 mM | 0.7078 mL | 3.5392 mL | 7.0784 mL |
| 10 mM | 0.3539 mL | 1.7696 mL | 3.5392 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet