Guanfacine hydrochloride |
| カタログ番号GC12132 |
α2-アドレナリン受容体作動薬
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | N-(diaminomethylidene)-2-(2,6-dichlorophenyl)acetamide;hydrochloride | ||
| Canonical SMILES | C1=CC(=C(C(=C1)Cl)CC(=O)N=C(N)N)Cl.Cl | ||
| Formula | C9H10Cl3N3O | M.Wt | 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 | Storage | Store at -20°C,sealed storage, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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