A 80426 mesylate |
カタログ番号GC13027
One-Click Copy Product Info
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α2アドレノセプター拮抗剤および5-HT再取り込み阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 152148-63-5
Sample solution is provided at 25 µL, 10mM.
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A-80426 is a potent and selective α2-adrenoceptor antagonist, it can block serotonin uptake and have putative antidepressant-like effects. It inhibits synaptosomal serotonin (5HT) uptake with an IC50 value of 13 nM and blocks [3H]-paroxetine binding to 5HT uptake sites with a Ki value of 3.8 nM. It inhibits [3H]-rauwolscine binding to α2-adrenoceptors with a Ki value of 2.0 nM, and blocks α2-adrenoceptors with a pEC30 of 7.4-7.5 in electrically stimulated rat vas deferens and atria [1].
α2-adrenoceptors mediate many physiological actions of endogenous noradrenaline and catecholamines adrenaline [2].
In radioligand binding assays with isolated tissues, the potent blocking activity of A-80426 against α2-adrenoceptor is not reflected [1].
P-chloroamphetamine (PCA)-induced hyperactivity is a measure of the blockade of serotonin uptake in vivo. In rats, p-chloroamphetamine (PCA)-induced hyperactivity was significantly reduced by A-80426 at doses of chronic (14 days) (ED50=4.1 ?mol/kg, po) and acute (ED50= 13 ?mol/kg, po). Administration (po) of A-80426 at doses of 6.7 and 22?mol/kg was effective for at least 12 h. Doses of 6.7 to 224?mol/kg, ip, of A-80426 failed to block hypoactivity and hypothermia resulted from the administration of α2-adrenoceptor agonist clonidine. Doses of 100 and 300 ?mol/kg, po, were required to block the mydriasis induced by clonidine [3].
References:
[1]. Hancock AA, Buckner SA, Oheim KW, et al. A-80426, a potent α2-adrenoceptor antagonist with serotonin uptake blocking activity and putative antidepressant-like effects: I. Biochemical profile. Drug Development Research, 1995, 35(4): 237-245.
[2]. Aantaa R, Marjam?ki A and Scheinin M. Molecular Pharmacology of α2-adrenoceptor Subtypes. Annals of Medicine, 1995, 27(4): 439-449.
[3]. Giardina WJ, Buckner SA, Brune ME, et al. A-80426, A Potent and Selective α2-Adrenoceptor Antagonist With Serotonin Uptake-Blocking Activity and Putative Antidepressant-Like Effects: II. Pharmacology Profile. Drug Development Research, 1995, 35(4): 246-260.
| Cas No. | 152148-63-5 | SDF | |
| Chemical Name | (R)-2-(benzofuran-6-yl)-N-((5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)methyl)-N-methylethanamine methanesulfonate | ||
| Canonical SMILES | CN(C[C@]1([H])CCCC2=C1C=CC=C2OC)CCC3=CC4=C(C=CO4)C=C3.CS(O)(=O)=O | ||
| Formula | C23H27NO2.CH3SO3H | M.Wt | 445.57 |
| 溶解度 | <44.56mg/ml in DMSO | Storage | Store at -20°C |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2443 mL | 11.2216 mL | 22.4432 mL |
| 5 mM | 448.9 μL | 2.2443 mL | 4.4886 mL |
| 10 mM | 224.4 μL | 1.1222 mL | 2.2443 mL |
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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 saline, 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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)