A 80426 mesylate
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.
| Physical Appearance | White solid |
| Storage | Store at -20°C |
| M.Wt | 445.57 |
| Cas No. | 152148-63-5 |
| Formula | C23H27NO2·CH3SO3H |
| Solubility | insoluble in H2O; <44.56mg/ml in DMSO |
| Chemical Name | (R)-2-(benzofuran-6-yl)-N-((5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)methyl)-N-methylethanamine methanesulfonate |
| SDF | Download SDF |
| Canonical SMILES | CN(C[C@]1([H])CCCC2=C1C=CC=C2OC)CCC3=CC4=C(C=CO4)C=C3.CS(O)(=O)=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
