Product Name :
A 80426 mesylate
Description:
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 . α2-adrenoceptors mediate many physiological actions of endogenous noradrenaline and catecholamines adrenaline . In radioligand binding assays with isolated tissues, the potent blocking activity of A-80426 against α2-adrenoceptor is not reflected . 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 .
CAS:
152148-63-5
Molecular Weight:
445.57
Formula:
C24H31NO5S
Chemical Name:
[2-(1-benzofuran-6-yl)ethyl]({[(1R)-5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl]methyl})methylamine; methanesulfonic acid
Smiles :
COC1=CC=CC2[C@H](CN(C)CCC3=CC4OC=CC=4C=C3)CCCC=21.CS(O)(=O)=O
InChiKey:
RKQPEIGWZATOHW-FYZYNONXSA-N
InChi :
InChI=1S/C23H27NO2.CH4O3S/c1-24(13-11-17-9-10-18-12-14-26-23(18)15-17)16-19-5-3-7-21-20(19)6-4-8-22(21)25-2;1-5(2,3)4/h4,6,8-10,12,14-15,19H,3,5,7,11,13,16H2,1-2H3;1H3,(H,2,3,4)/t19-;/m0.{{Eplerenone} site|{Eplerenone} Mineralocorticoid Receptor|{Eplerenone} Protocol|{Eplerenone} In Vitro|{Eplerenone} manufacturer|{Eplerenone} Epigenetic Reader Domain} /s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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 .{{Vemurafenib} web|{Vemurafenib} Raf|{Vemurafenib} Technical Information|{Vemurafenib} Data Sheet|{Vemurafenib} manufacturer|{Vemurafenib} Epigenetics} α2-adrenoceptors mediate many physiological actions of endogenous noradrenaline and catecholamines adrenaline .PMID:23255394 In radioligand binding assays with isolated tissues, the potent blocking activity of A-80426 against α2-adrenoceptor is not reflected . 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 .|Product information|CAS Number: 152148-63-5|Molecular Weight: 445.57|Formula: C24H31NO5S|Chemical Name: [2-(1-benzofuran-6-yl)ethyl]({[(1R)-5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl]methyl})methylamine; methanesulfonic acid|Smiles: COC1=CC=CC2[C@H](CN(C)CCC3=CC4OC=CC=4C=C3)CCCC=21.CS(O)(=O)=O|InChiKey: RKQPEIGWZATOHW-FYZYNONXSA-N|InChi: InChI=1S/C23H27NO2.CH4O3S/c1-24(13-11-17-9-10-18-12-14-26-23(18)15-17)16-19-5-3-7-21-20(19)6-4-8-22(21)25-2;1-5(2,3)4/h4,6,8-10,12,14-15,19H,3,5,7,11,13,16H2,1-2H3;1H3,(H,2,3,4)/t19-;/m0./s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|
