VU 0255035
Cat. No.:YN322161
产品名称: | VU 0255035 |
CAS No.: | 1135243-19-4 |
Chemical Name: | N-[3-oxo-3-[4-(4-pyridinyl)-1-piperazinyl]propyl]-2,1,3-benzothiadiazole-4-sulfonamide |
Synonyms: | VU 255035 |
分子量: | 432.5 |
分子式: | C18H20N6O3S2 |
SMILES: | O=C(CCNS(C1=CC=CC2=NSN=C21)(=O)=O)N(CC3)CCN3C4=CC=NC=C4 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | VU 0255035 是一种高度选择性、竞争性、可透过血脑屏障的毒蕈碱 M1 受体拮抗剂,IC50为 130 nM。VU 0255035 可减少毛果芸香碱诱导的小鼠癫痫发作。VU 0255035 用于检测 M1 受体在不同情况下的作用。 |
IC50和靶点: | |
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Sheffler, D.J., Williams, R., Bridges, T.M., et al.A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learningMol. Pharmacol.76(2),356-368(2009)
Weaver, C.D., Sheffler, D.J., Lewis, L.M., et al.Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probeCurr. Top. Med. Chem.9(13),1217-1226(2009)
Shirey, J.K., Brady, A.E., Jones, P.J., et al.A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learningJ. Neurosci.29(45),14271-14286(2009)
Xiang, Z., Thompson, A.D., Jones, C.K., et al.Roles of the M1 muscarinic acetylcholine receptor subtype in the regulation of basal ganglia function and implications for the treatment of Parkinson's diseaseJ. Pharmacol. Exp. Ther.340(3),595-603(2012)
Harada, K., Matsuoka, H., Miyata, H., et al.Identification of muscarinic receptor subtypes involved in catecholamine secretion in adrenal medullary chromaffin cells by genetic deletionBr. J. Pharmacol.172(5),1348-1359(2015)