MIDD0301是一种有效的正变构α5β3γ选择性GABAA受体(GABAAR)配体,EC50为17 nM。
产品描述
MIDD0301 is a potent positive allosteric α5β3γ selective GABAA receptor (GABAAR) ligand with EC50 of 17 nM.
体内活性
MIDD0301 did not reveal signs of general toxicity as determined by animal weight, organ weight or haematology after employing oral administration of mice twice daily with 100 mg/kg MIDD0301 mixed in peanut butter for 28 days [1]. Spleen and thymus weights were unchanged and the number of small intestine Peyer's patches was not affected in MIDD0301-treated mice.MIDD0301 treatment did not alter IgG antibody responses to dinitrophenyl following dinitrophenyl-keyhole limpet haemocyanin immunization [1]. MIDD0301 relaxed histamine-contracted guinea pig ( P< 0.05, n = 6-9) and human ( P< 0.05, n = 6-10) tracheal smooth muscle ex vivo in organ bath experiments, dilates mouse peripheral airways ex vivo in precision-cut lung-slice experiments ( P< 0.001, n = 16 airways from three mice), and alleviates bronchoconstriction in vivo in mice, as assessed by the forced-oscillation technique ( P< 0.05, n = 6 mice) [2].
Cas No.
2187489-08-1
分子式
C19H13BrFN3O2
分子量
414.23
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years