產(chǎn)品目錄

規(guī)格	5mg 10mg 25mg 50mg
CAS	211311-95-4
別名	N/A
化學(xué)名	N/A
分子式	C19H22N2O2S
分子量	342.5
溶解度	DMF: 15mg/mL,DMSO: 15mg/mL,DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL,Ethanol: 3mg/mL
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

LY404187 is a benzothiadiazide positive allosteric modulator of AMPA receptors.1 It increases glutamate-induced activation of GluR1i, -2i, -2o, -3i, and -4i subunit-containing AMPA receptors with EC50 values of 5.65, 0.15, 1.44, 1.66, and 0.21 μM, respectively, in a calcium influx assay. LY404187 is selective for these AMPA receptors over GluR6 subunit-containing kainate receptors at 10 μM. LY404187 increases currents induced by glutamate and AMPA in rat prefrontal cortex pyramidal neurons (EC50s = 1.3 and 1.2 μM, respectively) but not in AMPA-stimulated primary rat embryonic hippocampal or primary cerebellar Purkinje neurons.2,3 LY404187 prevents decreases in the number of dopaminergic neurons in the substantia nigra induced by MPTP and 6-OHDA in mouse and rat, respectively, models of Parkinson's disease when administered at a dose of 0.5 mg/kg per day.4

|1. Miu, P., Jarvie, K.R., Radhakrishnan, V., et al. Novel AMPA receptor potentiators LY392098 and LY404187: Effects on recombinant human AMPA receptors in vitro. Neuropharmacology 40(8), 976-983 (2001).|2. Baumbarger, P.J., Muhlhauser, M., Zhai, J., et al. Positive modulation of α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors in prefrontal cortical pyramidal neurons by a novel allosteric potentiator. J. Pharmacol. Exp. Ther. 298(1), 86-102 (2001).|3. Gates, M., Ogden, A., and Bleakman, D. Pharmacological effects of AMPA receptor potentiators LY392098 and LY404187 on rat neuronal AMPA receptors in vitro. Neuropharmacology 40(8), 984-991 (2001).|4. O'Neill, M.J., Murray, T.K., Whalley, K., et al. Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease. Eur. J. Pharmacol. 486(2), 163-174 (2004).

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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