192927-92-7
192927-92-7 結(jié)構(gòu)式
基本信息
中文別名
化合物L(fēng)Y3107621-(2-(4-(4-氟苯甲?；?哌啶-1-基)乙基)-3,3-二甲基吲哚啉-2-酮鹽酸鹽
1-[2-[4-(4-氟苯甲酰基)-1-哌啶基]乙基]-1,3-二氫-3,3-二甲基-2H-吲哚-2-酮鹽酸鹽
英文別名
CS-195LY 310762 HCl
LY310762
LY-310762
LY310762 USP/EP/BP
LY-310,762 HYDROCHLORIDE
1-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-3,3-dimethylindol-2-one
1-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-3,3-dimethylindol-2-one,hydrochloride
1-(2-(4-(4-fluorobenzoyl)piperidin-1-yl)ethyl)-3,3-diMethylindolin-2-one Hydrochloride
1-[2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl]-1,3-dihydro-3,3-dimethyl-2H-indol-2-onehydrochloride
3,3-Dimethyl-1-{2-[4-(4-fluorobenzoyl)-1-piperidinyl]-1-ethyl}-1,3-dihydro-2H-indol-2-one hydrochloride
所屬類別
生物化工：5-HT Receptor 拮抗劑物理化學(xué)性質(zhì)
儲存條件Desiccate at RT
儲存條件Sealed in dry,Room Temperature
溶解度DMSO: 10 mg/mL with heating, soluble
溶解度DMSO：可溶10 mg/mL 加熱
形態(tài)white powder
顏色White to off-white
CAS 數(shù)據(jù)庫192927-92-7
常見問題列表
生物活性
LY310762是一種5-HT1D受體拮抗劑，Ki為249 nM，對5-HT1B受體具有較低的親和力。體外研究
LY310762 has a higher affinity for the guinea pig 5-HT1D receptor than for the 5-HT1B receptor. LY310762 potentiates the potassium-induced [3H]5-HT outflow from guinea pig cortical slices with an EC50 of 30 nM. The maximum potentiation of the potassium-induced outflow which is obtained with LY310762 is about 40%. LY310762 blocks the decreased EPSC amplitude induced by Sumatriptan.體內(nèi)研究
Systemic administration of LY310762 (10 mg/kg i.p.) produces a further significant enhancement in the 5-HT response to fluoxetine (20 mg/kg i.p.) when compared to animals receiving a control vehicle injection. In fluoxetine treated animals, levels of 5-HT increases from 312±43% to a maximum of 683% after LY310762. In control animals, levels of 5-HT remains unchanged (250%). LY310762 administered alone also significantly increases basal levels of 5-HT above vehicle controls, reaching a maximum of 258% compared to the pre-injection control.靶點(diǎn)
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5-HT 1D Receptor 249 nM (Ki) |