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201943-63-7

中文名稱 (2S)-2-氨基-2-[(1S,2S)-2-羧基環(huán)丙-1-基]-3-(噸-9-基)丙酸
英文名稱 LY 341495
CAS 201943-63-7
分子式 C20H19NO5
分子量 353.37
MOL 文件 201943-63-7.mol
201943-63-7 結(jié)構(gòu)式 201943-63-7 結(jié)構(gòu)式

基本信息

中文別名
(2S)-2-氨基-2-[(1S,2S)-2-羧基環(huán)丙-1-基]-3-(噸-9-基)丙酸
(ALPHAS)-ALPHA-氨基-ALPHA-[(1S,2S)-2-羧基環(huán)丙基]-9H-噸-9-丙酸
英文別名
CS-416
LY 341495
LY 341495
LY-341495
9H-Xanthene-9-propanoic acid, α-amino-α-[(1S,2S)-2-carboxycyclopropyl]-, (αS)-
(2S)-2-AMINO-2-[(1S,2S)-2-CARBOXYCYCLOPROP-1-YL]-3-(XANTH-9-YL) PROPANOIC ACID
(alphaS)-alpha-Amino-alpha-[(1S,2S)-2-carboxycyclopropyl]-9H-xanthene-9-propanoic acid
(1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropane-1-carboxylic acid
(alphaS)-alpha-Amino-alpha-[(1S,2S)-2-carboxycyclopropyl]-9H-xanthene-9-propanoic acid LY 341495
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)580.8±40.0 °C(Predicted)
密度1.432
儲(chǔ)存條件Store at RT
溶解度Limited solubility, soluble in DMSO
酸度系數(shù)(pKa)2.02±0.10(Predicted)
形態(tài)結(jié)晶固體
顏色White to off-white

常見(jiàn)問(wèn)題列表

生物活性
LY341495 是代謝型谷氨酸受體 (mGluR) 拮抗劑,對(duì) mGlu2,mGlu3,mGlu1a,mGlu5a,mGlu8,mGlu7 和 mGlu4 受體的 IC50 分別為 21 nM,14 nM,7.8 μM,8.2 μM,170 nM,990 nM 和 22 μM。
靶點(diǎn)

mGluR1a

7.8 μM (IC 50 )

mGluR2

21 nM (IC 50 )

mGluR3

14 nM (IC 50 )

mGluR4

22 μM (IC 50 )

mGluR5a

8.2 μM (IC 50 )

mGluR7

990 nM (IC 50 )

mGluR8

170 nM (IC 50 )

體內(nèi)研究

LY341495 (0.3, 1, and 3 mg/kg, i.p.) displays a lower level of discrimination in rats. LY341495 (3.0 mg/kg) decreases Dvl-2, pGSK-3α/β and β-catenin protein levels but Dvl-1, Dvl-3 and GSK-3α/β are unaffected in both the PFC and STR. LY341495 has the generally the opposite effect following acute and chronic administration compared to mGlu2/3 agonist, LY379268. LY341495 (3 mg/kg, i.p., 2.5 h) -induced c-Fos expression is not altered in either KO brain. LY341495 is almost inactive in the central extended amygdala [central nucleus of the amygdala, lateral (CeL) and bed nucleus of the stria terminalis, laterodorsal (BSTLD)] in mGluR3-KO mice.

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