C0424
PK 11195
peripheral benzodiazepine antagonist, powder
别名:
1-（2-氯苯基）-N-甲基-N-（1-甲基丙基）-3-异喹啉羧
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关于此项目
经验公式（希尔记法）:
C21H21ClN2O
化学文摘社编号:
分子量:
352.86
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Form:
powder
Quality level:
产品名称
PK 11195,
SMILES string
CCC(C)N(C)C(=O)c1cc2ccccc2c(n1)-c3ccccc3Cl
InChI
1S/C21H21ClN2O/c1-4-14(2)24(3)21(25)19-13-15-9-5-6-10-16(15)20(23-19)17-11-7-8-12-18(17)22/h5-14H,4H2,1-3H3
InChI key
RAVIZVQZGXBOQO-UHFFFAOYSA-N
form
powder
Quality Level
Gene Information
human ... BZRAP1(9256), TSPO(706)
rat ... Gabra2(29706), Tspo(24230)
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相关类别
Application
PK 11195 已被用作胚胎原始红细胞和骨肉瘤细胞质杂交体中外周苯二氮卓受体（PBR）类似物的抑制剂。它还被用作心脏组织切片体外放射自显影实验中的未标记竞争性结合剂。
Biochem/physiol Actions
PK 11195是一种外周苯二氮卓拮抗剂。它还是人组成型雄烷受体（hCAR）和人孕烷 X 受体（PXR）的拮抗剂。在人原代肝细胞中，PK 11195通过反甲基化诱导对受体hCAR的激动剂功能。PK 11195还是B细胞淋巴瘤2（Bcl-2）的拮抗剂，有望成为线粒体靶向治疗和肝胆管型肝癌治疗的化合物。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
M Okubo et al.
European journal of pharmacology, 359(2-3), 243-249 (1998-12-01)
This study examined the influence of benzodiazepine receptors on amylase release from rat parotid acinar cells. Diazepam (10(-8)-10(-6) M), which is a potent agonist of both central- and peripheral-type benzodiazepine receptors, dose dependently decreased amylase release induced by isoprenaline and
A S Hazell et al.
Neuroscience letters, 271(1), 5-8 (1999-09-02)
Alterations of 'peripheral-type' benzodiazepine receptors (PTBRs) in brain are a feature of hepatic encephalopathy (HE). Although ammonia toxicity has been implicated in the disorder, recent findings suggest an accumulation of manganese in the brains of cirrhotic patients dying in hepatic
Pk11195, a mitochondrial benzodiazepine receptor antagonist, reduces apoptosis threshold in Bcl-XL and Mcl-1 expressing human cholangiocarcinoma cells
Okaro AC, et al.
Gut, 51(4), 556-561 (2002)
18-kDa translocator protein ligand 18 F-FEMPA: biodistribution and uptake into atherosclerotic plaques in mice
Hellberg S, et al.
Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology, 24(3), 862-871 (2017)
E P Wala et al.
Pharmacological research, 41(4), 461-468 (2000-03-08)
In spite of the extensive use of the peripheral benzodiazepine (BZ) receptor antagonist, PK 11195 (PK), in pharmacological studies, there is a lack of information of its pharmacokinetics in the rat. In this study the pharmacokinetics of PK were determined
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