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:
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
A Klegeris et al.
Biochemical pharmacology, 59(10), 1305-1314 (2000-03-29)
Peripheral benzodiazepine receptors (PBRs) are widely distributed throughout the body, but their functions are unknown. They are found on mononuclear phagocytes, and they are up-regulated in a number of neurological and other disease states. We explored the functional consequences of
Molecular basis of metabolism-mediated conversion of PK11195 from an antagonist to an agonist of the constitutive androstane receptor
Mackowiak B, et al.
Molecular Pharmacology, 92(1), 75-87 (2017)
Eryn L Werry et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 96, 186-192 (2016-10-28)
The 18kDa translocator protein (TSPO) is a target for novel glioblastoma therapies due to its upregulation in this cancer and relatively low levels of expression in the healthy cortex. The pyrazolo[1,5-a]pyrimidine acetamides, exemplified by DPA-713 and DPA-714, are a class
PBRL, a putative peripheral benzodiazepine receptor, in primitive erythropoiesis
Nakazawa F, et al.
Gene Expression Patterns, 9(2), 114-121 (2009)
Soria Iatmanen-Harbi et al.
International journal of molecular sciences, 20(6) (2019-03-25)
The optimization of translocator protein (TSPO) ligands for Positron Emission Tomography as well as for the modulation of neurosteroids is a critical necessity for the development of TSPO-based diagnostics and therapeutics of neuropsychiatrics and neurodegenerative disorders. Structural hints on the
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