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Merck
CN

C0424

PK 11195

peripheral benzodiazepine antagonist, powder

Synonym(s):

1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide

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About This Item

Empirical Formula (Hill Notation):
C21H21ClN2O
CAS Number:
85532-75-8
Molecular Weight:
352.86
MDL number:
MFCD00069334
UNSPSC Code:
12352200
PubChem Substance ID:
24278822
NACRES:
NA.77

Key Documents

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Product Name

PK 11195,

form

powder

Quality Level

200

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

Gene Information

human ... BZRAP1(9256), TSPO(706)
rat ... Gabra2(29706), Tspo(24230)

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Application

PK 11195 has been used as an inhibitor of peripheral benzodiazepine receptor (PBR) homologs in primitive erythrocytes of embryos and in osteosarcoma cytoplasmic hydrids. It has also been used as an unlabelled competitive binder in in vitro autoradiography experiments in cardiac tissue sections.

Biochem/physiol Actions

PK 11195 is a peripheral benzodiazepine antagonist. It is also an antagonist for human constitutive androstane receptor (hCAR) and human pregnane X receptor (PXR). In human primary hepatocytes, PK 11195 upon demethylation elicits agonist functionality towards the receptor hCAR. PK 11195 also antagonise B-cell lymphoma 2 (Bcl-2) and may serve as a potential compound for mitochondrial targeting therapies and in the treatment of cholangiocarcinoma.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000397927
0000397927
0000200561
0000145489
0000200561

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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)
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)
Justin V Louis et al.
Neuropharmacology, 118, 167-174 (2017-03-21)
Adaptor-associated kinase 1 (AAK1), a member of the Ark1/Prk1 family of serine/threonine kinases, plays a role in modulating clatherin coated endocytosis of specific surface receptors. We have demonstrated that AAK1 inhibitors are efficacious in rodent models of neuropathic pain (Kostich
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