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Halopemide

Product Name
Halopemide
CAS No.
59831-65-1
Chemical Name
Halopemide
Synonyms
R-34301;Halopemide;N-(2-(4-(5-Chloro-2-oxo-1-benzimidazolinyl)piperidino)ethyl)-p-fluorobenzamide;N-[2-[4-(5-chloro-2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]ethyl]-4-fluorobenzamide;N-[2-[4-(5-Chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)piperidino]ethyl]-4-fluorobenzamide;Benzamide, N-[2-[4-(5-chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-4-fluoro-;inhibit,psychotropic,calcification,MOVAS,Inhibitor,Halopemide,cells,dyskinesias,cancer,Phospholipase,Dopamine Receptor
CBNumber
CB61178881
Molecular Formula
C21H22ClFN4O2
Formula Weight
416.88
MOL File
59831-65-1.mol
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Halopemide Property

Density 
1.337±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: >10mg/mL
form 
powder
pka
11.10±0.30(Predicted)
color 
off-white
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Safety

Hazard Codes 
Xn
Risk Statements 
22
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
H3041
Product name
Halopemide
Purity
≥98% (HPLC)
Packaging
5mg
Price
$178
Updated
2024/03/01
Sigma-Aldrich
Product number
H3041
Product name
Halopemide
Purity
≥98% (HPLC)
Packaging
25mg
Price
$714
Updated
2024/03/01
Cayman Chemical
Product number
13205
Product name
Halopemide
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
13205
Product name
Halopemide
Purity
≥98%
Packaging
5mg
Price
$130
Updated
2024/03/01
Cayman Chemical
Product number
13205
Product name
Halopemide
Purity
≥98%
Packaging
10mg
Price
$235
Updated
2024/03/01
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Halopemide Chemical Properties,Usage,Production

Uses

Antipsychotic.

Uses

Halopemide acts as a small molecule inhibitor for phospholipase D (PLD), an important phosphlipid metabolism regulator which may be useful in the therapeutic treatment of Alzheimer’s Disease and other brain disorders.

Uses

Halopemide, a non-specific phospholipase D (PLD) antagonist, may be used with selective PLD antagonists (CAY10593, a PLD1 antagonist; CAY10594 or ML298, selective PLD2 antagonist) to help define the role and physiological effects regulated by phospholipase D enzymes. Halopemide may be used as the basis of the design and development of more selective PLD antagonists.

Biological Activity

halopemide is a phospholipase d (pld) inhibitor.phospholipase d (pld) is a key enzyme for the production of phosphatidic acid, a lipid second messenger. phosphatidic acid involves in both g protein-coupled receptor and receptor tyrosine kinase signal transduction networks.

Biochem/physiol Actions

Halopemide is a dopamine receptor antagonist and a phospholipase D2 inhibitor. Halopemide may be used as a screen to identify inhibitors of human PLD2 using an in vitro biochemical assay. It is also inhibitory at benzodiazepine binding sites.

in vitro

in a previous study, the ic50 of halopemide against pld2 was found to be similar to that previously reported, but the compound had no preference for pld2 over pld1 [1].

in vivo

animal study showed that the halopemide concentration in the rat brain was 10 times less than that of r29800, its chemical analog. however, the levels were the same in the pituitary gland. the highest level of halopemide was found to be in septal and thalamic areas while the neuroleptics were concentrated in the caudate nucleus. moreover, in the caudate nucleus, halopemide was far less particle-bound [2].

IC 50

220 and 310 nm for human pld1 and pld2, respectively

References

[1] scott, s. a.,selvy, p.e.,buck, j.r., et al. design of isoform-selective phospholipase d inhibitors that modulate cancer cell invasiveness. nature chemical biology 5(2), 108-117 (2009).
[2] loonen aj, van wijngaarden i, janssen pa, soudijn w. regional localization of halopemide, a new psychotropic agent, in the rat brain. eur j pharmacol. 1978 aug 15;50(4):403-8.
[3] de cuyper h, van praag hm, verstraeten d. the clinical significance of halopemide, a dopamine-blocker related to the butyrophenones. neuropsychobiology. 1984;12(4):211-6.

Halopemide Preparation Products And Raw materials

Raw materials

Preparation Products

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59831-65-1, HalopemideRelated Search:


  • Halopemide
  • N-[2-[4-(5-Chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)piperidino]ethyl]-4-fluorobenzamide
  • R-34301
  • N-(2-(4-(5-Chloro-2-oxo-1-benzimidazolinyl)piperidino)ethyl)-p-fluorobenzamide
  • N-[2-[4-(5-chloro-2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]ethyl]-4-fluorobenzamide
  • Benzamide, N-[2-[4-(5-chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-4-fluoro-
  • inhibit,psychotropic,calcification,MOVAS,Inhibitor,Halopemide,cells,dyskinesias,cancer,Phospholipase,Dopamine Receptor
  • 59831-65-1