59831-65-1 Usage
Uses
Used in Pharmaceutical Industry:
Halopemide is used as an antipsychotic agent for the treatment of various mental health disorders. Its antipsychotic properties make it a valuable asset in managing symptoms and improving the quality of life for patients.
Used in Alzheimer's Disease Treatment:
Halopemide acts as a small molecule inhibitor for phospholipase D (PLD), which may be useful in the therapeutic treatment of Alzheimer's Disease and other brain disorders. By targeting PLD, Halopemide has the potential to help regulate phospholipid metabolism and contribute to the management of these conditions.
Used in Research and Development:
Halopemide, as a non-specific phospholipase D (PLD) antagonist, may be used in combination 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. This application aids in the understanding of PLD's function and the development of more selective PLD antagonists for targeted treatments.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 59831-65-1 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 5,9,8,3 and 1 respectively; the second part has 2 digits, 6 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 59831-65:
(7*5)+(6*9)+(5*8)+(4*3)+(3*1)+(2*6)+(1*5)=161
161 % 10 = 1
So 59831-65-1 is a valid CAS Registry Number.
InChI:InChI=1/C21H22ClFN4O2/c22-15-3-6-19-18(13-15)25-21(29)27(19)17-7-10-26(11-8-17)12-9-24-20(28)14-1-4-16(23)5-2-14/h1-6,13,17H,7-12H2,(H,24,28)(H,25,29)
