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化驗
≥98% (HPLC)
形狀
powder
顏色
off-white
溶解度
DMSO: >10 mg/mL
儲存溫度
2-8°C
SMILES 字串
Fc1ccc(cc1)C(=O)NCCN2CCC(CC2)N3C(=O)Nc4cc(Cl)ccc34
InChI
1S/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)
InChI 密鑰
NBHPRWLFLUBAIE-UHFFFAOYSA-N
應用
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.
生化/生理作用
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.
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Journal of chromatography, 164(2), 177-185 (1979-10-11)
Dynamic (solvent generated) cation-exchange systems for the separation of drugs and main metabolites derived from butyrophenone and diphenylpiperidine (haloperidol, pimozide, halopemide) were investigated. The effect of organic modifier, detergent, counter-ion concentration and of the pH on the retention has been
Archives internationales de pharmacodynamie et de therapie, 258(1), 51-59 (1982-07-01)
Halopemide inhibits 3H-BZ binding to crude and washed rat forebrain membranes with IC50 values of 16-25 microM. Its putative metabolites are considerably less active. The actions of halopemide are probably not directly related to its ability to interfere with high-affinity
Probe Reports from the NIH Molecular Libraries Program (2013-06-14)
A diversity-oriented synthesis approach of the neuroleptic drug halopemide, reported to be a phospholipase D2 (PLD2) inhibitor (but later shown to be a dual PLD1/2 inhibitor) afforded ML298 (CID 53393915), a potent, >53-fold PLD2 selective allosteric inhibitor (cellular PLD1, IC
Naunyn-Schmiedeberg's archives of pharmacology, 336(1), 16-19 (1987-07-01)
Apomorphine (0.05 mg/kg intravenously) was given to conscious dogs, and gastrin levels were measured in peripheral venous blood with a radioimmunoassay. Apomorphine induced an increase of gastrin levels which peaked at 5 min. The peripheral dopamine D-2/DA2 receptor antagonist domperidone
Probe Reports from the NIH Molecular Libraries Program (2013-06-14)
A diversity-oriented synthesis approach of the neuroleptic drug halopemide, reported to be a phospholipase D2 (PLD2) inhibitor (but later shown to be a dual PLD1/2 inhibitor) afforded ML299 (CID 56593087), a potent, dual PLD1/2 selective allosteric inhibitor (cellular PLD1, IC
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