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卤培米特

卤培米特用途

Halopemide 是一种有效的磷脂酶 D (PLD) 抑制剂,对人 PLD1 和 PLD2 的 IC50 分别为 220 和 310 nM。Halopemide 是多巴胺受体拮抗剂,是一种精神药物。

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卤培米特名称

[ CAS 号 ]:
59831-65-1

[ 中文名 ]:
卤培米特

[ 英文名 ]:
halopemide

[英文别名 ]:

Halopemidum
Halopemida
R 34,301
halopemide
Halopemide (USAN/INN)

卤培米特生物活性

[ 描述 ]:

Halopemide 是一种有效的磷脂酶 D (PLD) 抑制剂,对人 PLD1 和 PLD2 的 IC50 分别为 220 和 310 nM。Halopemide 是多巴胺受体拮抗剂,是一种精神药物。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> 磷脂

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

[ 靶点 ]

PLD1:220 nM (IC50)

PLD2:310 nM (IC50)

dopamine receptors

[体外研究]

氟哌啶醇(1-2μM；21天)影响转分化MOVAS细胞的钙化[3]。

[体内研究]

氟哌啶醇(10 mg/kg；p.o.)在大多数受试猴子中引起运动障碍[2]。

[参考文献]

[1]. Scott SA, et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol. 2009 Feb;5(2):108-17.

[2]. Neale R, et al. Acute dyskinesias in monkeys elicited by halopemide, mezilamine and the "antidyskinetic" drugs, oxiperomide and tiapride. Psychopharmacology (Berl). 1981;75(3):254-7.

[3]. Skafi N, et al. Phospholipase D: A new mediator during high phosphate-induced vascular calcification associated with chronic kidney disease. J Cell Physiol. 2019 Apr;234(4):4825-4839.

卤培米特物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 分子式 ]:
C₂₁H₂₂ClFN₄O₂

[ 分子量 ]:
416.876

[ 精确质量 ]:
416.141541

[ PSA ]:
70.13000

[ LogP ]:
4.47

[ 折射率 ]:
1.612

[ 储存条件 ]:
2-8°C

卤培米特MSDS

详细MSDS(安全技术说明书)

卤培米特安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 危险品运输编码 ]:
NONH for all modes of transport

卤培米特文献

CAY10593 inhibits the human P2X7 receptor independently of phospholipase D1 stimulation.

Purinergic Signal. 9(4) , 609-19, (2013)

The P2X7 receptor is a trimeric ATP-gated cation channel important in health and disease. We have observed that the specific phospholipase D (PLD)1 antagonist, CAY10593 impairs P2X7-induced shedding o...

Halopemide, a new psychotropic agent. Cerebral distribution and receptor interactions.

Pharm. Weekbl. Sci. 7(1) , 1-9, (1985)

Halopemide is a new psychotropic agent, a structural analogue of the neuroleptics of the butyrophenone type but with different pharmacological and clinical properties. Preliminary clinical findings in...

Dynamic cation-exchange systems for the separation of drugs derived from butyrophenone and diphenylpiperidine by high-performance liquid chromatography and applied in the determination of halopemide in plasma.

J. Chromatogr. A. 164(2) , 177-85, (1979)

Dynamic (solvent generated) cation-exchange systems for the separation of drugs and main metabolites derived from butyrophenone and diphenylpiperidine (haloperidol, pimozide, halopemide) were investig...

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