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Haloperidol

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Chemical Structure| 52-86-8 同义名 : McN-JR 1625;R 1625;Aloperidol;Aloperidin;Serenace;Eukystol;Haldol;HSDB-3093;NSC 615296;NSC 170973
CAS号 : 52-86-8
货号 : A171381
分子式 : C21H23ClFNO2
纯度 : 98%
分子量 : 375.86
MDL号 : MFCD00051423
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(279.36 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:

10% DMSO+corn oil 5 mg/mL

生物活性
描述 Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic. Haloperidol (1 mg) intra-arterially attenuated the dopamine-induced pancreatic secretion. Haloperidol (3 mg) completely inhibits the action of 10 μg of dopamine in the pancreas of the dogs[1]. Large doses of haloperidol can safely be given intravenously and intramuscularly for rapid neuroleptisation; the bioavailability of this agent administered orally ranges from 60 to 65%[3]. The CNS delivery of major fraction of haloperidol via direct transnasal to brain pathway that can be a promising alternative to oral and parenteral routes in chronic and acute situations. Haloperidol concentration of 275.6 ng/g brain 8h post intranasal instillation, higher than therapeutic concentration range of haloperidol (0.8 to 5.15 ng/ml), suggests possible sustained delivery of the drug through nasal route[4]. Moreover, 0.5 mg haloperidol (i.v.) increased latent inhibition in one of two visual tasks. In the task where 0.5 mg haloperidol had enhanced latent inhibition, 1.0 mg had the same effect. In the task where 0.5 mg haloperidol had been ineffective, 1.0 mg haloperidol enhanced latent inhibition in high schizotypal subjects only. Thus, a dose dependence of haloperidol's effects on latent inhibition that parallels results from animal work[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.30mL

2.66mL

1.33mL

26.61mL

5.32mL

2.66mL

参考文献

[1]Furuta Y, Hashimoto K, Iwatsuki K, Takeuchi O. Effects of enzyme inhibitors of catecholamine metabolism and of haloperidol on the pancreatic secretion induced by L-DOPA and by dopamine in dogs. Br J Pharmacol. 1973;47(1):77‐84

[2]Shah NS, Shah KR, et al. Effects of chlorpromazine and haloperidol on the disposition of mescaline-14C in mice. J Pharmacol Exp Ther. 1973 Aug;186(2):297-304.

[3]Froemming JS, Lam YW, Jann MW, Davis CM. Pharmacokinetics of haloperidol. Clin Pharmacokinet. 1989;17(6):396‐423

[4]El-Setouhy DA, Ibrahim AB, Amin MM, Khowessah OM, Elzanfaly ES. Intranasal haloperidol-loaded miniemulsions for brain targeting: Evaluation of locomotor suppression and in-vivo biodistribution. Eur J Pharm Sci. 2016;92:244‐254

[5]Williams JH, Wellman NA, Geaney DP, Feldon J, Cowen PJ, Rawlins JN. Haloperidol enhances latent inhibition in visual tasks in healthy people. Psychopharmacology (Berl). 1997;133(3):262‐268