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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
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].
Haloperidol/氟哌啶醇 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human iPSC-derived hippocampal granule cells
10 ng/mL (0.003 µM) and 100 ng/mL (0.03 µM)
10 days
To assess the effect of Haloperidol on neurite outgrowth. Results showed that low concentration Haloperidol significantly promoted neurite outgrowth and arborization but had an inhibitory effect on cell number.
Biomolecules. 2024 Jun 13;14(6):688.
Peritoneal macrophages
10 µM
24 hours
To evaluate the effect of haloperidol on macrophage cholesterol efflux function. Results showed that haloperidol decreased ABCA1 mRNA expression (54%) and reduced cholesterol efflux to apolipoprotein A1 (30%).
Br J Pharmacol. 2015 May;172(9):2397-405.
Human pulmonary artery endothelial cells
10 µM
24 hours
To assess the effect of haloperidol on endothelial cell barrier function, results showed that haloperidol significantly attenuated thrombin-induced barrier disruption.
Cells. 2021 Aug 25;10(9):2186.
Human pulmonary artery endothelial cells
0.1-10 µM
24 hours
To assess the effect of haloperidol on tight junction protein expression, results showed that haloperidol significantly increased claudin-5, occludin, and ZO-1 expression levels.
Cells. 2021 Aug 25;10(9):2186.
Human plasma
10 ng/ml
24 hours
To evaluate the effect of haloperidol alone or in combination with lithium on oxidative stress parameters (TBARS and TAC) in human plasma. Results showed that haloperidol alone did not significantly alter TBARS levels, but when combined with lithium, it significantly increased TBARS levels.
Redox Rep. 2016 Jan;21(1):45-49.
MHippoE-2 cells
0.1 µM and 10 µM
24, 48, and 72 hours
HAL and OLA dose- and time-dependently suppressed cells’ proliferation and shortened the length of the cells’ projections. 10 µM OLA exhibited the most pronounced effect.
Int J Mol Sci. 2022 Jul 12;23(14):7711.
Human Endometrial Epithelial Cells (HEECs)
100 µM
28 days
Haloperidol promoted cellular transformation of HEECs, as evidenced by increased colony formation in soft agar.
Cancers (Basel). 2022 Jun 23;14(13):3089.
Human iPSC-derived neural progenitor cells
10 ng/mL (0.003 µM) and 100 ng/mL (0.03 µM)
3 days
To evaluate the effect of antipsychotics on the proliferation of neural progenitor cells. Results showed that Haloperidol did not significantly alter the proliferation rate of neural progenitor cells.
Biomolecules. 2024 Jun 13;14(6):688.
Rat brain synaptosomes
0.005 – 0.5 µM
3 min
Investigate the uptake mechanism of haloperidol in rat brain synaptosomes. Results showed a temperature-, sodium ion-, and energy-dependent process with high affinity (Km≈40 nM) and low capacity (Vmax=2.37 pmol mg−1 protein min−1).
Br J Pharmacol. 2003 Jan;138(1):188-92.
Human Endometrial Carcinoma Cells (HECCs)
10 µM
48 hours
Haloperidol promoted malignant progression of HECCs, including enhanced cell proliferation, migration, and invasion capabilities.
Cancers (Basel). 2022 Jun 23;14(13):3089.
Haloperidol/氟哌啶醇 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
Rat catalepsy model
Subcutaneous injection
0.05–1 mg/kg
Single dose, measured after 90 minutes
To investigate the effect of Haloperidol in combination with D9-THC on rat catalepsy, results showed that D9-THC enhanced Haloperidol-induced catalepsy.
Br J Pharmacol. 2003 Oct;140(3):520-6
LDL receptor knockout mice
Hyperlipidemia model
Subcutaneous implantation
0.125 mg/day
5 weeks
To evaluate the effect of haloperidol on atherosclerotic lesion development. Results showed that haloperidol significantly reduced atherosclerotic lesion size (31%) and decreased macrophage chemotactic protein-1 (MCP-1) expression and secretion.
Br J Pharmacol. 2015 May;172(9):2397-405.
Long-Evans rats
Adult and adolescent male and female rats
Intraperitoneal injection
0.3 mg/kg
Twice daily for 10 days
To evaluate the effects of sub-chronic haloperidol treatment on Δ9-THC-induced suppression of activity, hypothermia, and catalepsy. Results showed that in adult male rats, haloperidol enhanced Δ9-THC-mediated suppression of activity and hypothermia, but similar effects were not observed in adult female or adolescent rats
Neuropharmacology. 2008 Dec;55(7):1183-90
Sprague-Dawley rats
MK-801-induced animal schizophrenia model
Intraperitoneal injection
1 mg/kg
Once daily for 7 days
HAL and OLA suppressed the expression of DCX and NeuN genes in the HIP and SVZ. In the MK-801-induced schizophrenia model, OLA reversed the inhibitory effect of MK-801 on DCX and NeuN, while HAL only reversed the effect on DCX.
Int J Mol Sci. 2022 Jul 12;23(14):7711.
Wistar rats
Haloperidol-induced Parkinson's disease model
Intraperitoneal injection
1 mg/kg
Single dose
To evaluate the pharmacodynamic activity of lipid nanoparticles and hydrogel formulations in haloperidol-induced Parkinson's disease model. Results showed that haloperidol-induced PD model exhibited significantly increased lipid peroxidation levels and decreased glutathione, catalase activity, and dopamine levels. Lipid nanoparticles and hydrogel formulations significantly restored these biochemical parameters.
Pharmaceutics. 2020 May 13;12(5):448
C57BL/6J mice
Ovariectomy model
Oral
2 mg/kg
Once daily for 28 days
Haloperidol at clinically relevant doses induced endometrial hyperplasia in normal mice and promoted tumor growth and malignancy in mice with orthotopic EC.
Cancers (Basel). 2022 Jun 23;14(13):3089.
Swiss albino mice
No specific disease model mentioned
Oral and transdermal administration
33.3 mg
Single dose, observation up to 48 hours
To evaluate the distribution of Haloperidol in blood and brain after transdermal administration. Results showed that transdermal administration had a more sustained release pattern and higher brain drug concentration compared to oral administration.
To assess the protective effect of haloperidol on acute lung injury, results showed that haloperidol pretreatment significantly increased lung claudin-5 expression and reduced lung injury.
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