| Size | Price | Stock | Qty |
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| 50mg |
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DSP-4 hydrochloride (Neurotoxin DSP 4) is a novel, potent, BBB-penetrant and highly selective neurotoxin with neurotoxic effects on noradrenergic neurons of adult and developing rats. It can block the uptake of noradrenaline.
| Targets |
- DSP-4 hydrochloride (N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine hydrochloride) is a selective neurotoxin targeting noradrenergic neurons, acting via the norepinephrine transporter (NET) to induce neuronal damage[1,2]
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| ln Vivo |
Notwithstanding, DSP-4 hydrochloride (ip; 50 mg/kg; single dose) demolishes LC fibers and neurons [1].
- Impairment of locus coeruleus (LC)-inferior colliculus (IC) noradrenergic projections in adult rats: Adult Sprague-Dawley rats received a single intraperitoneal injection of DSP-4 hydrochloride (50 mg/kg). Seven days post-treatment, immunohistochemical staining showed a 75% reduction in tyrosine hydroxylase (TH)-positive noradrenergic fibers in the IC (a marker of noradrenergic projections from the LC). High-performance liquid chromatography (HPLC) analysis revealed an 80% decrease in norepinephrine (NE) content in the IC compared to the vehicle control group (saline injection)[1] - Neurotoxicity in adult and developing rats: In adult Wistar rats, intraperitoneal injection of DSP-4 hydrochloride (25–50 mg/kg) caused a dose-dependent reduction in NE content in noradrenergic projection areas (e.g., cerebral cortex, hippocampus, IC). A 50 mg/kg dose reduced cortical NE by 70% and hippocampal NE by 65% 14 days post-treatment. In developing rats (1–7 days old), a lower dose (10 mg/kg, intraperitoneal) induced significant NE depletion (55% reduction in the brainstem) and TH-positive neuron loss, indicating higher sensitivity to the neurotoxin than adult rats[2] - Selectivity for noradrenergic neurons: DSP-4 hydrochloride (50 mg/kg, adult rats) had no significant effect on dopamine (DA) or serotonin (5-HT) content in the brain (HPLC analysis) and did not reduce TH-positive dopaminergic neurons or tryptophan hydroxylase (TPH)-positive serotonergic neurons, confirming selective toxicity to noradrenergic neurons[2] |
| Animal Protocol |
Animal/Disease Models: Rat[1]
Doses: 50 mg/kg Route of Administration: intraperitoneally (ip) (ip), single dose Experimental Results: Large projection neurons and optical fibers of LC were not observed. - Adult rat LC-IC projection impairment model: Adult male Sprague-Dawley rats (250–300 g) were randomly divided into 2 groups (n=6/group): 1) Vehicle control: single intraperitoneal injection of sterile saline (1 mL/kg); 2) DSP-4 hydrochloride group: single intraperitoneal injection of DSP-4 hydrochloride (50 mg/kg, dissolved in sterile saline, 1 mL/kg). Seven days after injection, rats were deeply anesthetized, transcardially perfused with 4% paraformaldehyde, and brains were harvested for immunohistochemical staining (TH antibody) and HPLC analysis of NE content in the IC[1] - Adult and developing rat neurotoxicity model: 1) Adult male Wistar rats (200–250 g): divided into 4 groups (n=5/group) receiving single intraperitoneal injections of saline, 10 mg/kg, 25 mg/kg, or 50 mg/kg DSP-4 hydrochloride. 2) Developing rats (1, 3, 7 days old): divided into 2 groups (n=5/group) receiving saline or 10 mg/kg DSP-4 hydrochloride (intraperitoneal). Rats were sacrificed 1, 7, or 14 days post-treatment; brains were dissected into regions (cortex, hippocampus, brainstem, IC), and NE, DA, and 5-HT contents were measured by HPLC[2] |
| Toxicity/Toxicokinetics |
Selective neurotoxicity: At therapeutic doses (10–50 mg/kg, intraperitoneal), DSP-4 hydrochloride specifically damages norepinephrine neurons without affecting dopaminergic or serotonergic neurons [2]. - Age-dependent toxicity: Developing rats (newborn to 1 week old) are 3–5 times more sensitive to DSP-4 hydrochloride than adult rats; a dose of 10 mg/kg can induce significant norepinephrine depletion in newborn rats, while adult rats require a dose of ≥25 mg/kg to achieve a similar effect [2]. - Systemic toxicity: During a 14-day observation period, adult rats treated with DSP-4 hydrochloride (up to 50 mg/kg, intraperitoneal) did not exhibit significant systemic toxicity (e.g., weight loss <5%, no somnolence or organ damage) [1,2].
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| References |
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| Additional Infomation |
See also: DSP-4 (note moved to). DSP-4 hydrochloride is a widely used research tool for studying the function of the central noradrenergic system, particularly projections derived from the locus coeruleus, through selective ablation of noradrenergic neurons [1,2]. Its neurotoxic mechanism is thought to involve noradrenergic neurons taking up DSP-4 via the norepinephrine transporter (NET), subsequently forming cytotoxic metabolites that induce oxidative stress and neuronal apoptosis [2].
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| Molecular Formula |
C11H15NCLBR.HCL
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| Molecular Weight |
313.06144
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| Exact Mass |
310.984
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| CAS # |
40616-75-9
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| Related CAS # |
40616-75-9 (HCl); 62078-98-2;
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| PubChem CID |
11957497
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| Appearance |
White to off-white solid powder
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| Density |
1.338g/cm3
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| Boiling Point |
276.7ºC at 760 mmHg
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| Index of Refraction |
1.551
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| LogP |
4.311
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
15
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| Complexity |
154
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NDDRNRRNYOULND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H15BrClN.ClH/c1-2-14(8-7-13)9-10-5-3-4-6-11(10)12;/h3-6H,2,7-9H2,1H3;1H
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| Chemical Name |
N-[(2-bromophenyl)methyl]-2-chloro-N-ethylethanamine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~399.28 mM)
H2O : ~50 mg/mL (~159.71 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (159.71 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1943 mL | 15.9714 mL | 31.9428 mL | |
| 5 mM | 0.6389 mL | 3.1943 mL | 6.3886 mL | |
| 10 mM | 0.3194 mL | 1.5971 mL | 3.1943 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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