Purity: ≥98%
| Targets |
Octodrine hydrochloride targets the central nervous system as a stimulant. It increases the uptake of dopamine and noradrenaline, enhancing catecholaminergic neurotransmission. This leads to increased pain threshold, positive chronotropic effects (increased heart rate), and positive inotropic effects (increased myocardial contractility). The compound also functions as a local anesthetic and vasoconstrictor.
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| ln Vitro |
Octodrine is the trade name for Dimethylhexylamine (DMHA), a central nervous stimulant that increases the uptake of dopamine and noradrenaline. Originally developed as a nasal decongestant in the 1950's, it has recently been re-introduced on the market as a pre-workout and 'fat-burner' product but its use remains unregulated. Our work provides the first observational cross-sectional analytic study on Octodrine as a new drug trend and its associated harms after a gap spanning seven decades [2].
In vitro, Octodrine hydrochloride is a central nervous system activator that increases the uptake of dopamine and noradrenaline. It is found to increase the pain threshold, cardiac rate, and myocardial contractility. The compound is a local anesthetic and vasoconstrictor, but is mainly used as a pharmaceutical intermediate of octamylamine. Its effects on neurotransmitter uptake have been characterized in various in vitro systems. |
| ln Vivo |
Local anesthesia is produced by tropical application of solutions of the hydrochloride or free base of 2-Amino-6-methylheptane to rabbit's eyes. Intravenously in dogs anesthetized with pentobarbital sodium, 2-Amino-6-methylheptane hydrochloride exhibits 1/500-1/1000 the pressor activity of epinephrine. 2-Amino-6-methylheptane hydrochloride is found to cause an increase in cardiac rate and amplitude of contraction. Intravenously in dogs, anesthetized with pentobarbital sodium, doses of 0.5 to 1.0 mg per kilogram of body weight of 2-Amino-6-methylheptane hydrochloride has no detectable effect on the small intestine, detrusor of the urinary bladder, urine secretion or respiration. Intraperitoneally in rats, 2-Amino-6-methylheptane hydrochloride is found to be almost entirely devoid of a central nervous system stimulating action in non-toxic doses. No histological evidence of irritation of the tracheo-bronchial tree mucosa is noted in rabbits or rats which inhale 2-Amino-6-methylheptane free base daily for 10 and 30 days respectively[1].
In vivo, Octodrine hydrochloride is a central nervous system stimulant that enhances the uptake of dopamine and norepinephrine. It elevates pain thresholds and produces positive chronotropic and inotropic effects on the heart. Local anesthesia is produced by topical application of solutions of the hydrochloride or free base. The compound is used as a pharmaceutical intermediate and has been studied for its stimulant and cardiovascular effects. |
| Enzyme Assay |
In vitro transporter assays for Octodrine hydrochloride involve measuring dopamine and noradrenaline uptake inhibition. Dopamine transporter (DAT) and noradrenaline transporter (NET) activity are assessed by measuring the uptake of radiolabeled substrates into synaptosomes or cells expressing the transporters. The compound's effects on uptake are quantified. For cardiovascular studies, cardiac myocytes are treated with the compound and contractility is assessed. Assays are performed in appropriate buffer systems with positive controls such as known stimulants.
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| Cell Assay |
In vitro cell-based assays for Octodrine hydrochloride are conducted in neuronal cell lines and cardiac myocytes. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Dopamine and noradrenaline uptake are assessed using radiolabeled substrates. Cardiac contractility is assessed in cardiomyocyte models. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
Octodrine hydrochloride in vivo studies are conducted in animal models for cardiovascular and neurological research. Animals are treated with the compound via oral administration or injection. Heart rate and myocardial contractility are monitored. Pain threshold is assessed using standard pain models. For pharmacokinetic studies, blood samples are collected for analysis. Local anesthetic effects are assessed by topical application. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biochemical analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Octodrine hydrochloride (MW 165.70 g/mol, C8H20ClN) is a central nervous system stimulant. It is also known as 2-Amino-6-methylheptane hydrochloride, 1,5-dimethyl Hexylamine, and NSC 27116. The compound is soluble in water and other appropriate solvents. It is stable under recommended storage conditions. Octodrine hydrochloride is primarily used as a pharmaceutical intermediate. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies.
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| Toxicity/Toxicokinetics |
Octodrine hydrochloride is generally well-tolerated at therapeutic doses. The compound is a central nervous system stimulant with cardiovascular effects. It increases heart rate and myocardial contractility. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| References |
[1]. Fellows EJ, et al. The pharmacology of 2-amino-6-methylheptane. J Pharmacol Exp Ther. 1947 Aug;90(4):351-8.
[2]. Octodrine: New Questions and Challenges in Sport Supplements. Brain Sci. 2018 Feb; 8(2): 34. |
| Additional Infomation |
Octodrine hydrochloride (2-Amino-6-methylheptane hydrochloride) is a central nervous system stimulant that increases dopamine and noradrenaline uptake. It increases pain threshold, heart rate (positive chronotropic effect), and myocardial contractility (positive inotropic effect). The compound also functions as a local anesthetic and vasoconstrictor, primarily used as a pharmaceutical intermediate. All applications are limited to non-human research use.
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| Molecular Formula |
C8H19N.HCL
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|---|---|
| Molecular Weight |
165.7041
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| Exact Mass |
165.128
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| CAS # |
5984-59-8
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| Related CAS # |
Octodrine;543-82-8
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| PubChem CID |
521901
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| Appearance |
White to off-white solid
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| Boiling Point |
155ºC at 760 mmHg
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| Melting Point |
139-140 ºC
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| Flash Point |
48.9ºC
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| LogP |
3.662
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
10
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| Complexity |
59.6
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(N)CCCC(C)C.[H]Cl
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| InChi Key |
JWQWFYMPBWLERY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H19N.ClH/c1-7(2)5-4-6-8(3)9;/h7-8H,4-6,9H2,1-3H3;1H
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| Chemical Name |
6-methylheptan-2-amine;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 : ~100 mg/mL (~603.50 mM)
H2O : ≥ 50 mg/mL (~301.75 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.09 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 25.0 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: ≥ 2.5 mg/mL (15.09 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 25.0 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: ≥ 2.5 mg/mL (15.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.0350 mL | 30.1750 mL | 60.3500 mL | |
| 5 mM | 1.2070 mL | 6.0350 mL | 12.0700 mL | |
| 10 mM | 0.6035 mL | 3.0175 mL | 6.0350 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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