| Targets |
Adrenergic receptors and monoamine transporters. Octodrine increases the uptake of dopamine and noradrenaline. It binds to adrenergic receptors and stimulates the release of neurotransmitters such as dopamine and noradrenaline. The compound increases pain threshold, cardiac rate, and myocardial contractility.
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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].
Octodrine increases the uptake of dopamine and noradrenaline. It increases pain threshold, cardiac rate (positive chronotropic effect), and myocardial contractility (positive inotropic effect). The compound binds to adrenergic receptors and stimulates the release of neurotransmitters such as dopamine and noradrenaline. It is a central nervous system stimulant. |
| 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 acts as a central nervous system stimulant that increases pain threshold, cardiac rate, and myocardial contractility. It increases the uptake of dopamine and noradrenaline. The compound has been used as a stimulant and is the trade name for dimethylhexylamine (DMHA). Further in vivo studies are needed to fully characterize its effects. |
| Enzyme Assay |
In vitro receptor binding assays for octodrine involve measuring its affinity for adrenergic receptors and monoamine transporters using radioligand binding techniques. Membranes from cells expressing adrenergic receptors or monoamine transporters are incubated with radiolabeled ligands and increasing concentrations of octodrine. Bound and free ligand are separated by filtration, and radioactivity is measured.
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| Cell Assay |
In vitro cellular assays for octodrine involve treating neuronal cells with the compound and measuring dopamine or noradrenaline uptake. Cells are treated with various concentrations of octodrine, and neurotransmitter uptake is measured using radiolabeled tracers or fluorescent probes. The compound's ability to increase neurotransmitter uptake is assessed.
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| Animal Protocol |
In vivo animal studies for octodrine typically involve administration to rodent models to assess its stimulant effects, pain threshold, and cardiovascular effects. Octodrine increases pain threshold, cardiac rate, and myocardial contractility. Further studies are needed to fully characterize its in vivo effects and potential therapeutic applications.
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| ADME/Pharmacokinetics |
Octodrine has a molecular weight of 129.24 and a molecular formula of C8H19N. It is a central nervous system stimulant. The compound is the trade name for dimethylhexylamine (DMHA). Further pharmacokinetic studies are needed to fully characterize its absorption, distribution, metabolism, and elimination.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of octodrine are limited. The compound is a central nervous system stimulant that increases dopamine and noradrenaline uptake. It should be used with caution due to its stimulant effects. Comprehensive toxicological evaluation is needed for any potential therapeutic applications.
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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.
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| Additional Infomation |
Octodrine is an alkylamine.
Octodrine (2-amino-6-methylheptane, DMHA) is a central nervous system stimulant that increases the uptake of dopamine and noradrenaline. It increases pain threshold, cardiac rate (positive chronotropic effect), and myocardial contractility (positive inotropic effect). Octodrine interacts with adrenergic receptors and monoamine transporters. It is a research compound for studying neurotransmitter uptake and stimulant effects. |
| Molecular Formula |
C8H19N
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|---|---|
| Molecular Weight |
129.24
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| Exact Mass |
129.151
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| Elemental Analysis |
C, 74.34; H, 14.82; N, 10.84
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| CAS # |
543-82-8
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| Related CAS # |
Octodrine hydrochloride;5984-59-8
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| PubChem CID |
10982
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| Appearance |
Colorless to light yellow liquid
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| Density |
0.8±0.1 g/cm3
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| Boiling Point |
155.0±0.0 °C at 760 mmHg
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| Flash Point |
48.9±0.0 °C
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| Vapour Pressure |
3.1±0.2 mmHg at 25°C
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| Index of Refraction |
1.429
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| LogP |
2.69
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
4
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| Heavy Atom Count |
9
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| Complexity |
59.6
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
QNIVIMYXGGFTAK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H19N/c1-7(2)5-4-6-8(3)9/h7-8H,4-6,9H2,1-3H3
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| Chemical Name |
2-Heptanamine, 6-methyl-
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| Synonyms |
SKF-51; SKF 51; Octodrine
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 (~773.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (19.34 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 (19.34 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 (19.34 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 | 7.7375 mL | 38.6877 mL | 77.3754 mL | |
| 5 mM | 1.5475 mL | 7.7375 mL | 15.4751 mL | |
| 10 mM | 0.7738 mL | 3.8688 mL | 7.7375 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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