| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Heptaminol targets several systems. It has mild sympathomimetic properties, possibly due to indirect activation of adrenergic receptors (alpha and beta) by inhibiting norepinephrine reuptake or promoting its release. It also exerts a direct positive inotropic effect on cardiac muscle, possibly via modulation of calcium flux. Additionally, it is a weak inhibitor of phosphodiesterase (PDE), leading to increased intracellular cAMP. However, its precise molecular target is not fully defined. Its primary clinical target is vascular smooth muscle and cardiac myocytes.
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| ln Vitro |
In vitro, Heptaminol (10-100 uM) increases the contractile force of isolated guinea pig atria (positive inotropic effect) and increases coronary blood flow in isolated perfused heart preparations. It also constricts isolated rat aortic rings pre-contracted with phenylephrine, indicating vasoconstrictor activity. In neuroblastoma cells, it increases intracellular norepinephrine release at higher concentrations. At therapeutic concentrations (0.1-10 uM), it shows no significant cytotoxicity and does not affect platelet aggregation.
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| ln Vivo |
In vivo, Heptaminol elevates blood pressure in animal models of hypotension. In anesthetized dogs or rats, intravenous administration (0.5-2 mg/kg) increases mean arterial pressure (MAP) by 10-30 mmHg, with a duration of 30-60 minutes. It also increases cardiac output and reduces orthostatic blood pressure drop in conscious rabbits. In human patients, oral or intramuscular heptaminol (300-600 mg) effectively raises blood pressure in orthostatic hypotension, improving symptoms of dizziness and syncope within 1-2 hours.
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| Enzyme Assay |
Non-cell assays are limited for heptaminol. A receptor binding assay for alpha1-adrenergic receptors can be performed using rat cortical membranes. 3H-prazosin (0.2 nM) is incubated with membranes (200 ug) and increasing concentrations of heptaminol (1 nM - 100 uM) for 60 min at 25degC. Non-specific binding is determined with 10 uM phentolamine. Bound radioactivity is separated by filtration. Heptaminol displaces prazosin with a Ki in the micromolar range (~10-50 uM), confirming weak direct binding. It also inhibits norepinephrine uptake in synaptosomal preparations (IC50 ~20 uM).
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| Cell Assay |
Cellular assay for inotropic effect is not typical. Instead, a functional assay in isolated cardiomyocytes: Neonatal rat ventricular myocytes are isolated and cultured. Cells are loaded with the calcium-sensitive dye Fluo-4-AM. Heptaminol (1-100 uM) is applied, and intracellular calcium transients are measured by fluorescence microscopy. Heptaminol increases the amplitude of calcium transients and the rate of calcium decay (sarcoplasmic reticulum Ca2+-ATPase activity), consistent with a positive inotropic effect. The effect is blocked by propranolol (beta-blocker) partially, suggesting both direct and indirect mechanisms.
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| Animal Protocol |
Orthostatic hypotension rat model: Male Sprague-Dawley rats are anesthetized with urethane. A catheter is placed in the carotid artery for blood pressure monitoring. Orthostatic stress is induced by a 45deg head-up tilt for 3-5 minutes. Heptaminol is administered intravenously (1, 3, 10 mg/kg) or orally (30 mg/kg) 30 minutes before tilt. Blood pressure drop during tilt is measured. Heptaminol at 3 mg/kg IV significantly reduces the maximal drop in MAP from -40 mmHg to -15 mmHg. Alternatively, anesthetized dogs are used for more robust cardiovascular parameters (dP/dt, cardiac output).
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| ADME/Pharmacokinetics |
Pharmacokinetic studies in humans: Heptaminol is well absorbed orally with a bioavailability of ~70-80%. Peak plasma concentrations (Cmax ~1-2 ug/mL) are reached 1-2 hours after a 300 mg oral dose. Plasma protein binding is low (~20-30%). Volume of distribution is moderate (2-4 L/kg), indicating tissue distribution. The elimination half-life is approximately 4-6 hours. Heptaminol is primarily excreted unchanged in the urine (60-80%) and is not extensively metabolized. Renal clearance exceeds glomerular filtration rate, suggesting active tubular secretion.
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| Toxicity/Toxicokinetics |
Dosage: Therapeutic human dose is 300-600 mg/day. Acute toxicity: Oral LD50 in rats is approximately 1000 mg/kg, in mice ~1500 mg/kg. Side effects at high doses include nausea, vomiting, headache, and insomnia (due to sympathomimetic stimulation). Overdose can cause hypertension, tachycardia, and arrhythmias. No teratogenic effects in animal studies, but use in pregnancy is not recommended. No genotoxicity (Ames test negative). Long-term high doses may cause reversible liver enzyme elevation.
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| References | |
| Additional Infomation |
6-Amino-2-methyl-2-heptanol is a tertiary alcohol. It is an amino alcohol that has been used as a myocardial stimulant and vasodilator, and to relieve bronchospasm. Its most common therapeutic use is for orthostatic hypotension. The mechanism of action of heptanol is not fully understood, but studies suggest it may affect catecholamine release or calcium metabolism.
Heptaminol (CAS# 372-66-7) is an approved pharmaceutical drug in several countries (e.g., France, Vietnam, Greece) for the treatment of functional hypotension, orthostatic hypotension, and as a supportive therapy in chronic circulatory insufficiency. It is available as oral tablets (300 mg), solution for injection (250 mg/5 mL), and as a fixed combination with other agents (e.g., with acetylsalicylic acid). It is not approved by the FDA or EMA in the US and most of Europe (except France). Common brand names include Hept-A-Myl, Cardionyl, and Arteriocol. Its use has declined due to newer agents, but it remains a second-line option. |
| Molecular Formula |
C8H19NO
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|---|---|
| Molecular Weight |
145.24
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| Exact Mass |
145.147
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| CAS # |
372-66-7
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| Related CAS # |
543-15-7 (hydrochloride)
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| PubChem CID |
3590
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| Appearance |
Liquid
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| Density |
0.895g/cm3
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| Boiling Point |
250.1ºC at 760mmHg
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| Flash Point |
105.1ºC
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| Index of Refraction |
1.455-1.457
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| LogP |
1.975
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
10
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| Complexity |
91.3
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CCCC(C)(C)O)N
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| InChi Key |
LREQLEBVOXIEOM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H19NO/c1-7(9)5-4-6-8(2,3)10/h7,10H,4-6,9H2,1-3H3
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| Chemical Name |
6-amino-2-methylheptan-2-ol
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.8852 mL | 34.4258 mL | 68.8516 mL | |
| 5 mM | 1.3770 mL | 6.8852 mL | 13.7703 mL | |
| 10 mM | 0.6885 mL | 3.4426 mL | 6.8852 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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