| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
hMAO-A 0.5 μM (IC50); MAO-B 5 μM (IC50); α2-adrenergic receptor 18 μM (IC50); I1-Imidazoline receptor 30 nM (IC50); nAChR 24 μM (IC50); benzodiazepine receptor 7 nM (IC50); Opioid receptor 2.8 μM (IC50); Loperamide 163 μM (IC50); Serotonin 101 μM (IC50)
|
|---|---|
| ln Vitro |
Harmane hydrochloride inhibits spironol and serotonin with IC50 of 163 μM and 101 μM, respectively [1]. Harmane hydrochloride has an IC50 of 7 μM for the benzodiazepine receptor flunitrazepam, 24 μM for the muscarinic acetylcholine receptor (QNB), 2.8 μM for the opioid receptor, and 42 μM for the opioid receptor in the presence of 50 mM sodium ions. The IC50 for spironol and serotonin are 163 and 101 μM respectively [1]. Harmane hydrochloride has an IC50 of 30 nM for I1-imidazoline receptors and 18 μM for α2-adrenergic receptors [2]. Harmane hydrochloride (1 μM) increased the mutagenicity of AAF to Salmonella typhimurium TA98 by three times in the presence of an S-9 mixture (containing 4 μM NADH and NADPH per ml but no NADP); in the absence of S-9, it increased the mutagenicity of N-acetoxy AAF by 2.5 times [4]. Harmane hydrochloride (5-25 μM, 0-72 h) reduced the dopamine content in PC12 cells (IC50 of 21.2 μM) in a concentration-dependent manner and could reduce the dopamine content induced by L-DOPA [6]. Harmane hydrochloride (20 μM, 0-72 h) inhibited the activity of tyrosine hydroxylase (TH) in PC12 cells at 24 h and restored it to normal levels at 72 h; it inhibited the expression of TH mRNA at 6 h and recovered it at 48 h [6]. Harmane hydrochloride (20 μM, 30 min) reduces the intracellular cyclic AMP level and intracellular calcium concentration in PC12 cells[6]. Harmane hydrochloride (80-150 μM, 24-48 h) exhibits cytotoxicity and induces cell death[6].
|
| ln Vivo |
The ED50 of Harman (0-12.5 mg/kg, tail vein injection, single dose) in rats is 3.6 mg/kg, and the anticonvulsant effect lasts for a short time, delaying the reaction time to pain[1]. Harman (0.01-1 nM, injected into the rostral ventrolateral medulla, single dose) can cause a decrease in blood pressure in rats[2]. Harman (2.5-10 mg/kg, intraperitoneal injection) has anxiolytic and antidepressant effects in rats[5].
|
| Cell Assay |
Cell Cytotoxicity Assay [6]
Cell Types: PC12 Tested Tested Concentrations: 80-150 μM; 20, 100, 150 μM Incubation Duration: 24, 48 h Experimental Results: Showed cytotoxicity, and cell apoptosis was observed after 48 h of treatment with 150 μM. Tested Tested Concentrationss higher than 150 μM could induce apoptotic cell death. Had stronger cell viability than L-DOPA alone. Real Time qPCR [6] Cell Types: PC12 Tested Tested Concentrations: 10-30 μM Incubation Duration: 0-72 h Experimental Results: Inhibited the increase in dopamine content induced by L-DOPA. Reduced dopamine content, tyrosine hydroxylase activity and mRNA at 6 h, which was maintained for 48 h and gradually recovered at 72 h. |
| Animal Protocol |
Animal/Disease Models: Female Wistar rats[1]
Doses: 0, 3.125, 6.25 mg/kg, single dose; 0, 1.56, 3.125, 6 25, 12.5 mg/kg, single dose; 0, 1.56, 3.125, 6.25 mg/kg, single dose Route of Administration: Intravenous injection (i.v.) Experimental Results: Delayed apamorphine-induced licking. Increased body temperature in rats, reaching the highest value in 25 minutes. 3.125 mg/kg or above caused hypothermia in a dose-dependent manner. Body temperature returned to the control level 100 minutes after injection of 3.125 or 6.25 mg/kg. Prolonged the reaction time to nociception. At 3.125 mg/kg, a delay in reaction could be detected in 20 minutes. Animal/Disease Models: β-carbon alkali-induced hypotension in rats[2] Doses: 0.01-1 nM Route of Administration: Injection into RVLM (rostralventrolateral medulla) Experimental Results: Caused a dose-dependent decrease in mean arterial pressure (MAP) without significant changes in heart rate (HR). Phaloxan could reverse the decrease in MAP. Animal/Disease Models: Male adult Sprague-Dawley rats[5] Doses: 2.5, 5.0, 10 mg/kg Route of Administration: Intraperitoneal injection (i.p.) Experimental Results: Reduced the immobility time in the swimming test and increased the time in the open arms in the maze test dose-dependently. |
| References |
|
| Molecular Formula |
C12H11CLN2
|
|---|---|
| Molecular Weight |
218.68
|
| CAS # |
21655-84-5
|
| Related CAS # |
Harmane;486-84-0;Harmane-d4;2012598-89-7;Harmane (Standard);486-84-0
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CC1=C2C(=CC=N1)C3=CC=CC=C3N2.Cl
|
| Synonyms |
Harman's alkali hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 4.5729 mL | 22.8645 mL | 45.7289 mL | |
| 5 mM | 0.9146 mL | 4.5729 mL | 9.1458 mL | |
| 10 mM | 0.4573 mL | 2.2864 mL | 4.5729 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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