Harmane hydrochloride
Based on 2 publication(s) in Google Scholar
Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
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- Purity: 99.96%
- CAS No.: 21655-84-5
- 화학식: C12H11ClN2
- 분자량:218.68
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Harmane hydrochloride
MoreAll Adrenergic Receptor Isoforms
MoreAll Opioid Receptor Isoforms
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Biological Activity
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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) |
Harmane hydrochloride also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively[1].
The IC50 of Harmane hydrochloride for benzodiazepine receptor flunitrazepam is 7 μM, the IC50 for the opioid receptor is 2.8 μM, and in the presence of 50 mM sodium ions, the IC50 for the opioid receptor is 42 μM, and the IC50 for spiropyrinol and serotonin is 163, 101 μM[1].
The IC50 of Harmane hydrochloride for I1 imidazoline receptor is 30 nM), and the IC50 for α2-adrenergic receptor is 18 μM[2].
Harmane hydrochloride (1 μM) increases 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 increases the mutagenicity of N-acetyloxy AAF by 2.5 times[4].
Harmane hydrochloride (5-25 μM, 0-72 h) reduced the dopamine content in PC12 cells (IC50 is 21.2 μM) in a concentration-dependent manner and could reduce the dopamine content induces by L-DOPA[6].
Harmane hydrochloride (20 μM, 0-72 h) inhibits the activity of tyrosine hydroxylase (TH) in PC12 cells at 24 h and restores it to normal levels at 72 h; it inhibits the expression of TH mRNA at 6 h and restores it at 48 h[6].
Harmane hydrochloride (20μM, 30min) reduces the intracellular cyclic AMP level and intracellular calcium ion concentration in PC12 cells[6].
Harmane hydrochloride (80-150μM, 24-48h) exhibits cytotoxicity and induces cell death[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC12
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Concentration:80-150 μM; 20, 100, 150 μM
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Incubation Time:24, 48 h
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Result:Showed cytotoxicity, and cell apoptosis was observed after 48 h of treatment with 150 μM. Concentrations higher than 150 μM could induce apoptotic cell death.
Had stronger cell viability than L-DOPA alone.
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Cell Line:PC12
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Concentration:10-30 μM
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Incubation Time:0-72 h
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Result: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.
Harman (0.01-1 nM, injected into rostralventrolateral medulla, single dose) caused a decrease in blood pressure in rats[2].
Harman (2.5-10 mg/kg, i.p., single dose) had anxiolytic and antidepressant effects in rats[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Wistar rats[1]
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Dosage: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
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Administration:Intravenous injection (i.v.)
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Result: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.
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Animal Model:β-carbon alkali-induced hypotension in rats[2]
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Dosage:0.01-1 nM
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Administration:Injection into RVLM (rostralventrolateral medulla)
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Result:Caused a dose-dependent decrease in mean arterial pressure (MAP) without significant changes in heart rate (HR). Phaloxan could reverse the decrease in MAP.
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Animal Model:Male adult Sprague-Dawley rats[5]
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Dosage:2.5, 5.0, 10 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced the immobility time in the swimming test and increased the time in the open arms in the maze test dose-dependently.
Chemical Information
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CAS No. 21655-84-5
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Appearance Solid
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분자량 218.68
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화학식 C12H11ClN2
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Color White to off-white
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SMILES
CC1=NC=CC2=C1NC3=C2C=CC=C3.Cl
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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mSystems
2026 Jun 9:e0170425. PMID: 42262096 -
Front Mol Neurosci
Harmane Potentiates Nicotine Reinforcement Through MAO-A Inhibition at the Dose Related to Cigarette Smoking. [Abstract]2022 Jun 27;15:925272. PMID: 35832393
용액&용해도
DMSO : ≥ 100 mg/mL (457.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (291 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. W E Müller, et al. On the neuropharmacology of harmane and other beta-carbolines. Pharmacol Biochem Behav. 1981 May;14(5):693-9. [Content Brief]
[2]. Musgrave IF, et, al. Harmane produces hypotension following microinjection into the RVLM: possible role of I(1)-imidazoline receptors. Br J Pharmacol. 2000 Mar;129(6):1057-9. [Content Brief]
[3]. Glover V, et, al. β-Carbolines as selective monoamine oxidase inhibitors:In vivo implications [Content Brief]
[4]. https://pubmed.ncbi.nlm.nih.gov/345280/
[5]. E D Louis, et al. Harmane induces anxiolysis and antidepressant-like effects in rats. Ann N Y Acad Sci. 2005 Aug 9;65(3):391-6. [Content Brief]
[6]. Yoo Jung Yang, et al. Effects of harman and norharman on dopamine biosynthesis and L-DOPA-induced cytotoxicity in PC12 cells. Eur J Pharmacol. 2008 Jun 10;587(1-3):57-64. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.5729 mL | 22.8645 mL | 45.7289 mL | 114.3223 mL |
| 5 mM | 0.9146 mL | 4.5729 mL | 9.1458 mL | 22.8645 mL | |
| 10 mM | 0.4573 mL | 2.2864 mL | 4.5729 mL | 11.4322 mL | |
| 15 mM | 0.3049 mL | 1.5243 mL | 3.0486 mL | 7.6215 mL | |
| 20 mM | 0.2286 mL | 1.1432 mL | 2.2864 mL | 5.7161 mL | |
| 25 mM | 0.1829 mL | 0.9146 mL | 1.8292 mL | 4.5729 mL | |
| 30 mM | 0.1524 mL | 0.7621 mL | 1.5243 mL | 3.8107 mL | |
| 40 mM | 0.1143 mL | 0.5716 mL | 1.1432 mL | 2.8581 mL | |
| 50 mM | 0.0915 mL | 0.4573 mL | 0.9146 mL | 2.2864 mL | |
| 60 mM | 0.0762 mL | 0.3811 mL | 0.7621 mL | 1.9054 mL | |
| 80 mM | 0.0572 mL | 0.2858 mL | 0.5716 mL | 1.4290 mL | |
| 100 mM | 0.0457 mL | 0.2286 mL | 0.4573 mL | 1.1432 mL |
Harmane hydrochloride Related Classifications
HY-101392A Related Classifications
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