2. Neuronal Signaling GPCR/G Protein Membrane Transporter/Ion Channel
  3. Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor nAChR GABA Receptor Opioid Receptor
  4. Harmane

Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) .

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Harmane Chemical Structure

Harmane Chemical Structure

CAS No. : 486-84-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Harmane:

Harmane Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Harmane

View All Monoamine Oxidase Isoform Specific Products:

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MAO-A MAO-B

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α adrenergic receptor β adrenergic receptor

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) [1][2][3][4][5][6].

IC50 & Target[2][3]

I1-Imidazoline receptor

30 nM (IC50)

hMAO-A

0.5 μM (IC50)

MAO-B

5 μM (IC50)

α2-adrenergic receptor

18 μM (IC50)

nAChR

24 μM (IC50)

benzodiazepine receptor

7 nM (IC50)

Opioid receptor

2.8 μM (IC50)

Loperamide

163 μM (IC50)

Serotonin

101 μM (IC50)

In Vitro

The IC50 of Harmane 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 for I1 imidazoline receptor is 30 nM), and the IC50 for α2-adrenergic receptor is 18 μM[2].
Harmane (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 (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 (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 (20μM, 30min) reduces the intracellular cyclic AMP level and intracellular calcium ion concentration in PC12 cells[6].
Harmane (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.

Harmane Related Antibodies

Cell Cytotoxicity Assay[6]

Cell Line: PC12
Concentration: 80-150 μM; 20, 100, 150 μM
Incubation Time: 24, 48 h
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.

Real Time qPCR[6]

Cell Line: PC12
Concentration: 10-30 μM
Incubation Time: 0-72 h
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.
In Vivo

Harman (0-12.5mg/kg, i.v., single dose) has an ED50 of 3.6 mg/kg for convulsant activity in rats. Its anticonvulsant effect lasts for a short time and delays the reaction time to pain[1].
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.

Animal Model: Female Wistar rats[1]
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
Administration: Intravenous injection (i.v.)
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.
Animal Model: β-carbon alkali-induced hypotension in rats[2]
Dosage: 0.01-1 nM
Administration: Injection into RVLM (rostralventrolateral medulla)
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.
Animal Model: Male adult Sprague-Dawley rats[5]
Dosage: 2.5, 5.0, 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Reduced the immobility time in the swimming test and increased the time in the open arms in the maze test dose-dependently.
Molecular Weight

182.22

Formula

C12H10N2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC1=NC=CC2=C1NC3=C2C=CC=C3
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (548.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.4879 mL 27.4394 mL 54.8787 mL
5 mM 1.0976 mL 5.4879 mL 10.9757 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (13.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (13.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.91%

COA (255 KB) HNMR (237 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References

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
DMSO 1 mM 5.4879 mL 27.4394 mL 54.8787 mL 137.1968 mL
5 mM 1.0976 mL 5.4879 mL 10.9757 mL 27.4394 mL
10 mM 0.5488 mL 2.7439 mL 5.4879 mL 13.7197 mL
15 mM 0.3659 mL 1.8293 mL 3.6586 mL 9.1465 mL
20 mM 0.2744 mL 1.3720 mL 2.7439 mL 6.8598 mL
25 mM 0.2195 mL 1.0976 mL 2.1951 mL 5.4879 mL
30 mM 0.1829 mL 0.9146 mL 1.8293 mL 4.5732 mL
40 mM 0.1372 mL 0.6860 mL 1.3720 mL 3.4299 mL
50 mM 0.1098 mL 0.5488 mL 1.0976 mL 2.7439 mL
60 mM 0.0915 mL 0.4573 mL 0.9146 mL 2.2866 mL
80 mM 0.0686 mL 0.3430 mL 0.6860 mL 1.7150 mL
100 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3720 mL
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Harmane Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Harmane486-84-0Imidazoline ReceptorMonoamine OxidaseAdrenergic ReceptornAChRGABA ReceptorOpioid ReceptorMAOBeta ReceptorNicotinic acetylcholine receptorsGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorβ-CarbolinealkaloidBCAactiontremorpsychiatricmanifestationsI1-Imidazolineα2-adrenoceptormonoamineoxidasecomutagenicInhibitorinhibitorinhibit

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