Harmalan
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Harmalan is a tryptamine binding site stimulant and an imidazoline binding site ligand. Harmalan can be isolated from the leaves of Flindersia laevicarpa. Harmalan elevates 5-HT (HY-B1473A) levels and reduces 5-HIAA levels in the cerebral cortex. Harmalan increases spontaneous motor activity, induces clonic convulsions, produces anxiogenic effects, and elicits head weaving, hindlimb abduction, trunk curvature, piloerection, resting tremor, ataxia, forelimb abduction with increased muscle tone, and occasional alternating forepaw treading behaviors.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.45%
- CAS 番号: 525-41-7
- 分子式: C12H12N2
- 分子量:184.24
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保管条件:
Store at room temperature, keep dry and cool.
In solvent -80°C, 1 year , -20°C, 6 months
5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| FM3A | EC50 |
1.0 x 10-5 M
Compound: 6
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In vitro cytotoxic activity tested in mouse mammary tumor FM3A cells
In vitro cytotoxic activity tested in mouse mammary tumor FM3A cells
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[PMID: 15026051] |
| H9 | EC50 |
32 μM
Compound: 21
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Antiviral activity against HIV1 in human H9 cells assessed as inhibition of viral replication
Antiviral activity against HIV1 in human H9 cells assessed as inhibition of viral replication
|
[PMID: 11473435] |
| H9 | IC50 |
110.3 μM
Compound: 21
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Cytotoxicity against human H9 cells
Cytotoxicity against human H9 cells
|
[PMID: 11473435] |
Harmalan exhibits low affinity for benzodiazepine binding sites in rat brain cell membranes, with an IC50 of 419 μM[1].
Harmalan binds to the 5-HT2 receptor sites on the cell membrane of the rat prefrontal cortex, with an IC50 value of 1.92 μM[1].
Harmalan exhibits high affinity for tryptamine binding sites in rat cerebral cortex cell membranes, with an IC50 of 0.038 μM[1].
Harmalan potently binds to the I-1 imidazoline binding site on rat renal cell membranes, with an IC50 of 46 nM[3].
Harmalan (40 min) potently binds to the I-2 imidazoline binding sites in rat whole brain cell membranes, with a Ki value of 148 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Harmalan (1-40 mg/kg; i.v.) dose-dependently induces clonic convulsions in female Wistar rats, an effect antagonized by benzodiazepine agonist but not benzodiazepine site blockers, and modulated by serotonin/tryptamine receptor agents[1].
Harmalan (34 µmol/kg; i.v.) increases cerebral cortex 5-HT concentrations and decreases 5-HIAA concentrations in female Wistar rats, with additive effects when combined with monoamine oxidase inhibitor and indolealkylamine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (female, 180-220 g)[1]
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Dosage:3.125 mg/kg; 6.25 mg/kg; 9.375 mg/kg; 10 mg/kg; 12.5 mg/kg
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Administration:i.v.
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Result:Caused lateral head weaving, hind limb abduction, back bending, coat ruffling, and resting torso tremor in 8/10 rats at 3.125 mg/kg.
Induced head and torso resting tremor lasting 2-3 hours, ataxia, forelimb abduction, increased extensor muscle tone, and occasional reciprocal forepaw treading in all rats, plus clonic convulsions followed by postictal relaxation in 3/10 rats at 6.25 mg/kg.
Triggered seizure trains lasting up to 15 minutes post-injection in 7/10 rats at 9.375 mg/kg.
Produced clonic convulsions in 9/10 rats at 10 mg/kg.
Induced marked excitation with generalized convulsions and jumping up to 0.5 m in all rats at 12.5 mg/kg.
化学情報
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CAS 番号 525-41-7
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性状 Solid
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分子量 184.24
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分子式 C12H12N2
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Color Yellow to brown
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SMILES
CC1=NCCC2=C1NC3=CC=CC=C23
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Store at room temperature, keep dry and cool
In solvent -80°C 1 year -20°C 6 months
溶剤 & 溶解度
DMSO : 50 mg/mL (271.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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取扱説明書 (2659 KB)
参考文献
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.4277 mL | 27.1385 mL | 54.2770 mL | 135.6926 mL |
| 5 mM | 1.0855 mL | 5.4277 mL | 10.8554 mL | 27.1385 mL | |
| 10 mM | 0.5428 mL | 2.7139 mL | 5.4277 mL | 13.5693 mL | |
| 15 mM | 0.3618 mL | 1.8092 mL | 3.6185 mL | 9.0462 mL | |
| 20 mM | 0.2714 mL | 1.3569 mL | 2.7139 mL | 6.7846 mL | |
| 25 mM | 0.2171 mL | 1.0855 mL | 2.1711 mL | 5.4277 mL | |
| 30 mM | 0.1809 mL | 0.9046 mL | 1.8092 mL | 4.5231 mL | |
| 40 mM | 0.1357 mL | 0.6785 mL | 1.3569 mL | 3.3923 mL | |
| 50 mM | 0.1086 mL | 0.5428 mL | 1.0855 mL | 2.7139 mL | |
| 60 mM | 0.0905 mL | 0.4523 mL | 0.9046 mL | 2.2615 mL | |
| 80 mM | 0.0678 mL | 0.3392 mL | 0.6785 mL | 1.6962 mL | |
| 100 mM | 0.0543 mL | 0.2714 mL | 0.5428 mL | 1.3569 mL |