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

Harmane hydrochloride  (Synonyms: 哈尔满碱盐酸盐)

目录号: HY-101392A
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摩尔计算器

Harmane hydrochloride 是苯二氮卓类受体抑制剂 (IC50=7 μM)，对 mACh、Opioid Receptor、MAO-A/B、α2-肾上腺素受体的 IC50 分别为 24 μM，2.8 μM，0.5 μM，5 μM 和 18 μM。Harmane hydrochloride 抑制 I1 咪唑啉受体 (IC50 = 30 nM) 来降低血压并具有抗抑郁、抗焦虑、抗惊厥、镇痛作用。Harmane hydrochloride 通过降低酪氨酸羟化酶 (TH) 活性和增强左旋多巴 (L-DOPA) 诱导的 PC12 细胞毒性来抑制多巴胺的生物合成。Harmane hydrochloride 还能提高 2-乙酰氨基芴 (AAF) 诱导的致突变作用。

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Harmane hydrochloride Chemical Structure

Harmane hydrochloride Chemical Structure

CAS No. : 21655-84-5

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Harmane hydrochloride 的其他形式现货产品:

Other Forms of Harmane hydrochloride:

Harmane hydrochloride 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)[1][2][3][4][5][6].

IC50 & Target

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)

体外研究
(In Vitro)

Harmane hydrochloride 抑制螺哌啶醇和血清素，IC50 分别为 163 μM 和 101 μM[1]。
Harmane hydrochloride 对苯二氮卓类受体氟硝西泮的 IC50 为 7 μM，对毒蕈碱型乙酰胆碱受体 (QNB) 的 IC50 为 24 μM，对阿片受体在的 IC50 为 2.8 μM，在含 50 mM 钠离子存在下，对阿片受体在的 IC50 为 42 μM，对螺哌啶醇和血清素的 IC50 为 163，101 μM[1]。
Harmane hydrochloride 对 I1 咪唑啉受体的 IC50为 30 nM)，对 α2-肾上腺素受体的 IC50 为 18 μM[2]。
Harmane hydrochloride (1μM) 在 S-9 混合物 (每毫升含有 4 μM 的 NADH 和 NADPH，但不含 NADP) 存在的情况下，将 AAF 对鼠伤寒沙门氏菌 TA98 的诱变性提高三倍；无 S-9 的情况下，将 N-乙酰氧基 AAF 的致突变性提高 2.5 倍[4]。
Harmane hydrochloride (5-25 μM，0-72 h) 使 PC12 细胞 (IC50 为 21.2 μM) 内的多巴胺含量呈浓度依赖性降低，且可以降低左旋多巴 (L-DOPA) 诱导的多巴胺含量[6]。
Harmane hydrochloride (20 μM，0-72 h) 在 24 h 时抑制 PC12 细胞的酪氨酸羟化酶 (TH) 的活性，并在 72 h 恢复到正常水平; 在 6 h 时抑制 TH mRNA 的表达，在 48 h 恢复[6]。
Harmane hydrochloride (20 μM，30 min) 降低 PC12 细胞内环 AMP 水平和细胞内钙离子浓度[6]。
Harmane hydrochloride (80-150 μM，24-48 h) 表现出细胞毒性，诱导细胞死亡[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Harmane hydrochloride 相关抗体:

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.
体内研究
(In Vivo)

Harman (0-12.5 mg/kg，尾静脉注射，单次剂量) 在大鼠中的惊厥活性 ED50 为 3.6 mg/kg，抗惊厥作用持续时间较短，延迟对痛觉的反应时间[1]。
Harman (0.01-1 nM，注射入延髓头端腹外侧区，单次剂量) 可引起大鼠血压降低[2]。
Harman (2.5-10 mg/kg，腹腔注射) 使大鼠具有抗焦虑和抗抑郁作用[5]。

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.
分子量

218.68

Formula

C12H11ClN2
CAS 号
中文名称

哈尔满碱盐酸盐
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Harmane hydrochloride 相关分类

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Keywords:

Harmane21655-84-5哈尔满碱盐酸盐Imidazoline ReceptorMonoamine OxidaseAdrenergic ReceptornAChRGABA ReceptorOpioid ReceptorMAOBeta ReceptorNicotinic acetylcholine receptorsGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorβ-CarbolinealkaloidBCAactiontremorpsychiatricmanifestationsI1-Imidazolineα2-adrenoceptormonoamineoxidasecomutagenicInhibitorinhibitorinhibit

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