| Bioactivity | 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]. |
| Invitro | 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. 0 --> Harmane hydrochloride 相关抗体: Cell Cytotoxicity Assay [6] Cell Line: |
| 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: |
| CAS | 21655-84-5 |
| Formula | C12H11ClN2 |
| Molar Mass | 218.68 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. W E Müller, et al. On the neuropharmacology of harmane and other beta-carbolines. Pharmacol Biochem Behav. 1981 May;14(5):693-9. [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. [3]. Glover V, et, al. β-Carbolines as selective monoamine oxidase inhibitors:In vivo implications [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. [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. |
Harmane hydrochloride
CAS: 21655-84-5 F: C12H11ClN2 W: 218.68
Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, M
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