Harmane

Harmane 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 inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF)^{[1][2][3][4][5][6]}. IC50 & Target:Harmane 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。
Harmane 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]。 In Vitro:Harmane also inhibits haloperidol and serotonin, with IC₅₀ values of 163 μM and 101 μM, respectively^[1].
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]. 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].