Harmane - CAS:486-84-0 - KKL Med Inc.

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Harmane (Synonyms:哈尔满碱)

目录号 : KM6293 CAS No. : 486-84-0 纯度 : 98%

Data Sheet SDS 产品使用指南

Harmane，一种 β-咔啉生物碱 (BCA)，是有效的神经毒素，可引起严重的动作震颤和精神病学表现。Harmane 对 I1 咪唑啉受体 (I1-Imidazoline receptor, IC₅₀=30 nM) 的选择性是对 α2-肾上腺素受体 (IC₅₀=18 μM) 的 1000 倍。Harmane 还是有效和选择性的单胺氧化酶抑制剂 (对 MAO A/B 的 IC₅₀ 值分别为 0.5 μM 和 5 μM)。Harmane 具有致突变作用。

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200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC₅₀=30 nM) over α2-adrenoceptor (IC₅₀=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC₅₀s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect.

体外研究

Harmane inhibits spiropyridinol and quercetin with IC50 values of 163 μM and 101 μM, respectively[1].
Harmane has an IC50 of 7 μM for the benzodiazepine receptor flunitrazepam, 24 μM for the muscarinic acetylcholine receptor (QNB), 2.8 μM for the androgen receptor, 42 μM for the androgen receptor in the presence of 50 mM sodium ions, and 163101 μM for spiropyridinol and quercetin.
Harmane has an IC50 of 30 nM for the I1 imidazoline receptor and an IC50 of 18 μM for the α 2-adrenergic receptor.
Harmane (1 μM) increased the mutagenicity of AAF against Salmonella typhimurium TA98 by three times in the presence of S-9 mixture (containing 4 μM NADH and NADPH per milliliter, but not NADP); Without S-9, the mutagenicity of N-acyloxy AAF was increased by 2.5 times.
Harmane (5-25 μM, 0-72 h) led to a concentration dependent decrease in dopamine levels in PC12 cells (IC50 of 21.2 μM), and also reduced dopamine levels induced by levodopa (LDOPA).
Harmane (20 μM, 0-72 h) inhibited the activity of tyrosine hydroxylase (TH) in PC12 cells at 24 h and returned to normal levels at 72 h; Inhibition of TH mRNA expression at 6 hours and recovery at 48 hours.
Harmane (20 μM, 30 min) reduced the level of intracellular AMP and intracellular calcium ion concentration in PC12 cells.
Harmane (80-150 μM, 24-48 h) exhibits cytotoxicity and induces cell death.

Cell Cytotoxicity Assay

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

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

Harman (0-12.5 mg/kg, tail vein injection, single dose) has a convulsive activity ED50 of 3.6 mg/kg in rats, with a short duration of anticonvulsant action and delayed response time to pain sensation [1].
Harman (0.01-1 nM, injected into the ventral lateral area of the medulla oblongata, single dose) can cause a decrease in high blood pressure [2].
Harman (2.5-10 mg/kg, intraperitoneal injection) has anti anxiety and anti depression effects on rats.

Animal Model:	Female Wistar rats[1]
Dosage:	0, 3.125, 6.25 mg/kg, single dose; 0, 1.56, 3.125, 625, 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
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.

分子式

C₁₂H₁₀N₂

分子量

182.22

CAS号

486-84-0

中文名称

哈尔满碱

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (548.77 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.4878 mL	27.4392 mL	54.8784 mL
5 mM	1.0976 mL	5.4878 mL	10.9757 mL
10 mM	0.5488 mL	2.7439 mL	5.4878 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

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

此方案可获得 ≥ 2.5 mg/mL (13.72 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

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

此方案可获得 ≥ 2.5 mg/mL (13.72 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

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

此方案可获得 ≥ 2.5 mg/mL (13.72 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。