(–)-Stepholidine - CAS:16562-13-3

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(–)-Stepholidine (Synonyms:左旋千金藤啶碱; L-千金藤立定; L-Stepholidine; L-SPD)

目录号 : KCM11885 CAS No. : 16562-13-3 纯度 : ≥95%

Data Sheet SDS 产品使用指南

(–)-Stepholidine is a dopamine receptor antagonist and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT (–)-Stepholidine binds to dopamine D, D, D, D, and D receptors (Ks = 5.1, 11.6, 24, 1,450, and 5.8 nM, respectively) as well as 5-HT, 5-HT, α-adrenergic receptors (α-ARs), and sigma-2 (σ) receptors in a radioligand binding assay (Ks = 143, 226, 215, and 53 nM, respectively). It inhibits dopamine-induced cAMP accumulation in HEK293 cells expressing dopamine D, D, and D receptors with IC values of 20.5, 128, and 27 nM, respectively. (–)-Stepholidine inhibits forskolin-induced cAMP production in CHO cells expressing rat 5-HT receptors (EC = 1.2 μM). In vivo, (–)-stepholidine (1 mg/kg, i.v.) increases dopamine neuron firing rates, the number of spikes in bursts, and the amplitude of slow oscillations by 20, 155, and 126%, respectively, in the rat ventral tegmental area (VTA), effects that can be blocked by the 5-HT antagonist WAY-100635 . Pretreatment with (–)-stepholidine inhibits amphetamine- and phencyclidine-induced locomotor activity in rats (EDs = 2.4 and 6.5 mg/kg, respectively).

规格	价格	是否有货
500μg		In-stock
1mg	询价	In-stock
5mg	询价	In-stock

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生物活性

(–)-Stepholidine is an alkaloid. L-Stepholidine exhibits mixed dopamine D1 receptor agonist and D2 antagonist properties. L-Stepholidine has neuroprotective effect. L-Stepholidine can be used for the researches of neurological disease, such as Parkinson disease, Alzheimer's disease and opiate addiction.

IC₅₀&Target

D₁ Receptor D₂ Receptor

体内研究

L-Stepholine (2.5-10 mg/kg, intraperitoneal injection) can inhibit neuronal substance induced relapse without altering spontaneous activity in SD rats.
L-Stepholine (10 mg/kg, intraperitoneal injection, once daily, for 22 consecutive days) can alleviate levodopa (L-DOPA) induced dyskinesia (LID) in a Parkinson's disease rat model with 6-OHDA injury.
L-Stepholine (20 mg/kg, intraperitoneal injection, once daily for 7-21 consecutive days) can attenuate the maintenance of conditioned place preference (CPP) induced by neural substances in rats.
L-Stepholine (10-20 mg/kg, intraperitoneal injection, administered 30 minutes before morphine injection) can block the reacquisition of conditioned place preference (CPP) induced by morphine in rats.
L-Stepholine (10 mg/kg, intraperitoneal injection) can improve memory impairment and restore synaptic plasticity in APP/PS1 transgenic mice.

Animal Model:	6-hydroxydopamine (6-OHDA) -lesioned PD rats models treated with L-DOPA
Dosage:	10 mg/kg
Administration:	Intraperitoneally injection, daily for 22 days
Result:	Displayed much less severe dyskinesia. Attenuated L-DOPA-induced axial and limb dyskinesia. Did not produce any significant axial, limb, and orolingual AIMs.

Animal Model:	APP/PS1 transgenic mice
Dosage:	10 mg/kg
Administration:	Intraperitoneally injection
Result:	Improved impaired learning and memory. Rescued the surface expression of GluA1-containing AMPA receptors and spine density in the hippocampus.

分子式

C₁₉H₂₁NO₄

分子量

327.37

CAS号

16562-13-3

中文名称

左旋千金藤啶碱

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 (305.46 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0546 mL	15.2732 mL	30.5465 mL
5 mM	0.6109 mL	3.0546 mL	6.1093 mL
10 mM	0.3055 mL	1.5273 mL	3.0546 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。

纯度： ≥95%

Data Sheet

SDS

产品使用指南

Mo J, et al. L-stepholidine reduced L-DOPA-induced dyskinesia in 6-OHDA-lesioned rat model of Parkinson's disease. Neurobiol Aging. 2010 Jun;31(6):926-36.

Wang W, et al. The effect of L-stepholidine, a novel extract of Chinese herb, on the acquisition, expression, maintenance, and re-acquisition of morphine conditioned place preference in rats. Neuropharmacology. 2007 Feb;52(2):355-61.

Hao JR, et al. L-Stepholidine rescues memory deficit and synaptic plasticity in models of Alzheimer's disease via activating dopamine D1 receptor/PKA signaling pathway. Cell Death Dis. 2015 Nov 5;6(11):e1965.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

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计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器