(–)-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%
(–)-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).
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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.
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| 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. |
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| 分子式 |
C19H21NO4
|
| 分子量 |
327.37
|
| CAS号 |
16562-13-3
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| 中文名称 |
左旋千金藤啶碱
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
2-8°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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| 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。
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