Naloxone - CAS:465-65-6

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Naloxone (Synonyms:纳洛酮)

目录号 : KM32596 CAS No. : 465-65-6 纯度 : 99%

Data Sheet 产品使用指南

Naloxone 为具有口服活性的阿片受体 (opioid receptor) 拮抗剂。Naloxone 可减弱脊髓刺激相关的抗痛觉过敏效应，拮抗与中枢神经系统损伤后遗症相关的内源性阿片肽生理作用；发挥升压作用，使平均动脉压轻度升高；具备神经保护作用，改善创伤后神经运动功能；阻断阿片受体介导的遗忘通路，增强记忆巩固，逆转促肾上腺皮质激素 (ACTH) 与肾上腺素诱发的遗忘，并增强二者的促记忆效应。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock

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生物活性

Naloxone is an orally active opioid receptor antagonist. Naloxone attenuates spinal cord stimulation‑associated anti‑hyperalgesic effects, antagonizes physiologic effects of endogenous opioid peptides linked to central nervous system injury sequelae, functions as a pressor agent to induce modest elevations in mean arterial blood pressure, exerts neuroprotective effects to improve post‑traumatic neurologic motor function, blocks opioid receptor‑mediated amnesic pathways, enhances memory consolidation, reverses ACTH‑ and epinephrine‑induced amnesia, and potentiates the memory‑facilitatory effects of ACTH and epinephrine.

体外研究

Naloxone (containing 800 µg per tablet; annealed for 2 hours, freeze-dried for 5 days) can form freeze-dried oral tablets, which can form a stable amorphous matrix and maintain chemical and physical integrity for up to 9 months at 4 ° C or 25 ° C.

Naloxone (800 µg per tablet; maximum 30 seconds) can be made into freeze-dried buccal tablets, with a disintegration rate of 90% within 4.8 seconds under cheek related conditions (37 ° C, 0.7 mL phosphate buffer), and can completely disintegrate within 30 seconds under all tested temperature and medium volume conditions.

体内研究

Naloxone (10 mg/kg; intraperitoneal injection; Single dose administration can significantly inhibit the reversal of neuropathic mechanical hyperalgesia induced by early spinal cord electrical stimulation (SCS) in male Sprague Dawley rats, but has no effect on the incremental anti hyperalgesia effect of late SCS [1].
Naloxone (2.0 mg/kg; 1.7 mg/kg/h; intravenous injection); First, administer the loading dose within 60 seconds, followed by continuous infusion; A duration of 4 hours can significantly improve the long-term neurological and motor function recovery of male Sprague Dawley rats after moderate hydraulic shock traumatic brain injury for up to 4 weeks, with a median comprehensive neurological score of 18.5 at week 4 [2].
Naloxone (0.4 mg/kg; intraperitoneal injection; Immediate single administration after training can significantly promote the memory of male Wistar rats trained on tasks 1 and 2, and reverse the forgetting effect caused by ACTH and adrenaline after training [3].

Animal Model:	Sprague Dawley (adult male, 200-250 g, neuropathic pain model via partial sciatic nerve ligation and epidural monopolar electrode implantation at spinal segments T12/13)
Dosage:	10 mg/kg
Administration:	i.p.; single dose
Result:	Decreased the ipsilateral:contralateral paw withdrawal threshold ratio after SCS1. Exerted no discernible effect on the anti-hyperalgesic effect induced by SCS2.

Animal Model:	Sprague-Dawley (male, moderate severity lateral fluid-percussion traumatic brain injury induced via 2.4 to 2.5 atmosphere pressure pulse)
Dosage:	2.0 mg/kg (bolus); 1.7 mg/kg/h (infusion)
Administration:	i.v.; bolus over 60 seconds followed by constant infusion; 4 hours
Result:	Caused a modest, nonsignificant increase in mean arterial blood pressure during 4-hour postinjury monitoring period. Showed no significant changes to arterial blood gases, pH, or brain temperature. Exhibited no significant improvement in composite neurologic motor scores at 24 hours postinjury. Achieved a significant improvement in median composite neurologic motor scores at 1 week postinjury. Reached a median composite neurologic motor score of 18.5 out of maximum 20 by week 4. Resulted in 100% survival rate over the 4-week study period.

Animal Model:	Wistar rats (male, age 51-69 days, weight 140-200 g, step-down inhibitory avoidance task 1 training)
Dosage:	0.4 mg/kg
Administration:	i.p.; single immediate post-training injection
Result:	Produced a median (mean) training-test step-down latency difference of 180.00 sec. Produced a median (mean) training-test step-down latency difference of 180.00 (144.45) sec when co-administered with 2.0 μg/kg ACTH_1-24, reversing the amnesic effect of ACTH alone and showing a significant difference from naloxone alone. Produced a median (mean) training-test step-down latency difference of 180.00 (134.98) sec when co-administered with 50.0 μg/kg epinephrine HC1, reversing the amnesic effect of epinephrine alone and showing a significant difference from naloxone alone.

Animal Model:	Wistar rats (male, age 51-69 days, weight 140-200 g, step-down inhibitory avoidance task 2 training)
Dosage:	0.4 mg/kg
Administration:	i.p.; single immediate post-training injection
Result:	Produced a median (mean) training-test step-down latency difference of 24.13 (56.18) sec, showing significant memory facilitation compared to saline controls. Produced a median (mean) training-test step-down latency difference of 105.07 (113.65) sec when co-administered with 2.0 μg/kg ACTH_1-24, potentiating the facilitatory effect of ACTH alone and showing a significant difference from naloxone alone . Produced a median (mean) training-test step-down latency difference of 81.85 (96.86) sec when co-administered with 50.0 μg/kg epinephrine HC1, potentiating the facilitatory effect of epinephrine alone and showing a significant difference from naloxone alone.

分子式

C₁₉H₂₁NO₄

分子量

327.37

CAS号

465-65-6

中文名称

纳洛酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light, stored under nitrogen

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

溶解性数据

In Vitro:

DMSO : 100 mg/mL (305.46 mM; Need ultrasonic)

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 (protect from light, stored under nitrogen)。-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: ≥ 5 mg/mL (15.27 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (15.27 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (15.27 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (15.27 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (15.27 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (15.27 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： 99%

Data Sheet

产品使用指南

[1]. Sun L, et al. Endocannabinoid activation of CB receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. European journal of pain (London, England). 2017 May;21(5):804-814.

[2]. McIntosh TK, et al. Beneficial effect of the nonselective opiate antagonist naloxone hydrochloride and the thyrotropin-releasing hormone (TRH) analog YM-14673 on long-term neurobehavioral outcome following experimental brain injury in the rat. J Neurotrauma. 1993 Winter;10(4):373-84.

[3]. Izquierdo I, et al. Effect of ACTH, epinephrine, beta-endorphin, naloxone, and of the combination of naloxone or beta-endorphin with ACTH or epinephrine on memory consolidation. Psychoneuroendocrinology. 1983;8(1):81-7.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

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

重置计算

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

计算重置

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。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器