Loxapine 洛沙平|cas:1977-10-2|西域试剂

Loxapine 洛沙平,99.69%

产品编号：Bellancom-17390| CAS NO：1977-10-2| 分子式：C₁₈H₁₈ClN₃O| 分子量：327.81

Loxapine琥珀酸盐是D2DR/D4DR抑制剂和5-羟色胺受体拮抗剂，有抗精神病活性。

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-17390		￥700.00	杭州北京（现货）
Bellancom-17390		￥2400.00	杭州北京（现货）

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Loxapine 洛沙平

产品介绍

Loxapine 是一种具有口服活性的多巴胺（dopamine）抑制剂和 5-HT 受体拮抗剂，有抗精神病活性。

生物活性

Loxapine is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent^[4].

体外研究

In the presence of Loxapine, [³H]ketanserin binds to 5-HT₂ receptor in Frontal cortex of brain in human and bovine with K_i value of 6.2 nM and 6.6 nM, respectively. Loxapine has the rank order of potency for the various receptors appears to be as follows: 5-HT₂≥D₄>>>D₁>D₂ in comparing competition experiments involving the human membranes.
Loxapine (0-20 μM, 24 h or 72 h) reduces IL-1β secretion by LPS-activated mixed glia cultures, reduces IL-2 secretion in mixed glia cultures, and decreases IL-1β and IL-2 secretion in LPS-induced microglia cultures.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Loxapine (5 mg/kg; i.p.; daily for 4 or 10 weeks) decreases serotonin (S₂) but does not elevate dopamine (D2) receptor numbers in the rat brain.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male Wistar rats (150-175 g)
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection, daily for 4 or 10 weeks
Result:	Induced a very significant reduction (more than 50%) of serotonin (S₂) receptor density after 4 weeks or 10 weeks of daily injection, but did not produce any significant increase in dopamine receptor density.

体内研究

Loxapine (5 mg/kg; i.p.; daily for 4 or 10 weeks) decreases serotonin (S₂) but does not elevate dopamine (D2) receptor numbers in the rat brain.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Adult male Wistar rats (150-175 g)
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection, daily for 4 or 10 weeks
Result:	Induced a very significant reduction (more than 50%) of serotonin (S₂) receptor density after 4 weeks or 10 weeks of daily injection, but did not produce any significant increase in dopamine receptor density.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 33.33 mg/mL (101.67 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0505 mL	15.2527 mL	30.5055 mL
5 mM	0.6101 mL	3.0505 mL	6.1011 mL
10 mM	0.3051 mL	1.5253 mL	3.0505 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 (7.63 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.63 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.63 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.63 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.63 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.63 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。