Xylazine hydrochloride   中文名称: 盐酸甲苯噻嗪

α2-adrenergic receptor[1]

给予赛拉嗪（5.2 mg/kg；腹膜内注射；10-60分钟；雄性 Sprague-Dawley 大鼠）可改变 AMPK 信号分子的 mRNA 表达和蛋白质磷酸化水平，表明 LKB1-AMPK 通路在赛拉嗪治疗引起的中枢神经系统镇静和安神作用中发挥作用[1]。

Animal/Disease Models:Male Sprague-Dawley rats (160-180 g)[1]
Doses: 5.2 mg/kg
Route of Administration: Intraperitoneal injection; for 10 minutes, 20 minutes, 40 minutes or 60 minutes
Experimental Results: Increased in AMPK activity in the cerebral cortex, hippocampus, thalamus and cerebellum. Phosphorylated LKB1 and AMPKα protein levels were decreased.

5707 women TDLo oral 8 mg/kg BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY); BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY); CARDIAC: PULSE RATE Clinical Toxicology., 18(663), 1981 [PMID:6115734]
5707 women TDLo intramuscular 734 ug/kg SENSE ORGANS AND SPECIAL SENSES: MIOSIS (PUPILLARY CONSTRICTION): EYE; CARDIAC: PULSE RATE; VASCULAR: BP LOWERING NOT CHARACTERIZED IN AUTONOMIC SECTION American Journal of Emergency Medicine., 4(222), 1986 [PMID:3964361]
5707 women TDLo intramuscular 22 mg/kg BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY); CARDIAC: PULSE RATE; LUNGS, THORAX, OR RESPIRATION: PLEURAL THICKENING American Journal of Emergency Medicine., 4(222), 1986 [PMID:3964361]
5707 rat LD50 oral 130 mg/kg Deutsche Tieraerztliche Wochenschrift., 75(565), 1968 [PMID:4973114]
5707 mouse LD50 oral 240 mg/kg Deutsche Tieraerztliche Wochenschrift., 75(565), 1968 [PMID:4973114]

[1]. Xylazine Activates Adenosine Monophosphate-Activated Protein Kinase Pathway in the CentralNervous System of Rats. PLoS One. 2016 Apr 6;11(4):e0153169.

Xylazine hydrochloride is the hydrochloride salt of xylazine. It is used as a sedative, analgesic, and muscle relaxant in veterinary medicine. It has a role as an alpha-adrenergic agonist, an analgesic, an emetic, a muscle relaxant and a sedative. It contains a xylazine(1+).
An adrenergic alpha-2 agonist used as a sedative, analgesic and centrally acting muscle relaxant in VETERINARY MEDICINE.
See also: Xylazine (has active moiety).

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Xylazine is a potent analgesic extensively used in veterinary and animal experimentation. Evidence exists that the analgesic effect can be inhibited using adenosine 5'-monophosphate activated protein kinase (AMPK) inhibitors. Considering this idea, the aim of this study was to investigate whether the AMPK signaling pathway is involved in the central analgesic mechanism of xylazine in the rat. Xylazine was administrated via the intraperitoneal route. Sprague-Dawley rats were sacrificed and the cerebral cortex, cerebellum, hippocampus, thalamus and brainstem were collected for determination of liver kinase B1 (LKB1) and AMPKα mRNA expression using quantitative real-time polymerase chain reaction (qPCR), and phosphorylated LKB1 and AMPKα levels using western blot. The results of our study showed that compared with the control group, xylazine induced significant increases in AMPK activity in the cerebral cortex, hippocampus, thalamus and cerebellum after rats received xylazine (P < 0.01). Increased AMPK activities were accompanied with increased phosphorylation levels of LKB1 in corresponding regions of rats. The protein levels of phosphorylated LKB1 and AMPKα in these regions returned or tended to return to control group levels. However, in the brainstem, phosphorylated LKB1 and AMPKα protein levels were decreased by xylazine compared with the control (P < 0.05). In conclusion, our data indicates that xylazine alters the activities of LKB1 and AMPK in the central nervous system of rats, which suggests that xylazine affects the regulatory signaling pathway of the analgesic mechanism in the rat brain.[1]

C12H17CLN2S

256.79

256.08

23076-35-9

7361-61-7 (Parent)

68554

Solid powder

1.15g/cm3

334.2ºC at 760mmHg

150-164?C (dec.)

155.9ºC

0.00013mmHg at 25°C

3.518

49.69

2

2

2

16

230

0

Cl[H].S1C(=NC([H])([H])C([H])([H])C1([H])[H])N([H])C1C(C([H])([H])[H])=C([H])C([H])=C([H])C=1C([H])([H])[H]

QYEFBJRXKKSABU-UHFFFAOYSA-N

InChI=1S/C12H16N2S.ClH/c1-9-5-3-6-10(2)11(9)14-12-13-7-4-8-15-12;/h3,5-6H,4,7-8H2,1-2H3,(H,13,14);1H

N-(2,6-dimethylphenyl)-5,6-dihydro-4H-1,3-thiazin-2-amine;hydrochloride

Xylazine hydrochloride; N-(2,6-Dimethylphenyl)-5,6-dihydro-4H-1,3-thiazin-2-amine; Rompun; Xilazina; Xylazin; Chanazine; Xylazinum; BAY 1470 hydrochloride

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 100 mg/mL (389.42 mM)
H2O : ≥ 50 mg/mL (194.71 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (9.74 mM)(饱和度未知) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (这些助溶剂从左到右依次添加，逐一添加),澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (9.74 mM)(饱和度未知) in 10% DMSO 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加),澄清溶液。
例如，若需制备1 mL的工作液，可将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。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (9.74 mM)(饱和度未知) in 10% DMSO 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加),澄清溶液。
例如，若需制备1 mL的工作液，可将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。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。