alpha 2-adrenergic receptor

体外活性：育亨宾（Antagonil）已被用作散瞳剂并用于治疗阳痿。它也被认为是一种春药。育亨宾是一种突触前 α2-肾上腺素能阻断剂。育亨宾可能通过阻断中枢α2-肾上腺素能受体，产生继发于去甲肾上腺素释放和大脑去甲肾上腺素能核细胞放电率增加的交感神经驱动力的增加，从而对勃起能力发挥有益作用。

每天在应激训练前1小时向大鼠注射盐酸育亨宾（0.2 mg/kg，腹腔注射），连续14天，并评估其效果。本节的结果表明，将大鼠浸入冷水中会显着降低性唤起和动机，如潜伏期和间隔时间增加所示。大鼠睾丸中睾酮、黄体生成素 (LH) 和卵泡刺激素 (FSH) 水平的降低以及胆固醇含量的降低证实了交配活性的降低。育亨宾治疗显着增加了性唤起和性能力，并纠正了压力对雄性大鼠交配行为的影响。
α2肾上腺素受体拮抗剂育亨宾（YO）增加肾上腺素能/去甲肾上腺素能（NA）神经元的递质释放。系统性YO激活大鼠下丘脑-垂体-肾上腺（HPA）轴，抑制进食，并支持条件性风味回避（CFA）。为了确定这些作用是否需要NA输入到终纹床核（BNST），将与抗多巴胺β-羟化酶（DSAP）抗体偶联的载体或saporin毒素双侧微注射到BNST中以去除其NA输入。随后的测试未能揭示对YO（5.0 mg/kg，i.p.）抑制食物摄入或支持CFA的能力的任何损伤影响。相反，DSAP大鼠HPA轴对YO的反应显著减弱。在最终实验中，DSAP和对照大鼠在腹膜内注射YO或载体后90-120分钟进行灌注。对大脑进行处理，以揭示Fos免疫标记和病变程度。DSAP大鼠的BNST和内侧小细胞室旁下丘脑（PVNmp）中的NA纤维明显减少，这是向这些区域提供辅助NA输入的证据。DSAP大鼠在YO后表现出尾部髓质NA神经元的显著损失，并显著减弱了BNST和促肾上腺皮质激素释放激素阳性PVNmp神经元中Fos的激活。我们得出的结论是，髓质NA神经元群体为BNST和PVNmp提供了侧支输入，这些输入对YO治疗后Fos表达和HPA轴激活有重要贡献。相反，NA介导的BNST和PVNmp神经元的激活对于YO抑制食物摄入或支持CFA是不必要的，这证明了其他完整的神经通路在介导这些效应方面是充分的[2]。

yohimbine (YO) preparation and administration [2]
yohimbine (YO) was freshly dissolved before each experiment by vortexing in sterile 0.15 m NaCl for 5 min at room temperature, followed by passage through a 0.45 μm syringe filter to remove particulate residue. Rats were injected intraperitoneally with 2.0 ml of 0.15 m NaCl vehicle alone, or with vehicle containing YO at a dose of 5.0 mg/kg BW. Injection volumes were adjusted around an average of 2.0 ml per rat to account for small between-animal differences in BW within each experimental cohort. The 5.0 mg/kg BW dose of YO was selected based on recent findings demonstrating that a lower dose of YO (i.e., 1.0 mg/kg BW) did not produce significant effects on food intake, CFA, or central Fos activation (Myers et al., 2005).[2]

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Effect of DSAP lesions on the ability of yohimbine (YO) to inhibit food intake. [2]
Food was removed from cages at 3:30 P.M. (i.e., 3.5 h before dark onset). At 3:00 P.M. on the following day (i.e., 23.5 h later), food-deprived rats (n = 8 DSAP; n = 8 sham control) were injected intraperitoneally with either YO (n = 4 DSAP; n = 4 sham control) or vehicle (n = 4 DSAP; n = 4 sham control). A measured amount of pelleted chow was provided 30 min later, at 3:30 P.M.. Cumulative food intake by each rat, corrected for spillage, was determined after 30 min, 60 min, and 18 h of food access. Rats then were returned to ad libitum chow access for 48 h. The 24 h food deprivation and feeding test was repeated in a counterbalanced design in which rats treated previously intraperitoneally with YO subsequently received vehicle intraperitoneally, and vice versa. Thus, each rat served as its own control for determining the effect of YO on deprivation-induced food intake.[2]

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0.2 mg/kg, i.p.

Rats

Absorption
Rapidly absorbed following oral administration. Bioavailability is highly variable, ranging from 7 to 87% (mean 33%).

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Metabolism / Metabolites
Yohimbine appears to undergo extensive metabolism in an organ of high flow such as the liver or kidney, however, the precise metabolic fate of yohimbine has not been fully determined.

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Biological Half-Life
Elimination half-life is approximately 36 minutes.

rat LD50 intraperitoneal 55 mg/kg

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Hepatotoxicity
In small clinical trials and case series, yohimbine therapy has not been linked to serum enzyme elevations or clinical liver disease. Although yohimbine is often found in weight loss and muscle building herbal combinations, it has not been associated with cases of clinically apparent acute liver injury.br> Likelihood score: E (unlikely cause of clinically apparent liver injury).

[1]. J Urol . 1998 Feb;159(2):433-6.

[2]. J Neurosci . 2006 Nov 1;26(44):11442-53.

[3]. J Chem Ecol, 1998, 24(11), 1881-1937.

A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.
See also: Yohimbine (has active moiety).

C21H26N2O3.HCL

390.9

390.171

C, 64.52; H, 6.96; Cl, 9.07; N, 7.17; O, 12.28

65-19-0

Rauwolscine hydrochloride; 6211-32-1; Yohimbine; 146-48-5; Rauwolscine; 131-03-3

6169

White to light yellow solid powder

542.979ºC at 760 mmHg

288-290 °C (dec.)(lit.)

282.184ºC

103 ° (C=1, H2O)

3.387

65.56

3

4

2

27

555

5

Cl[H].O([H])[C@@]1([H])C([H])([H])C([H])([H])[C@@]2([H])C([H])([H])N3C([H])([H])C([H])([H])C4C5=C([H])C([H])=C([H])C([H])=C5N([H])C=4[C@]3([H])C([H])([H])[C@]2([H])[C@@]1([H])C(=O)OC([H])([H])[H]

PIPZGJSEDRMUAW-VJDCAHTMSA-N

InChI=1S/C21H26N2O3.ClH/c1-26-21(25)19-15-10-17-20-14(13-4-2-3-5-16(13)22-20)8-9-23(17)11-12(15)6-7-18(19)24;/h2-5,12,15,17-19,22,24H,6-11H2,1H3;1H/t12-,15-,17-,18-,19+;/m0./s1

methyl (1S,15R,18S,19R,20S)-18-hydroxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylate;hydrochloride

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

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

配方 1 中的溶解度: ≥ 2.5 mg/mL (6.40 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；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 (6.40 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澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*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 (6.40 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 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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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。