Dopamine D2/D3 receptor

尽管所有组中的 DA 含量均存在左脑偏向，且盐水对照显示出比所有药物治疗组更大的不对称性，但“侧”和“组”并没有显着相互作用。当独立检查每一侧时，很明显，长期喹吡罗治疗会导致左脑结构中的 DA 水平逐渐下降，QQ 大鼠与盐水对照组表现出显着差异。相反，急性喹吡罗仅引起右皮质 DA 水平的显着（增加）变化。在各组中，DOPAC 水平也被发现存在左脑偏差。然而，没有发现值得注意的群体效应或相互作用效应。与 QS 组或盐水对照组相比，给予急性喹吡罗的大鼠表现出 DA 含量的特定增加和周转率的降低。与急性喹吡罗组相比，致敏（QQ）大鼠的 DOPAC 水平较高。纹状体中的所有三个 DA 功能测量也显示出显着的组间差异（DA，F3,33=6.27，P=0.0020；F3,33=7.98， P=0.0004；换手率，F3,33=16.85，P<0.0001），以及DA功能的差异。与所有其他组相比，急性喹吡罗大鼠的 DOPAC 和周转率均显着下降。与两个慢性盐水组相比，两个慢性喹吡罗组的周转率均有所增加，而 QQ 大鼠中的 DOPAC 水平显着高于任何其他组[1]。

DA 含量在各组之间存在左脑偏差，尽管这种不对称性在盐水对照组中表现得比所有药物治疗组更大，但侧组和组之间没有显着的相互作用。当单独考虑每一侧时，可以看出，在左脑结构中，随着长期喹吡罗治疗，DA 水平逐渐降低，QQ 大鼠与盐水对照组存在显着差异。相比之下，急性喹吡罗仅显着改变（增加）右皮质 DA 水平。可以发现，DOPAC 水平在各组之间也存在左脑偏差。然而，没有发现显着的群体效应或交互效应。相对于盐水对照组或 QS 组，接受急性喹吡罗的大鼠表现出 DA 含量的选择性增加和周转率的降低。然而，与急性喹吡罗组相比，致敏（QQ）大鼠的 DOPAC 水平升高。在纹状体中，DA 功能的所有三个测量值在各组之间也存在显着差异（DA，F3,33=6.27，P=0.0020；DOPAC，F3,33=7.98，P=0.0004；周转率，F3,33=16.85，P <0.0001）。在急性喹吡罗大鼠中，DOPAC 和更新率相对于所有其他组均显着降低。在QQ大鼠中，DOPAC水平显着高于所有其他组，而就周转率而言，两个慢性喹吡罗组与两个慢性盐水组相比均有所增加[1]。

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Quinpirole/喹匹罗，（4 aR反式）-4,4a，5,6,7,8,8a，9-八氢-5-丙基-1H-吡唑并[3,4-g]喹啉，是一种对多巴胺受体D2亚型具有选择性的多巴胺激动剂。在大鼠中，0.3 mg/kg或更高剂量的喹匹罗可降低下丘脑肾上腺素浓度。这种效果所需的剂量仅略高于降低大脑半球多巴胺代谢物浓度的最低剂量。在较高剂量的喹匹罗（2-3mg/kg i.p.）下，下丘脑中的多巴胺浓度增加，去甲肾上腺素浓度降低，脑干和下丘脑中的MHPG硫酸盐（去甲肾上腺素代谢产物）浓度增加。奎尼罗的所有这些神经化学作用都被多巴胺拮抗剂斯皮罗酮预处理所阻断。选择性D1激动剂SKF 38393或缺乏D2激动剂活性的奎尼罗右旋对映体均未产生这些作用。这些数据支持这样的解释，即喹匹罗通过激活D2受体，导致大鼠脑中多巴胺代谢物减少，下丘脑肾上腺素浓度降低，去甲肾上腺素向硫酸MHPG的转化增加，这可能是通过增强去甲肾上腺素的释放[2]。

Rat: After giving injections of either saline or Quinpirole (Hydrochloride) (0.5 mg/kg, s.c., n = 18/condition) to 36 male Long-Evans rats every day for 12 days, the rats are promptly placed in Omnitech activity monitors (60×60×40 cm) for a 90-minute period. n=9/group) of rats in each chronic condition were given saline and half quinpirole on the last test day. Thus, the four groups stood for sensitized Quinpirole (drug) (QQ), acute Quinpirole (SQ), sensitized Quinpirole (no drug) (QS), and saline controls (SS). Thirty minutes following the last injection, every rat is taken out of the activity monitors and brought to a nearby room where it is promptly beheaded. Since acute quinpirole inhibits activity at this time, and chronic quinpirole is linked to marked hyperlocomotion at 30 minutes, this time point is selected to disentangle the behavioral effects of quinpirole between groups[1].

mouse LDLo intraperitoneal 800 mg/kg Journal of Medicinal Chemistry., 26(1112), 1983

[1]. Effects of quinpirole on central dopamine systems in sensitized and non-sensitized rats. Neuroscience. 1998 Apr;83(3):781-9.

[2]. Decrease in hypothalamic epinephrine concentration and other neurochemical changes produced by quinpirole, a dopamine agonist, in rats. J Neural Transm . 1985;61(3-4):161-73.

Quinpirole is a pyrazoloquinoline that is (4aR,8aR)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrazolo[3,4-g]quinoline substituted by a propyl group at position 5. It acts as a dopamine agonist. It has a role as a dopamine agonist.
A dopamine D2/D3 receptor agonist.

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The present study examined post mortem changes in central dopaminergic terminal regions following acute or chronic treatment regimens with the dopamine D2/D3 receptor agonist quinpirole, a psychomotor stimulant which induces pronounced behavioural sensitization when given chronically. Drug-induced changes in nucleus accumbens, striatum and amygdala were bilateral in nature, while in prefrontal cortex (medial prefrontal and anterior cingulate combined), left and right brain regions responded differentially to quinpirole. Acute drug treatment increased dopamine tissue levels in nucleus accumbens and right prefrontal cortex, while the dopamine metabolite 3,4-dihydroxyphenylacetic acid, was decreased in amygdala. In contrast, sensitization to quinpirole was associated with decreased dopamine levels in left prefrontal cortex, and increases in 3,4-dihydroxyphenylacetic acid levels in subcortical structures, particularly striatum and amygdala. Additionally, the increase in striatal 3,4-dihydroxyphenylacetic acid in chronic quinpirole animals was independent of drug treatment on the final day of injections. In summary, quinpirole induces a variety of simultaneous, regional changes in dopaminergic function, with the sensitized condition being primarily associated with an up-regulation of subcortical dopamine activity. While the nucleus accumbens and striatum play a well known role in motor activation and sensitized behaviour, it is concluded that the amygdala and prefrontal cortex have significant modulatory influences on these processes, with the role of the prefrontal cortex being asymmetrical in nature. Given the suggested relevance of behavioural sensitization to psychopathological states in humans, parallels are drawn between the present data and clinical findings, particularly in relation to obsessive-compulsive disorder.[1]

C13H21N3

219.32594

219.174

C, 71.19; H, 9.65; N, 19.16

80373-22-4

rel-Quinpirole dihydrochloride; 73625-62-4; 80373-22-4; 85798-08-9 (HCl); 73625-62-4 (2HCl)

54562

Typically exists as solid at room temperature

1.936

31.92

1

2

2

16

243

2

CCCN1CCC[C@@H]2CC3NN=CC=3C[C@@H]12

FTSUPYGMFAPCFZ-ZWNOBZJWSA-N

InChI=1S/C13H21N3/c1-2-5-16-6-3-4-10-7-12-11(8-13(10)16)9-14-15-12/h9-10,13H,2-8H2,1H3,(H,14,15)/t10-,13-/m1/s1

(4aR,8aR)-5-propyl-1,4,4a,6,7,8,8a,9-octahydropyrazolo[3,4-g]quinoline

QUINPIROLE; 80373-22-4; Quinpirole [INN]; Quinpirolum; Quinpirol; CHEBI:75401; 1H-Pyrazolo(3,4-g)quinoline, 4,4a,5,6,7,8,8a,9-octahydro-5-propyl-, (4aR-trans)-; (4aR,8aR)-5-propyl-1,4,4a,6,7,8,8a,9-octahydropyrazolo[3,4-g]quinoline;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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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。