GlpBio

(−)-Apomorphine (hydrochloride hydrate)

目录号: GC26151纯度: >95.00%同义词: 5,6,6aR,7-tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol, monohydrochloride, hydrate
(-)-Apomorphine (hydrochloride hydrate)是一种强效的多巴胺受体激动剂，对D1-和D2类受体（D1、D2S、D2L、D3、D4、D5）都具有广泛作用。
(−)-Apomorphine (hydrochloride hydrate)
Cas No.: 58117-94-5
规格价格库存数量操作
10mg¥477.00现货
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50mg¥1,047.00现货
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100mg¥1,833.00现货
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产品描述 Description

(-)-Apomorphine (hydrochloride hydrate) acts as a potent dopamine receptor agonist with a broad spectrum on all D1- and D2-like receptors (D1, D2S, D2L, D3, D4, D5) [1]. (-)-Apomorphine (hydrochloride hydrate) is extremely lipophilic and can cross the blood–brain barrier freely[2]. (-)-Apomorphine (hydrochloride hydrate) is the oldest dopaminergic drug available for Parkinson’s disease[3][4]. (-)-Apomorphine (hydrochloride hydrate) is a highly potent antioxidant and free radical scavenger with a neuroprotective effect[5].

(-)-Apomorphine (hydrochloride hydrate) at concentrations of higher than 2 x10-5M treatment dramatically reduced the growth-stimulatory effect of retinal pigment epithelium (RPE) cells on the scleral chondrocytes[6]. (-)-Apomorphine (hydrochloride hydrate) exhibits potent relaxant effects on rat corpus cavernosum tissues in vitro, particularly on phenylephrine-induced contractions, without altering cyclic nucleotides[7].

(-)-Apomorphine (hydrochloride hydrate) induced erections in awake rats, peaking at 300nmol/kg, but had no effect on basal or nerve-stimulated cavernous pressure in anesthetized rats[7]. (-)-Apomorphine (hydrochloride hydrate) (20mg/kg, i.p) administration to rats with normal 4-day estrous cycles reduced serum prolactin levels during diestrus and prevented the proestrous rise in serum prolactin[8].

References:
[1]. Auffret M, Drapier S, Vérin M. Pharmacological Insights into the Use of Apomorphine in Parkinson's Disease: Clinical Relevance. Clin Drug Investig. 2018 Apr;38(4):287-312. doi: 10.1007/s40261-018-0619-3. PMID: 29327219.
[2]. Corboy DL, Wagner ML, Sage JI. Apomorphine for motor fluctuations and freezing in Parkinson's disease. Ann Pharmacother. 1995 Mar;29(3):282-8. doi: 10.1177/106002809502900310. PMID: 7606075.
[3]. Boyle A, Ondo W. Role of apomorphine in the treatment of Parkinson's disease. CNS Drugs. 2015 Feb;29(2):83-9. doi: 10.1007/s40263-014-0221-z. PMID: 25676564.
[4]. Unti E, Ceravolo R, Bonuccelli U. Apomorphine hydrochloride for the treatment of Parkinson's disease. Expert Rev Neurother. 2015;15(7):723-32. doi: 10.1586/14737175.2015.1051468. Epub 2015 Jun 2. PMID: 26037961.
[5]. Grünblatt E, Mandel S, Gassen M, et al. Potent neuroprotective and antioxidant activity of apomorphine in MPTP and 6-hydroxydopamine induced neurotoxicity. J Neural Transm Suppl. 1999;55:57-70. doi: 10.1007/978-3-7091-6369-6_6. PMID: 10335493.
[6]. Seko Y, Tanaka Y, Tokoro T. Apomorphine inhibits the growth-stimulating effect of retinal pigment epithelium on scleral cells in vitro. Cell Biochem Funct. 1997 Sep;15(3):191-6. doi: 10.1002/(SICI)1099-0844(199709)15:3<191::AID-CBF738>3.0.CO;2-2. PMID: 9377797.
[7]. Matsumoto K, Yoshida M, Andersson KE, Hedlund P. Effects in vitro and in vivo by apomorphine in the rat corpus cavernosum. Br J Pharmacol. 2005 Sep;146(2):259-67. doi: 10.1038/sj.bjp.0706317. PMID: 16025145; PMCID: PMC1576267.
[8]. Smalstig EB, Sawyer BD, Clemens JA. Inhibition of rat prolactin release by apomorphine in vivo and in vitro. Endocrinology. 1974 Jul;95(1):123-9. doi: 10.1210/endo-95-1-123. PMID: 4857693.

(-)-Apomorphine (hydrochloride hydrate)是一种强效的多巴胺受体激动剂，对D1-和D2类受体（D1、D2S、D2L、D3、D4、D5）都具有广泛作用[1]。(-)-Apomorphine (hydrochloride hydrate)极具脂溶性，能自由穿过血脑屏障[2]。(-)-Apomorphine (hydrochloride hydrate)是目前用于帕金森病的最早的多巴胺能药物[3][4]。 (-)-Apomorphine (hydrochloride hydrate)具有很强的抗氧化和清除自由基的作用，并具有神经保护效应[5]。

(-)-Apomorphine (hydrochloride hydrate)在浓度高于 2 x10-5M时，可以显著降低retinal pigment epithelium (RPE)细胞对巩膜软骨细胞的生长刺激作用[6]。(-)-Apomorphine (hydrochloride hydrate)在体外对大鼠阴茎海绵体组织表现出强效的松弛作用，特别是对去甲肾上腺素诱导的收缩，但不改变环核苷酸水平[7]。

(-)-Apomorphine (hydrochloride hydrate)在清醒大鼠中可以诱导勃起，效果在300nmol/kg时达到峰值，但在麻醉大鼠中对基础或神经刺激的海绵体压力没有影响[7]。(-)-Apomorphine (hydrochloride hydrate)（20mg/kg，腹腔注射）处理正常4天动情周期的大鼠，可以降低了动情间期的血清催乳素水平，并防止了动情前期血清催乳素的升高[8]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Chondrocytes

Preparation Method

Chondrocytes with or without co-cultured retinal pigment epithelium (RPE) cells were treated with 2 x10-5M (-)-Apomorphine (hydrochloride hydrate) for 3 days. Then the number of chondrocytes was then counted using a Coulter counter to calculate the proliferation rate.

Reaction Conditions

2 x10-5M, 3d

Applications

(-)-Apomorphine (hydrochloride hydrate) treatment dramatically reduced the growth-stimulatory effect of RPE cells on the scleral chondrocytes.
Animal experiment [2]:

Animal models

Sprague-Dawley rats

Preparation Method

Rats were treated with Chlorpromazine (CPZ), followed by an intraperitoneal injection of (-)-Apomorphine (hydrochloride hydrate) 1 hour later. Then rats were sacrificed and their blood was collected from individual rats, allowed to clot over ice, then serum was removed and assayed for prolactin (PRL) by a double antibody radioimmunoassay.

Dosage form

20mg/kg, 1h, i.p.

Applications

(-)-Apomorphine (hydrochloride hydrate) treatment significantly lowered the elevated levels of prolactin (PRL) produced by Chlorpromazine (CPZ) pretreatment of diestrous rats.

References:
[1]. Seko Y, Tanaka Y, Tokoro T. Apomorphine inhibits the growth-stimulating effect of retinal pigment epithelium on scleral cells in vitro. Cell Biochem Funct. 1997 Sep;15(3):191-6. doi: 10.1002/(SICI)1099-0844(199709)15:3<191::AID-CBF738>3.0.CO;2-2. PMID: 9377797.
[2]. Smalstig EB, Sawyer BD, Clemens JA. Inhibition of rat prolactin release by apomorphine in vivo and in vitro. Endocrinology. 1974 Jul;95(1):123-9. doi: 10.1210/endo-95-1-123. PMID: 4857693.

产品文档 Product Documents

Purity:>95.00%

化学性质Chemical Properties

CAS 号
58117-94-5
同义词
5,6,6aR,7-tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol, monohydrochloride, hydrate
分子式
C17H17NO2 • HCl [XH2O]
分子量
303.8 g/mol
溶解性
DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 15 mg/ml; Ethanol: 1 mg/ml
保存条件
Store at -20°C
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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