(−)-Apomorphine (hydrochloride hydrate)

Name: (−)-Apomorphine (hydrochloride hydrate)
SKU: GC26151
Availability: InStock
Rating: 5 (30 reviews)

(Synonyms: 5,6,6aR,7-tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol, monohydrochloride, hydrate) 目录号 : GC26151

(-)-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) Chemical Structure

Cas No.:58117-94-5

规格价格库存购买数量

10mg	¥434.00	现货
50mg	¥952.00	现货
100mg	¥1,666.00	现货

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Sample solution is provided at 25 µL, 10mM.

GlpBio产品文献引用

Nature
610.7931 (2022): 366-372

Nature
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Cell
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Cell Research
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Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
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Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
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Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

产品描述实验参考方法化学性质产品文档

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

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.

化学性质

Cas No.	58117-94-5	SDF
别名	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
溶解度	DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 15 mg/ml; Ethanol: 1 mg/ml	储存条件	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℃，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。

溶解性数据

制备储备液
		1 mg	5 mg	10 mg
	1 mM	3.2916 mL	16.4582 mL	32.9164 mL
	5 mM	0.6583 mL	3.2916 mL	6.5833 mL
	10 mM	0.3292 mL	1.6458 mL	3.2916 mL

摩尔浓度计算器
稀释计算器
分子量计算器

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动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

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第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % saline

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计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系GLPBIO）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。

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Purity: >95.00%