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(+)-AJ 76 hydrochloride Sale

目录号 : GC13156

(+)-AJ 76 hydrochloride是一种对突触前受体具有优先作用的多巴胺受体(dopamine receptors, DRs)拮抗剂(hD3、hD4、hD2S、hD2L和rD2受体的pKi值分别为6.95、6.67、6.37、6.21和6.07)。

(+)-AJ 76 hydrochloride Chemical Structure

Cas No.:85379-09-5

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5mg
¥990.00
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10mg
¥1,530.00
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25mg
¥3,420.00
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Sample solution is provided at 25 µL, 10mM.

Description

(+)-AJ 76 hydrochloride is a dopamine receptors (DRs) antagonist [1] with preferential action at presynaptic receptors (pKi values are 6.95, 6.67, 6.37, 6.21 and 6.07 at hD3, hD4, hD2S, hD2L and rD2 receptors respectively). Dopamine is not only a neurotransmitter involved in motor, cognitive, and reward regulation, but it also plays an immunomodulatory role in the central and peripheral nervous systems[2]. (+)-AJ 76 hydrochloride can increase extracellular dopamine concentration by blocking presynaptic inhibitory receptors D2R and/or D3R on dopaminergic neuron terminals, which promotes dopamine transmission[3], and is therefore commonly used in neurology and studies of neurological related diseases such as Alzheimer's disease.

In vitro, (+)-AJ 76 hydrochloride (1μM) treatment of HEK 293 cells transfected with the D3 receptor for 35min reduced cellular phospholipase D (PLD) levels[4].

In vivo, MitoPark mice treated with intraperitoneal injection (+)-AJ 76 hydrochloride (20mg/kg) for 60 minutes significantly reduced the levels of DOPAC (3,4-Dihydroxyphenylacetic acid) in mouse cerebrospinal fluid and HVA (homovanillic acid) in mouse cerebrospinal fluid and plasma, suggesting that dopamine neuron challenge Test (DNC Test) using (+)-AJ 76 hydrochloride is helpful for early detection of PD (Parkinson’s disease)[5]. (+)-AJ 76 hydrochloride (300μmol/kg/day) fed to male Sprague-Dawley rats for 7 days increased voluntary activity activity and DOPAC levels in the striatum[6].

References: 
[1] Svensson K, Johansson AM, Magnusson T, Carlsson A. (+)-AJ 76 and (+)-UH 232: central stimulants acting as preferential dopamine autoreceptor antagonists. Naunyn Schmiedebergs Arch Pharmacol. 1986 Nov;334(3):234-45. doi: 10.1007/BF00508777. PMID: 2880302.
[2] Channer, Breana et al. “Dopamine, Immunity, and Disease.” Pharmacological reviews vol. 75,1 (2023): 62-158. doi:10.1124/pharmrev.122.000618
[3] Waters N, Lagerkvist S, Löfberg L, Piercey M, Carlsson A. The dopamine D3 receptor and autoreceptor preferring antagonists (+)-AJ76 and (+)-UH232; a microdialysis study. Eur J Pharmacol. 1993 Sep 28;242(2):151-63. doi: 10.1016/0014-2999(93)90075-s. PMID: 8253112.
[4] Everett PB, Senogles SE. D3 dopamine receptor activates phospholipase D through a pertussis toxin-insensitive pathway. Neurosci Lett. 2004 Nov 16;371(1):34-9. doi: 10.1016/j.neulet.2004.08.033. PMID: 15500962.
[5] Zhou, Jingheng et al. “AJ76 and UH232 as potential agents for diagnosing early-stage Parkinson's disease.” Neuropharmacology vol. 226 (2023): 109397. doi:10.1016/j.neuropharm.2022.109397
[6] Kullingsjö H, Carlsson A, Svensson K. Effects of repeated administration of the preferential dopamine autoreceptor antagonist, (+)-AJ76, on locomotor activity and brain DA metabolism in the rat. Eur J Pharmacol. 1991 Dec 3;205(3):241-6. doi: 10.1016/0014-2999(91)90904-5. PMID: 1817961.

(+)-AJ 76 hydrochloride是一种对突触前受体具有优先作用的多巴胺受体(dopamine receptors, DRs)拮抗剂(hD3、hD4、hD2S、hD2L和rD2受体的pKi值分别为6.95、6.67、6.37、6.21和6.07)[1]。多巴胺不仅是一种参与运动、认知和奖励调节的神经递质,它在中枢神经系统和外周神经系统也起免疫调节的作用[2]。而(+)-AJ 76 hydrochloride可以通过阻断多巴胺能神经元末梢上突触前抑制性受体D2R和 (或) D3R,使得细胞外多巴胺浓度升高, 促进多巴胺的传递[3],因此常用于神经学和阿尔兹海默症等神经相关疾病的研究。

在体外,(+)-AJ 76 hydrochloride(1μM)处理转染D3受体的HEK 293细胞35min,可降低细胞磷脂酶D(phospholipase D,PLD)的水平[4]

在体内,(+)-AJ 76 hydrochloride(20mg/kg)腹腔注射处理MitoPark mice小鼠60分钟,显著降低了小鼠脑脊液中3,4-二羟基苯乙酸(3,4-Dihydroxyphenylacetic acid, DOPAC)和小鼠脑脊液和血浆中高香草酸(homovanillic acid, HVA)的水平,揭示使用(+)-AJ 76 hydrochloride的多巴胺神经元挑战试验(Dopamine Neuron Challenge Test, DNC Test)有助于帕金森病(Parkinson’s disease , PD)的早期检测[5]。(+)-AJ 76 hydrochloride(300μmol/kg/day)喂食雄性Sprague-Dawley大鼠7天,可以提高大鼠纹状体的自主活动活动和DOPAC水平[6]

实验参考方法

Cell experiment [1]:

Cell lines

HEK 293 cells

Preparation Method

Firstly, transient transfection of human D3 receptor into HEK 293 cells, 24 hours post-transfection, HEK 293 cells were plated in 12-well cluster dishes and labeled with 10μCi/well (μCi is a unit of radioactive activity) of [3H]-myristic acid for 48h. Then added (+)-AJ 76 hydrochloride (1μM) for 5min. Finally, PLD (phospholipase D) activity was determined by the transphosphatidylation reaction in the presence of 1% ethanol and (+) 7-OH DPAT (a D3 receptor agonist) indicated for 30min at 37°C.

Reaction Conditions

1μM; 35min

Applications

D3 receptor selective antagonists (+) 7-OH DPAT (a D3 receptor agonist) at a concentration of 1μM ablated D3 receptor-mediated PLD (phospholipase D) activity.

Animal experiment [2]:

Animal models

MitoPark mice

Preparation Method

The 20-week-old MitoPark mouse were injected with (+)-AJ 76 hydrochloride (20mg/kg) for 60min, then collected the CSF (cerebrospinal fluid) and plasma sample and compared the levels of DOPAC (3,4-Dihydroxyphenylacetic acid) and HVA (homovanillic acid) in CSF samples and the level of HVA in plasma samples between 20-week-old MitoPark mice and their littermate controls at the resting state.

Dosage form

20mg/kg for 60min; i.p. injection

Applications

The levels of HVA in plasma samples of (+)-AJ 76 hydrochloride treated mice were decreased, as were the levels of HVA and DOPA in CSF sample, suggesting that the (+)-AJ 76 hydrochloride can detect Parkinson’s disease (PD) at an early stage.

References: 
[1] Everett PB, Senogles SE. D3 dopamine receptor activates phospholipase D through a pertussis toxin-insensitive pathway. Neurosci Lett. 2004 Nov 16;371(1):34-9. doi: 10.1016/j.neulet.2004.08.033. PMID: 15500962.
[2] Zhou, Jingheng et al. “AJ76 and UH232 as potential agents for diagnosing early-stage Parkinson's disease.” Neuropharmacology vol. 226 (2023): 109397. doi:10.1016/j.neuropharm.2022.109397.

化学性质

Cas No. 85379-09-5 SDF
化学名 (1S,2R)-5-methoxy-1-methyl-N-propyl-1,2,3,4-tetrahydronaphthalen-2-amine hydrochloride
Canonical SMILES CCCN[C@]1([H])CCC2=C([C@]1([H])C)C=CC=C2OC.Cl
分子式 C15H23NO.HCl 分子量 269.81
溶解度 Soluble to 10 mM in Water 储存条件 Store at RT
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1 mM 3.7063 mL 18.5316 mL 37.0631 mL
5 mM 0.7413 mL 3.7063 mL 7.4126 mL
10 mM 0.3706 mL 1.8532 mL 3.7063 mL
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