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A 412997 dihydrochloride

カタログ番号GC14610

選択的D4アゴニスト

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A 412997 dihydrochloride 化学構造

Cas No.: 1347744-96-0

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

412997ジヒドロクロライドは、人間およびラットのD4受容体に対するKi値がそれぞれ7.9nMおよび12.1nMである、ドーパミンD4受容体の選択的アゴニストです[1]。

ドーパミンD4受容体はGタンパク質共役受容体であり、ドーパミンによって活性化されます。認知機能、パーキンソン病、中毒性行動などに重要な役割を果たしています。

412997ジヒドロクロライドは、選択的なドーパミンD4受容体アゴニストです。カルシウムフラックス機能アッセイでは、A-412997はラットのドーパミンD4受容体をEC50値28.4nMおよび固有活性0.83で活性化しました[1]。

Spontaneous Hypertensive Rat pups(SHRの子ネズミ)では、A 412997は5回繰り返される取得モデルで獲得を有意に増加させました。短期社会的記憶では、A 412997は2回目の調査時間を有意に短くしました。Wistar ラットと Dawley ラットでは、A 412997(3 μM/kg, 10 μM/kg)は運動活性を増加させました[2]。ラットでは、A 412997は非急速眼球運動(NREM)睡眠時間を減少させ覚醒時間を増加させます。また、A 412997は急速眼球運動(REM)睡眠時間も減少させてその開始時刻を遅らせます[3]。

References:
[1].  Moreland RB, Patel M, Hsieh GC, et al. A-412997 is a selective dopamine D4 receptor agonist in rats. Pharmacol Biochem Behav, 2005, 82(1): 140-147.
[2].  Browman KE, Curzon P, Pan JB, et al. A-412997, a selective dopamine D4 agonist, improves cognitive performance in rats. Pharmacol Biochem Behav, 2005, 82(1): 148-155.
[3].  Nakazawa S, Nakamichi K, Imai H, et al. Effect of dopamine D4 receptor agonists on sleep architecture in rats. Prog Neuropsychopharmacol Biol Psychiatry, 2015, 63: 6-13.

Chemical Properties

Cas No. 1347744-96-0 SDF
Chemical Name (Z)-2-(4-(pyridin-2-yl)piperidin-1-yl)-N-(m-tolyl)acetimidic acid dihydrochloride
Canonical SMILES CC1=CC(/N=C(O)/CN2CCC(C3=CC=CC=N3)CC2)=CC=C1.Cl.Cl
Formula C19H23N3O.2HCl M.Wt 382.33
溶解度 <38.23mg/ml in Water; <19.12mg/ml in DMSO Storage Desiccate at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6155 mL 13.0777 mL 26.1554 mL
5 mM 0.5231 mL 2.6155 mL 5.2311 mL
10 mM 0.2616 mL 1.3078 mL 2.6155 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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