A-77636
Based on 1 publication(s) in Google Scholar
A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity.
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- CAS 番号: 778546-51-3
- 分子式: C20H27NO3
- 分子量:329.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 A-77636
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生物活性
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Dopamine D1 receptor 1.1 nM (EC50) |
Dopamine D1 receptor 39.8 nM (Ki) |
A-77636 (1-10 mg/kg) attenuates addiction-induced locomotor activity in a dose-dependent manner[2].
A-77636 produce forelimb clonus in rats (ED50=12.3 μmol/kg s.c.) and mice (ED50=12.1 μmol/kg s.c.)[1].
In marmosets treated with MPTP to induce a parkinsonian-like state, A-77636 (0.5, 1.0 or 2.0 μmol/kg, p.o.) increases locomotor activity and decreases the severity of the parkinsonian-like symptoms: the compound is active after either subcutaneous or oral administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats with unilateral 6-OHDA (6-hydroxydopamine) lesions of the nigrostriatal pathway (six/group)[1]
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Dosage:0.32, 1.0, 3.2 μmol/kg
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Administration:Subcutaneously
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Result:Elicited prolonged (> 20 h) contralateral turning, which was blocked by SCH 23390, a D1 receptor antagonist, but not by haloperidol at doses selective for the dopamine D2 receptor.
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Animal Model:Male Swiss Webster mice (18-25 g, five or six per cage)[2]
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Dosage:1, 3, 10 mg/kg
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Administration:
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Result:Attenuated addiction-induced locomotor activity in a dose-dependent manner. When administered alone, 1 and 3 mg/kg A-77636 produced little change in locomotor activity, whereas 10 mg/kg produced a significant and substantial decrease in locomotor activity.
化学情報
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CAS 番号 778546-51-3
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分子量 329.43
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分子式 C20H27NO3
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SMILES
NC[C@@H]1O[C@H](C2(C[C@@H]3C4)C[C@H](C3)C[C@H]4C2)CC5=C(O)C(O)=CC=C51
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Nature
2023 Dec;624(7992):672-681. PMID: 37935376
純度とドキュメンテーション
参考文献
[1]. Kebabian JW, et al. A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets. Eur J Pharmacol. 1992 Dec 15;229(2-3):203-9. [Content Brief]
[2]. Chausmer AL, et al. Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodents. Psychopharmacology (Berl). 2002 Jan;159(2):145-53. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
A-77636 関連分類
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