Alentemol
Alentemol (U-66444B (free base)) is a blood-brain barrier-permeable dopamine receptor D1, D2, D3, and D4 agonist. Alentemol inhibits dopamine release, reduces dopamine synthesis, regulates dopamine metabolism, suppresses the impulse activity of dopaminergic neurons, and decreases the impulse frequency of dopaminergic neurons in the substantia nigra pars compacta and ventral tegmental area. Alentemol is applicable to research related to schizophrenia.
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- CAS 番号: 112891-97-1
- 分子式: C19H25NO
- 分子量:283.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Dopamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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D1 Receptor |
D2 Receptor |
D3 Receptor |
D4 Receptor |
体内実験
Alentemol (0.001-0.1 mg/kg; s.c.) inhibits dopamine synthesis in healthy male Sprague-Dawley rats, with enhanced efficacy when presynaptic terminals are isolated from postsynaptic feedback via gamma-butyrolactone[1].
Alentemol (3.0 μg/kg; i.v.; single dose; 6 mg/kg; daily; 14 days) acts as a potent dopaminergic autoreceptor agonist with an ED50 of 3.0 μg/kg i.v. for inhibiting SNPC neurons, three times more potent than Apomorphine (HY-12723), and shows weak tolerance development following 14 days of daily 6 mg/kg administration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CF-1 (male, 18-22 g; 25-35 g for striatal 3-methoxytyramine studies)[1]
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Dosage:10.0 mg/kg (hypothermia testing); 0.001-10.0 mg/kg (locomotor activity inhibition); 0.0001-0.1 mg/kg (d-amphetamine-stimulated locomotor activity antagonism); 0.0001-0.1 mg/kg (striatal 3-methoxytyramine measurement); 1.0 mg/kg (brain concentration analysis)
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Administration:i.p. (hypothermia testing); s.c. (locomotor activity inhibition, d-amphetamine-stimulated locomotor activity antagonism, striatal 3-methoxytyramine measurement, single dose for brain concentration analysis); p.o. (single dose for brain concentration analysis)
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Result:Induced hypothermia, an effect blocked by haloperidol but not yohimbine.
Inhibited locomotor activity by 24% at 10.0 mg/kg, 25% at 3.0 mg/kg, 50% at 1.0 mg/kg, 33% at 0.3 mg/kg, 63% at 0.1 mg/kg, 62% at 0.03 mg/kg, 56% at 0.01 mg/kg, 54% at 0.003 mg/kg, and 28% at 0.001 mg/kg; this inhibition was blocked by haloperidol at 0.02 mg/kg.
Antagonized d-amphetamine-stimulated locomotor activity by 82% at 0.1 mg/kg, 69% at 0.01 mg/kg, 52% at 0.003 mg/kg, 26% at 0.001 mg/kg, and 48% at 0.0003 mg/kg.
Reduced striatal 3-methoxytyramine (an index of dopamine release) to 26% of control at 0.1 mg/kg, 52% of control at 0.01 mg/kg, and 70% of control at 0.001 mg/kg.
Achieved brain concentrations of 116 ng/g at 30 minutes, 40 ng/g at 60 minutes, and 13 ng/g at 120 minutes after 1.0 mg/kg s.c. administration; achieved a brain concentration of 27 ng/g at 60 minutes after 1.0 mg/kg p.o. administration.
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Animal Model:Sprague-Dawley (male, approximately 150 g)[1]
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Dosage:0.001-0.1 mg/kg
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Administration:s.c.
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Result:Reduced striatal DOPA concentration (an index of dopamine synthesis) to 34% of control at 0.1 mg/kg and 62% of control at 0.01 mg/kg; 0.001 mg/kg resulted in striatal DOPA levels at 74% of control.
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Animal Model:Sprague-Dawley (male, 300-400 g, chloral hydrate-anesthetized)[2]
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Dosage:3.0 μg/kg (acute electrophysiology); 6 mg/kg (chronic tolerance assessment)
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Administration:i.v.; single dose (acute electrophysiology); daily; 14 days (chronic tolerance assessment)
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Result:Depressed dopaminergic neurons in SNPC and VTA with three times the potency of Apomorphine.
Inhibited SNPC neurons with an ED50 of 3.0 μg/kg i.v.
Induced similar responses in dopaminergic cells in the VTA.
Had its induced inhibition of SNPC and VTA cells reversed by haloperidol.
Showed weak propensity to produce tolerance, as chronically treated rats still responded to its potent dopaminergic autoreceptor agonist effects.
化学情報
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CAS 番号 112891-97-1
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分子量 283.41
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分子式 C19H25NO
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SMILES
OC1=CC2=C3C(CC(N(CCC)CCC)C2)=CC=CC3=C1
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別名
U-66444B free base
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Alentemol 関連分類
HY-124524 関連分類
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