AZD3676
AZD3676 is an orally active and blood-brain barrier-permeable ligand for 5-HT1ₐ and 5-HT1ᵦ receptors, with nanomolar binding affinity. AZD3676 is applicable to research related to cognitive impairment in Alzheimer's disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1259929-13-9
- 分子式: C22H26N4O2
- 分子量:378.48
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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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
5-HT 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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5-HT1A Receptor |
5-HT1B/D Receptor |
体外実験
AZD3676 (16 h) exhibits nanomolar affinity for 5-HT1A (Ki = 0.13 nM) and 5-HT1B (Ki = 2.4 nM) receptors in cynomolgus monkey brain homogenates[1].
AZD3676 (0.4-20 μM) shows concentration-dependent plasma protein binding, with species-specific unbound fractions ranging from 0.014 (human) to 0.37 (guinea pig) at the predicted therapeutic maximum concentration of ~1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | CLplasma | Vdss | AUC0-inf | Cmax | T1/2 | Bioavailability |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 83 mL/min/kg | 5.2 L/kg | / | / | / | / |
| Rat[1] | 1 mg/kg | i.v. | 83 mL/min/kg | 5.2 L/kg | / | / | / | / |
| Rat[1] | 3 mg/kg | p.o. | / | / | 0.3 μM·h | 0.40 μM | 0.7 h | 21 % |
| Rat[1] | 3 mg/kg | p.o. | / | / | 0.3 μM·h | 0.40 μM | 0.7 h | 21 % |
| Dog[1] | 1 mg/kg | i.v. | 37 mL/min/kg | 3.5 L/kg | / | / | / | / |
| Dog[1] | 1 mg/kg | i.v. | 37 mL/min/kg | 3.5 L/kg | / | / | / | / |
| Dog[1] | 3 mg/kg | p.o. | / | / | 1.3 μM·h | 2.6 μM | 2.8 h | / |
| Dog[1] | 3 mg/kg | p.o. | / | / | 1.3 μM·h | 2.6 μM | 2.8 h | / |
体内実験
AZD3676 (1-10 μmol/kg; s.c., p.o.; single dose) significantly reverses Scopolamine(HY-N0296)-induced cognitive impairment in C57BL/6 mice, as demonstrated by restored freezing behavior in a contextual fear conditioning assay[1].
AZD3676 (0.03-3 μmol/kg; s.c.; single dose) dose-dependently occupies 5-HT1ₐ receptors in healthy C57BL/6 mice, with a half-maximum receptor occupancy of 0.05 μmol/kg s.c. in the frontal cortex[1].
AZD3676 (0.1-10 μmol/kg; s.c.; single dose) dose-dependently occupies 5-HT1A receptors in healthy Sprague Dawley rats, with a half-maximum receptor occupancy of 0.17 μmol/kg s.c. in the frontal cortex[1].
AZD3676 (0.3-10 μmol/kg; s.c.; single dose) dose-dependently occupies 5-HT1A and 5-HT1B receptors in healthy Dunkin Hartley guinea pigs, with half-maximum receptor occupancy values of 0.3 μmol/kg s.c. and 1.2 μmol/kg s.c., respectively[1].
AZD3676 (0.16-0.82 μmol/kg; i.v.; maintenance infusion following initial low-dose bolus) dose-dependently occupies 5-HT1A receptors in healthy cynomolgus monkeys, with a Ki,plasma of 84 nM for half-maximum occupancy in the prefrontal cortex[1].
AZD3676 (0.1-1.8 μmol/kg; i.v.; maintenance infusion following initial low-dose bolus) dose-dependently occupies 5-HT1B receptors in healthy cynomolgus monkeys, with a Ki,plasma of 72 nM for half-maximum occupancy in the occipital cortex[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6[1]
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Dosage:10 μmol/kg
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Administration:s.c.; single dose
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Result:Significantly reverted the R-8-OH-DPAT-induced memory deficit, as measured by increased freezing behavior relative to R-8-OH-DPAT-only treated mice.
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Animal Model:C57BL/6[1]
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Dosage:3 μmol/kg; 10 μmol/kg; 1 μmol/kg
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Administration:s.c.; single dose; p.o.; single dose
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Result:Significantly reverted the scopolamine-induced memory deficit at 3 μmol/kg s.c., 10 μmol/kg s.c., and 1 μmol/kg p.o., as measured by increased freezing behavior relative to scopolamine-only treated mice.
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Animal Model:C57BL/6[1]
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Dosage:0.03 μmol/kg; 0.1 μmol/kg; 0.3 μmol/kg; 1 μmol/kg; 3 μmol/kg
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Administration:s.c.; single dose
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Result:Dose-dependently occupied 5-HT1ₐ receptors in the mouse frontal cortex, with a half-maximum receptor occupancy of 0.05 μmol/kg s.c.
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Animal Model:Sprague Dawley[1]
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Dosage:0.1 μmol/kg; 1 μmol/kg; 3 μmol/kg; 10 μmol/kg
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Administration:s.c.; single dose
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Result:Dose-dependently occupied 5-HT1ₐ receptors in the rat frontal cortex, with aa half-maximum receptor occupancy of 0.17 μmol/kg s.c.
化学情報
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CAS 番号 1259929-13-9
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分子量 378.48
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分子式 C22H26N4O2
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SMILES
O=C(C=1OC2=C(C=CC=C2N3CCN(CCC4=NC=CC=C4)CC3)C1)N(C)C
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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.
プロトコル
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
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)
AZD3676 関連分類
HY-122557 関連分類
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