AZD3783
AZD3783 is an orally active, blood-brain barrier-penetrant 5-HT1B receptor antagonist. AZD3783 reverses agonist-induced hypothermia, inhibits separation-induced vocalizations in guinea pig pups, and acts as a moderately permeable glycoprotein substrate with moderate clearance. AZD3783 inhibits hERG channel activity. AZD3783 is applicable for research on depression, anxiety disorders, and other psychiatric diseases associated with serotonergic neurotransmission.
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: 1162658-64-1
- 分子式: C26H34N4O4
- 分子量:466.57
-
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]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
5-HT Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
|
5-HT1B Receptor 12.5 nM (Ki) |
AZD3783 (Compound 1a) binds to human 5-HT1B receptors expressed on CHO cell membranes, with a Ki value of 12 nM[1].
AZD3783 (1 h) acts as a functional antagonist of the 5-HT1B receptor expressed on human CHO cell membranes, and produces 120% inhibition of 5-HT-stimulated GTPγS binding[1].
AZD3783 inhibits hERG channel activity in cell-based in vitro assays, with an IC50 of 19 μM and a maximal effect of 81% at a concentration of 100 μM[1].
AZD3783 (300 μM) exhibits pro-phospholipidogenic activity in in vitro cell assays, producing 81% of the maximum effect at a concentration of 300 μM[1].
AZD3783 (170 pM-10 μM; 1 h) exhibits high affinity for recombinant human 5-HT1B receptor, with a Ki value of 12.5 nM[2].
AZD3783 (170 pM-10 μM; 1 h) exhibits high affinity for recombinant guinea pig 5-HT1B receptors, with a Ki value of 11.1 nM[2].
AZD3783 (170 pM-10 μM; 1 h) is a reversible competitive antagonist of the recombinant human 5-HT1B receptor, with an EC50 of 42 nM for inhibiting 5-HT-induced GTPγ[35S] binding[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-∞ | CLplasma | Vdss | T1/2 | Cmax | Tmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|
| Rat[2] | 10 μmol/Kg | i.v. | 8.8 μM·h | 19 mL/min/kg | 2.3 L/kg | 1.4 h | / | / | / |
| Rat[2] | 30 μmol/Kg | p.o. | 26 μM·h | / | / | / | 9.5 μM | 0.25 h | 98 % |
| Dog[2] | 2.0 μmol/Kg | i.v. | 1.9 μM·h | 18 mL/min/kg | 4.3 L/kg | 3.7 h | / | / | / |
| Dog[2] | 2.0 μmol/Kg | p.o. | 1.1 μM·h | / | / | / | 0.24 μM | 1.00 h | 58 % |
| Monkey[2] | 3.0 μmol/Kg | i.v. | 1.5 μM·h | 35 mL/min/kg | 5.9 L/kg | 4.6 h | / | / | / |
AZD3783 (0.2-2.0 μmol/kg; subcutaneous injection; single administration) reduces separation-induced vocalizations in guinea pig pups at doses as low as 0.2 μmol/kg, exhibiting anxiolytic-like activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Dunkin-Hartley (adult, male, body weight 0.2 to 0.4 kg)[2]
-
Dosage:0.002, 0.006, 0.06, 0.2, 0.6, 2, 6, 20 μM/kg
-
Administration:s.c.; single dose
-
Result:Reversed CP135.807-induced hypothermia in a dose-dependent manner.
Achieved an unbound plasma EC50 of 18 nM for blockade of hypothermia.
Achieved an unbound brain EC50 of 16 nM for blockade of hypothermia.
-
Animal Model:Dunkin-Hartley (pups, 4 to 6 days postnatal to 23 to 25 days postnatal)[2]
-
Dosage:0.2, 0.6, 2.0 μM/kg
-
Administration:s.c.; single dose per test session
-
Result:Significantly decreased separation-induced vocalizations overall.
Produced significant reductions in vocalizations at all tested doses.
Demonstrated a minimum efficacious dose at or below 0.2 μM/kg.
化学情報
-
CAS 番号 1162658-64-1
-
分子量 466.57
-
分子式 C26H34N4O4
-
SMILES
O=C([C@@H]1OC2=C(N3CCN(CC3)C)C=C(C=C2CC1)OC)NC4=CC=C(N5CCOCC5)C=C4
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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
[1]. Nugiel DA, et al. De novo design of a picomolar nonbasic 5-HT(1B) receptor antagonist. J Med Chem. 2010 Feb 25;53(4):1876-80. [Content Brief]
[2]. Zhang M, et al. Preclinical pharmacology and pharmacokinetics of AZD3783, a selective 5-hydroxytryptamine 1B receptor antagonist. J Pharmacol Exp Ther. 2011;339(2):567-578. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AZD3783 関連分類
HY-182440 関連分類
Powered by Bioz