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.
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- CAS No.: 1162658-64-1
- Formule: C26H34N4O4
- Masse moléculaire:466.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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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.
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Animal Model:Dunkin-Hartley (adult, male, body weight 0.2 to 0.4 kg)[2]
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Dosage:0.002, 0.006, 0.06, 0.2, 0.6, 2, 6, 20 μM/kg
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Administration:s.c.; single dose
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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.
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Animal Model:Dunkin-Hartley (pups, 4 to 6 days postnatal to 23 to 25 days postnatal)[2]
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Dosage:0.2, 0.6, 2.0 μM/kg
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Administration:s.c.; single dose per test session
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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.
Chemical Information
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CAS No. 1162658-64-1
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Masse moléculaire 466.57
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Formule C26H34N4O4
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SMILES
O=C([C@@H]1OC2=C(N3CCN(CC3)C)C=C(C=C2CC1)OC)NC4=CC=C(N5CCOCC5)C=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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