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.
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- CAS. Nr.: 1259929-13-9
- Formel: C22H26N4O2
- Molecular Weight:378.48
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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5-HT1A Receptor |
5-HT1B/D Receptor |
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.
| 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 | / |
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.
Chemical Information
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CAS. Nr. 1259929-13-9
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Molecular Weight 378.48
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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