2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 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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AZD3676

AZD3676 Chemical Structure

CAS No. : 1259929-13-9

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AZD3676 Related Antibodies

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Description

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[1].

IC50 & Target[1][2]

5-HT1A Receptor

 

5-HT1B/D Receptor

 

In Vitro

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.

AZD3676 Related Antibodies
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 /
In Vivo

AZD3676 (10 μmol/kg; s.c.; single dose) significantly reverses R-8-OH-DPAT-induced cognitive impairment in C57BL/6 mice, as demonstrated by restored freezing behavior in a contextual fear conditioning assay[1].
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.

Animal Model: C57BL/6[1]
Dosage: 10 μmol/kg
Administration: s.c.; single dose
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.
Animal Model: C57BL/6[1]
Dosage: 3 μmol/kg; 10 μmol/kg; 1 μmol/kg
Administration: s.c.; single dose; p.o.; single dose
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.
Animal Model: C57BL/6[1]
Dosage: 0.03 μmol/kg; 0.1 μmol/kg; 0.3 μmol/kg; 1 μmol/kg; 3 μmol/kg
Administration: s.c.; single dose
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.
Animal Model: Sprague Dawley[1]
Dosage: 0.1 μmol/kg; 1 μmol/kg; 3 μmol/kg; 10 μmol/kg
Administration: s.c.; single dose
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.
Molecular Weight

378.48

Formula

C22H26N4O2
CAS No.
SMILES

O=C(C=1OC2=C(C=CC=C2N3CCN(CCC4=NC=CC=C4)CC3)C1)N(C)C
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AZD3676 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD36761259929-13-9AZD 3676AZD-36765-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorrodent models5-HT1? receptorC57BL/6 micecynomolgus monkey brain homogenatesDunkin Hartley guinea pigsAlzheimer’s diseaseSprague Dawley ratsnon-human primate braincynomolgus monkeysInhibitorinhibitorinhibit

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