2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 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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AZD3783

AZD3783 Chemical Structure

CAS No. : 1162658-64-1

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Description

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[1][2].

IC50 & Target[1]

5-HT1B Receptor

12.5 nM (Ki)

In Vitro

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.

AZD3783 Related Antibodies
Parmacokinetics
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 / / /
In Vivo

AZD3783 (0.002-20 μM/kg; subcutaneous injection; single administration) blocks 5-HT1B agonist-induced hypothermia in guinea pigs, with a free plasma EC50 of 18 nM, and achieves dose-dependent 5-HT1B receptor occupancy in guinea pig brains, with a mean free plasma EC50 of 11 nM[2].
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.
Molecular Weight

466.57

Formula

C26H34N4O4
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AZD3783 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:

AZD37831162658-64-1AZD 3783AZD-37835-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptordogs5-HT1B receptorhERG channelcynomolgus monkeyCHO cell membraneshuman liver microsomesguinea pigratsanxietydepressionInhibitorinhibitorinhibit

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