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NGB2904 | NGB2904 : Antagonist of DRD3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DRD3
  • Ki:1.4 ± 0.6 nM
  • IC50:5.0 nM
Antagonist
10-100 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within family: greater than 150-fold selectivity over all other dopamine receptor subtyp ...

Potency
Cellular
In Vitro

DRD3

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/S0960-894X(98)00469-7

In Vivo Validations

Rat
Dose: 10 mg/kg
Route of delivery: Intravenous
Plasma half life: 2.60 (plasma), 2.48 (brain) h
Systemic clearance: 2.46 ± 0.19 l/h/kg
Area Under the Curve:: 3.45 ± 0.21 (plasma), 40.78 ± 1.52 (brain) h·μg/mL
Volume of Distribution at Steady-State: 7.85 ± 1.14 L/Kg

DOI Reference: 10.1124/jpet.109.165084

Dose: 10 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 2.58 ± 1.15 h
Systemic clearance: 13.84 ± 3.51 l/h/kg
Area Under the Curve:: 0.66 ± 0.07 (plasma), 4.97 ± 1.40 (brain) h·μg/ml

DOI Reference: 10.1124/jpet.109.165084

Chemical Information

Molecular Formula C28H29Cl2N3O
SMILEs O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2
InChI InChI=1S/C28H29Cl2N3O/c29-25-8-5-9-26(27(25)30)33-16-14-32(15-17-33)13-4-3-12-31-28(34)21-10-11-24-22(19-21)18-20-6-1-2-7-23(20)24/h1-2,5-11,19H,3-4,12-18H2,(H,31,34)
Molecular weight 493.17 Da
AlogP 0.0
HBond acceptors 4
HBond donors 1
Atoms 63

Vendors

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Expert Reviews

by SERP
(on 16 Nov 2023)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 28 Dec 2023)
Cellular Use Rating
In Model Organisms
Based on the original report and other published literature (eg: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3771110/pdf/CNS-13-240.pdf.) NGB2904 has off target activity on D2, alpha1 and 5HT2 receptors....
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