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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 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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