NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.

  title={NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.},
  author={J Yuan and X Chen and Robbin M. Brodbeck and Renee J. Primus and Julia Braun and Jan W. F. Wasley and Andrew Thurkauf},
  journal={Bioorganic \& medicinal chemistry letters},
  volume={8 19},
Effects of Two Novel D3-Selective Compounds, NGB 2904 [N-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butyl)-9H-fluorene-2-carboxamide] and CJB 090 [N-(4-(4-(2,3-Dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide], on the Reinforcing and Discriminative Stimulus Effects of Cocaine in Rhesus M
The data indicate that compounds with relatively high affinity and selectivity for the D3 receptor can attenuate the discriminative and reinforcing stimulus effects of cocaine while not producing cocaine-like effects.
Characterization of the Transport, Metabolism, and Pharmacokinetics of the Dopamine D3 Receptor-Selective Fluorenyl- and 2-Pyridylphenyl Amides Developed for Treatment of Psychostimulant Abuse
Brain exposure levels of NGB 2904 and PG 01037 were significantly reduced after intraperitoneal administration compared with intravenous administration, suggesting decreased bioavailability via extravascular administration that may be attributed to high drug efflux and hepatic metabolism.
High-affinity and selective dopamine D₃ receptor full agonists.
Pharmacological actions of NGB 2904, a selective dopamine D3 receptor antagonist, in animal models of drug addiction.
The data reviewed in this paper suggest that NGB 2904 or other D3-selective antagonists may have potential in controlling motivation for drug-taking behavior or relapse to drug-seeking behavior, but may have a limited role in antagonizing the acute rewarding effects produced by cocaine or other addictive drugs.
S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.
S33084 is a novel, potent, selective, and competitive antagonist at hD(3)-receptors that tonically inhibit ascending dopaminergic pathways, although the latter may contribute to phasic suppression of DA release in frontal cortex.
Dopamine Receptor Subtype-Selective Drugs: D2-Like Receptors
The most interesting structural features required for high selectivity and affinity are presented as well as structure–activity relationship (SAR) studies and the use of subtype-selective radioligands is discussed.
A solid phase parallel synthesis of diverse amides as dopamine D3 receptor ligands
A solid phase parallel synthesis using SynPhase™ technology was used to couple a series of 21 carboxylic with three different 4-(4-arylpiperazinyl)butanamines, giving rise to several compounds with affinities in the low nanomolar concentration range.


Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents.
These studies establish nafadotride as a pure, extremely potent, competitive and preferential dopamine D3 receptor antagonist in vitro.
Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics
The D3 receptor is localized to limbic areas of the brain, which are associated with cognitive, emotional and endocrine functions, and seems to mediate some of the effects of antipsychotic drugs and drugs used against Parkinson's disease.
Activation of heterologously expressed D3 dopamine receptors: comparison with D2 dopamine receptors.
Comparison of the potencies at the two receptors reveals that none of the agonists is as selective for D3 receptors as was previously thought based on radioligand binding data.
Molecular neurobiology of dopaminergic receptors.