A-412997 is a selective dopamine D4 receptor agonist in rats

  title={A-412997 is a selective dopamine D4 receptor agonist in rats},
  author={Robert B. Moreland and Meena V. Patel and Gin C. Hsieh and Jill M. Wetter and Kennan Marsh and Jorge D. Brioni},
  journal={Pharmacology Biochemistry and Behavior},

A-412997, a selective dopamine D4 agonist, improves cognitive performance in rats

Dopamine D4 Receptor-Selective Compounds Reveal Structure–Activity Relationships that Engender Agonist Efficacy

A series of eighteen novel ligands based on the classical D4R agonist A-412997 are reported, highlighting receptor–ligand interactions that control efficacy at D2-like receptors and may provide insights into targeted drug discovery, leading to a better understanding of the role of D4Rs in neuropsychiatric disorders.

Selective dopamine D4 receptor agonist (A-412997) improves cognitive performance and stimulates motor activity without influencing reward-related behaviour in rat

Comparing the effects of a selective D4 receptor agonist, A-412997, with methylphenidate or amphetamine in preclinical models of efficacy versus abuse liability suggests that selective activation of the D4 receptors may represent a target for the treatment of attention deficit hyperactivity disorder without the potential drug abuse liability associated with current psychostimulant therapies.

Adenosine A2A receptors modulate the dopamine D2 receptor‐mediated inhibition of synaptic transmission in the mouse prefrontal cortex

A reported positive A2AR–D2R interaction controlling PFC synaptic transmission provides a mechanistic justification for the anti‐psychotic potential of A2 AR antagonists.

A Novel Class of Dopamine D4 Receptor Ligands Bearing an Imidazoline Nucleus

Molecular docking analysis, performed using a homology model of the human D4 receptor developed using the X‐ray crystal structure of the antagonist‐bound human D3 receptor as a template, was in accordance with the binding results and provided useful information for the design of novel imidazoline D 4 receptor ligands based on this new scaffold.

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.

Role of dopamine D2-like receptors and their modulation by adenosine receptor stimulation in the reinstatement of methamphetamine seeking

These results demonstrate the sufficiency of dopamine D3 receptors to reinstate MA seeking that is inhibited when combined with adenosine A1 receptor stimulation.

Characterization of Dopamine Receptors

This unit details protocols for radioligand binding assays for various subtypes of dopamine receptor, including the most widely used, well established protocols for bindingAssays, which employ commercially available tritiated ligands.

Penile erection and yawning induced by dopamine D2-like receptor agonists in rats: influence of strain and contribution of dopamine D2, but not D3 and D4 receptors

The present data do not support a major implication of either DA D3 or D4 receptors in the control of PE and YA in rats, but indicate a preponderant role of DA D2 receptors.



Enhanced expression of dopamine D1 and glutamate NMDA receptors in dopamine D4 receptor knockout mice

The findings suggest that D1, D4, andNMDA receptors might interact functionally and that developmental absence of D4 receptors might trigger compensatory mechanisms that enhance expression of D1 receptors in NAc and CPu, and NMDA receptors in N-methyl-d-aspartic acid, NAc, CPU, and hippocampus.

Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist.

The aminomethylchroman derivative BAY x 3702 (R-(-)-2-[(chroman-2-ylmethyl)-amino]-butyl]-1,1-dioxo-benzo[d] isothiazolone hydrochloride) is a new high affinity 5-hydroxytryptamine (5-HT)1A receptor ligand found to suppress 5-HT neuronal firing in the DRN of anesthetized rats.

The dopamine D(4) receptor: one decade of research.

Dopamine receptors: from structure to function.

Target deletion of several of these dopamine receptor genes in mice should provide valuable information about their physiological functions and provide unequivocal evidence for the involvement of one of these receptors in the etiology of various central nervous system disorders.

Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats.

The ability of ABT-724 to facilitate penile erection together with the favorable side-effect profile indicates that ABT -724 could be useful for the treatment of erectile dysfunction.

Two Novel and Selective Nonimidazole Histamine H3 Receptor Antagonists A-304121 and A-317920: I. In Vitro Pharmacological Effects

In vitro pharmacological data for two novel piperazine amide ligands represent useful leads for the development of H3R antagonist therapeutic agents.

Differential regional and cellular distribution of dopamine D2‐like receptors: An immunocytochemical study of subtype‐specific antibodies in rat and human brain

Differential patterns of D2, D3, and D4 receptor expression in rat and human brain should shed light on the therapeutic actions of neuroleptic drugs and may lead to the development of more specifically targeted antipsychotic drugs.