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Aplindore (DAB-452), a high affinity selective dopamine D2 receptor partial agonist.

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Aplindore (DAB-452) is a potent partial agonist with high affinity for dopamine D(2) and D(3) receptors. Its selective profile suggests potential for treating schizophrenia and Parkinson's disease.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Receptor Binding Assays

Background:

  • Understanding dopamine receptor interactions is crucial for treating neurological disorders.
  • Aplindore (DAB-452) is a novel compound investigated for its dopaminergic activity.

Purpose of the Study:

  • To characterize the pharmacological profile of aplindore (DAB-452).
  • To evaluate its potential as a therapeutic agent for dopaminergic-based disorders.

Main Methods:

  • Competition binding assays using [(3)H]-spiperone.
  • Guanosine 5'-O-(3-thiotriphosphate) ([(35)S]GTPgammaS) binding assays.
  • Extracellular signal-regulated kinase (ERK) phosphorylation assays.
  • Intracellular calcium flux assays ([Ca(2+)](i)-FLIPR) in CHO-K1 cells expressing human dopamine D(2) short isoform receptors.
  • Behavioral studies in 6-hydroxydopamine (6-OHDA) lesioned rats.

Main Results:

  • Aplindore demonstrated high affinity for dopamine D(2) and D(3) receptors.
  • It exhibited potent partial agonist activity across multiple assay modalities.
  • In vivo, aplindore induced contralateral turning in lesioned rats, blocked by raclopride.
  • Its potency was lower than dopamine but higher than aripiprazole.

Conclusions:

  • Aplindore possesses a dopamine D(2) receptor selective partial agonist profile.
  • This profile indicates potential efficacy in treating schizophrenia and Parkinson's disease.
  • Further research into aplindore's therapeutic applications is warranted.