Peer-reviewed veterinary case report
Identification of a novel orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor with efficacy in animal models of schizophrenia.
- Journal:
- Journal of medicinal chemistry
- Year:
- 2015
- Authors:
- Bartolomé-Nebreda, José Manuel et al.
- Affiliation:
- Neuroscience Medicinal Chemistry and ‡ · Spain
Abstract
We report the continuation of a focused medicinal chemistry program aimed to further optimize a series of imidazo[1,2-a]pyrazines as a novel class of potent and selective phosphodiesterase 10A (PDE10A) inhibitors. In vitro and in vivo pharmacokinetic and pharmacodynamic evaluation allowed the selection of compound 25a for its assessment in preclinical models of psychosis. The evolution of our medicinal chemistry program, structure-activity relationship (SAR) analysis, as well as a detailed pharmacological profile for optimized lead 25a are described.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/25495129/