Dataset Information

Multitarget 1,4-Dioxane Compounds Combining Favorable D₂-like and 5-HT_1A Receptor Interactions with Potential for the Treatment of Parkinson's Disease or Schizophrenia.

ABSTRACT: The effect of methoxy and hydroxy substitutions in different positions of the phenoxy moiety of the N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-phenoxyethan-1-amine scaffold on the affinity/activity for D₂-like, 5-HT_1A, and α₁-adrenoceptor subtypes was evaluated. Multitarget compounds with suitable combinations of dopaminergic and serotoninergic profiles were discovered. In particular, the 2-methoxy derivative 3 showed a multitarget combination of 5-HT_1A/D₄ agonism and D₂/D₃/5-HT_2A antagonism, which may be a favorable profile for the treatment of schizophrenia. Interestingly, the 3-hydroxy derivative 8 behaved as a partial agonist at D₂ and as a potent full agonist at D₃ and D₄

SUBMITTER: Del Bello F

PROVIDER: S-EPMC8378419 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature

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Dataset Information

Multitarget 1,4-Dioxane Compounds Combining Favorable D₂-like and 5-HT_1A Receptor Interactions with Potential for the Treatment of Parkinson's Disease or Schizophrenia.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Dataset Information

Multitarget 1,4-Dioxane Compounds Combining Favorable D2-like and 5-HT1A Receptor Interactions with Potential for the Treatment of Parkinson's Disease or Schizophrenia.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Multitarget 1,4-Dioxane Compounds Combining Favorable D₂-like and 5-HT_1A Receptor Interactions with Potential for the Treatment of Parkinson's Disease or Schizophrenia.