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A highly D₃R-selective and efficacious partial agonist (S)-ABS01-113 compared to its D₃R-selective antagonist enantiomer (R)-ABS01-113 as potential treatments for opioid use disorder.

ABSTRACT: The non-medical use of opioids has become a national crisis in the USA. Developing non-opioid pharmacotherapies for controlling this opioid epidemic is urgent. Dopamine D₃ receptor (D₃R) antagonists and low efficacy partial agonists have shown promising profiles in animal models of opioid use disorders (OUD). However, to date, advancement to human studies has been limited. Here we report the effects of (S)- and (R)-enantiomers of (±)-ABS01-113, structural analogs of the D₃R partial agonist, (±)-VK4-40, in which the 3-OH in the linking chain is replaced by 3-F group. (S)- and (R)-ABS01-113 are identical in chemical structure but with opposite chirality. In vitro receptor binding and functional assays indicate that (S)-ABS01-113 is an efficacious (55%) and po

SUBMITTER: Galaj E

PROVIDER: S-EPMC9309443 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature

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Dataset Information

A highly D₃R-selective and efficacious partial agonist (S)-ABS01-113 compared to its D₃R-selective antagonist enantiomer (R)-ABS01-113 as potential treatments for opioid use disorder.

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Dataset Information

A highly D3R-selective and efficacious partial agonist (S)-ABS01-113 compared to its D3R-selective antagonist enantiomer (R)-ABS01-113 as potential treatments for opioid use disorder.

OmicsDI is part of the ELIXIR infrastructure

Tweets

A highly D₃R-selective and efficacious partial agonist (S)-ABS01-113 compared to its D₃R-selective antagonist enantiomer (R)-ABS01-113 as potential treatments for opioid use disorder.