What question did this study set out to answer?

To synthesize and evaluate novel atypical dopamine transporter inhibitors that display high target affinity, reduced hERG channel liability, and lack cocaine-like abuse potential.

August 16, 2026Journal of Medicinal ChemistryOpen Access

A Series ofAryl-Substituted-(biphenyl)methyl-sulfinylmethylthiazolesas Novel and Atypical Dopamine Transporter Inhibitors

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Authors

GCGisela A. Camacho-HernandezNational Institutes of Health JCJianjing CaoNational Institutes of Health AOAmarachi OkoromNational Institutes of Health

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Implication

Preclinical evaluation shows novel sulfinylmethylthiazoles inhibit dopamine transporters without addictive behaviors in mice, suggesting potential treatments for psychostimulant dependence.

Key Points

To synthesize and evaluate novel atypical dopamine transporter inhibitors that display high target affinity, reduced hERG channel liability, and lack cocaine-like abuse potential.
Synthesized a series of aryl-substituted-(biphenyl)methyl-sulfinylmethylthiazoles and screened for human dopamine transporter (hDAT) binding affinity and hERG channel activity.
Assessed in vivo brain penetrability, target engagement, locomotor stimulation, and conditioned place preference in mice.
Identified lead molecules 32b and 39b displaying high binding affinity at hDAT (Ki = 63.0 nM and 78.5 nM, respectively) alongside low predicted micromolar activity at the hERG channel.
Demonstrated target engagement and brain penetrability in mice without inducing cocaine-like locomotor activation or conditioned place preference.

Cite This Study

Camacho-Hernandez et al. (2026) studied this question.

synapsesocial.com/papers/6a817a11f2fb91fc834adb24 https://doi.org/10.1021/acs.jmedchem.6c01907

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Implication

Preclinical evaluation shows novel sulfinylmethylthiazoles inhibit dopamine transporters without addictive behaviors in mice, suggesting potential treatments for psychostimulant dependence.

A Series ofAryl-Substituted-(biphenyl)methyl-sulfinylmethylthiazolesas Novel and Atypical Dopamine Transporter Inhibitors

Discussion

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Implication

Key Points

Cite This Study

A Series ofAryl-Substituted-(biphenyl)methyl-sulfinylmethylthiazolesas Novel and Atypical Dopamine Transporter Inhibitors

Discussion

Member takes

Implication

Key Points

Cite This Study

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