Uncovering Structure-Activity Relationships of Phenethylamines: Paving the Way for Innovative Mental Health Treatments. 2024

Sedat Karabulut, and Harpreet Kaur, and James W Gauld
Department of Chemistry and Biochemistry, University of Windsor, Windsor, Ontario N9B 3P4, Canada.

The rapidly evolving psychedelic industry has garnered considerable attention due to 3,4-methylenedioxymethamphetamine-assisted psychotherapy's ground-breaking success in treating moderate-to-severe Post-traumatic Stress Disorder in two Phase 3 clinical trials. This has opened Pandora's box for the development of innovative therapeutic modalities. Of particular interest are the phenethylamines and their ability to inhibit monoamine transporters. In this study, we employed the quantitative structure-activity relationship methodology to develop three vigorous models for the reuptake of serotonin, dopamine, and norepinephrine through monoamine transporters. These models were thoroughly validated using various criteria, including fitting (R2DAT = 0.869, R2SERT = 0.828, and R2NET = 0.887), internal (Q2looDAT = 0.795, Q2looSERT = 0.784, and Q2looNET = 0.820), and external (RMSEextDAT = 0.373, R2extDAT = 0.831, RMSEextSERT = 0.200, R2extSERT = 0.955, RMSEextNET = 0.318, and R2extNET = 0.711) criteria.

UI MeSH Term Description Entries

Related Publications

Sedat Karabulut, and Harpreet Kaur, and James W Gauld
January 1977, Arzneimittel-Forschung,
Sedat Karabulut, and Harpreet Kaur, and James W Gauld
January 2018, London journal of primary care,
Sedat Karabulut, and Harpreet Kaur, and James W Gauld
January 1985, Nursing times,
Sedat Karabulut, and Harpreet Kaur, and James W Gauld
February 1997, Current biology : CB,
Sedat Karabulut, and Harpreet Kaur, and James W Gauld
December 2021, Science signaling,
Sedat Karabulut, and Harpreet Kaur, and James W Gauld
August 2018, JAMA,
Sedat Karabulut, and Harpreet Kaur, and James W Gauld
January 2016, Indian journal of dentistry,
Sedat Karabulut, and Harpreet Kaur, and James W Gauld
December 2013, JEMS : a journal of emergency medical services,
Sedat Karabulut, and Harpreet Kaur, and James W Gauld
March 2012, Perspectives in public health,
Sedat Karabulut, and Harpreet Kaur, and James W Gauld
October 2005, Scientific American,
Copied contents to your clipboard!