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Theresa Kopajtic, B.S.

Theresa Kopajtic, B.S.

Position

Former Research Biologist, Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit

Contact

Biomedical Research Center
251 Bayview Boulevard
Baltimore, MD 21224

Education

B.S. - Biology, Towson University

Research Interests

I am a Marylander born and bred, where I attended Mercy High School and Towson University achieving a Bachelor of Science in Biology with a minor in Chemistry. During my storied tenure with the National Institute Against Drug Abuse, which spans nearly 28 years, I have had the privilege to work under the esteemed guidance of Dr. Michael Kuhar and Dr. Jonathan Katz. Since 1989 I have specialized in the field of pharmacology and drug development, specifically working with the dopamine transporter and the mu, kappa and delta opioid receptors. I live in a rural area of Maryland with my husband and two rambunctious black labs. I enjoy world travel, the culinary arts, gardening, and the ocean. My passions are my kids (adults now) and my grandson.

Theresa is now retired!

Publications


PubMed | Research Gate

Selected Publications

2016

Cao, Jianjing; Slack, Rachel D; Bakare, Oluyomi M; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J; Newman, Amy Hauck

Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors. Journal Article

In: J Med Chem, vol. 59, no. 23, pp. 10676–10691, 2016, ISSN: 1520-4804 (Electronic); 0022-2623 (Linking).

Abstract | Links

@article{Cao2016,
title = {Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.},
author = {Jianjing Cao and Rachel D Slack and Oluyomi M Bakare and Caitlin Burzynski and Rana Rais and Barbara S Slusher and Theresa Kopajtic and Alessandro Bonifazi and Michael P Ellenberger and Hideaki Yano and Yi He and Guo-Hua Bi and Zheng-Xiong Xi and Claus J Loland and Amy Hauck Newman},
url = {https://www.ncbi.nlm.nih.gov/pubmed/27933960},
doi = {10.1021/acs.jmedchem.6b01373},
issn = {1520-4804 (Electronic); 0022-2623 (Linking)},
year = {2016},
date = {2016-12-08},
journal = {J Med Chem},
volume = {59},
number = {23},
pages = {10676--10691},
address = {Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.},
abstract = {The development of pharmacotherapeutic treatments of psychostimulant abuse has remained a challenge, despite significant efforts made toward relevant mechanistic targets, such as the dopamine transporter (DAT). The atypical DAT inhibitors have received attention due to their promising pharmacological profiles in animal models of cocaine and methamphetamine abuse. Herein, we report a series of modafinil analogues that have an atypical DAT inhibitor profile. We extended SAR by chemically manipulating the oxidation states of the sulfoxide and the amide functional groups, halogenating the phenyl rings, and/or functionalizing the terminal nitrogen with substituted piperazines, resulting in several novel leads such as 11b, which demonstrated high DAT affinity (Ki = 2.5 nM) and selectivity without producing concomitant locomotor stimulation in mice, as compared to cocaine. These results are consistent with an atypical DAT inhibitor profile and suggest that 11b may be a potential lead for development as a psychostimulant abuse medication.},
keywords = {},
pubstate = {published},
tppubtype = {article}
}

Close

The development of pharmacotherapeutic treatments of psychostimulant abuse has remained a challenge, despite significant efforts made toward relevant mechanistic targets, such as the dopamine transporter (DAT). The atypical DAT inhibitors have received attention due to their promising pharmacological profiles in animal models of cocaine and methamphetamine abuse. Herein, we report a series of modafinil analogues that have an atypical DAT inhibitor profile. We extended SAR by chemically manipulating the oxidation states of the sulfoxide and the amide functional groups, halogenating the phenyl rings, and/or functionalizing the terminal nitrogen with substituted piperazines, resulting in several novel leads such as 11b, which demonstrated high DAT affinity (Ki = 2.5 nM) and selectivity without producing concomitant locomotor stimulation in mice, as compared to cocaine. These results are consistent with an atypical DAT inhibitor profile and suggest that 11b may be a potential lead for development as a psychostimulant abuse medication.

Close

  • https://www.ncbi.nlm.nih.gov/pubmed/27933960
  • doi:10.1021/acs.jmedchem.6b01373

Close

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  • Treatment Information
  • Contact Us
  • Careers at NIDA IRP
  • Accessibility
  • Privacy
  • HHS Vulnerability Disclosure
  • Freedom of Information Act
  • Document Viewing Tools
  • Offsite Links

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    • Administrative Management Branch
    • Molecular Targets and Medications Discovery Branch
    • Cellular and Neurocomputational Systems Branch
    • Molecular Neuropsychiatry Research Branch
    • Neuroimaging Research Branch
    • Behavioral Neuroscience Research Branch
    • Integrative Neuroscience Research Branch
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