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David Lapinsky, Ph.D.

Assistant Professor of Medicinal Chemistry
Mylan School of Pharmacy
Pharmaceutical Sciences

Mellon 422B
Phone: 412.396.6069

Education:

Ph.D., Medicinal Chemistry, The Ohio State University, 2003
B.S., Pharmacy, Duquesne University, 1997
Research

Watch a video that explains the research done in the Lapinski lab

My research group primarily focuses on the design and synthesis of chemical probes as tools for mapping drug-binding pockets within central nervous system (CNS) proteins such asmonoamine transporters, nicotinic acetylcholine receptors, and metabotropicglutamate receptors.  Such probes are tremendously valuable for carrying out structure-function studies of these therapeutically significantproteins.  Collaborative efforts featuring computer molecularmodeling-guided site-directed mutagenesis of amino acid residues and molecular pharmacology of the obtained mutant proteins are employed in elucidating binding sites for abused psychostimulants (e.g., cocaine,amphetamine), antidepressants, and other CNS drugs.& nbsp; These molecular models are also used in virtual screening of small molecule structural libraries in search of novel drug candidates. Such lead compounds are then tested as candidate therapeutics for a variety of CNS disordersor become the subject of a medicinal chemistry drug development program. Our research team consists of molecular pharmacologists, computational chemists, synthetic organic medicinal chemists, biophysical chemists, and behavioral neuropharmacologists at Duquesne University and several other research institutes.

Grants/Contracts

R03DA027081 NIDA NIH Grant (Early Career Award in the Chemistry of Drug Abuse)
Principal Investigator: D. J. Lapinsky, Ph.D.
Co-investigators: C. K. Surratt, Ph.D. and J. D. Madura, Ph.D.
Non-Tropane Irreversible Dopamine Transporter Ligands
$364,182
7/1/09 to 6/30/11

Duquesne University Faculty Development Fund
Principal Investigator: D. J. Lapinsky, Ph.D.
Co-investigators: C. K. Surratt, Ph.D. and J. D. Madura, Ph.D.
The Search for Medications to Treat Psychostimulant Dependence: Rational Drug Design by Molecular Hybridization of Modafinil and Piperazine-Based Dopamine Transporter Inhibitors
$7,137
5/1/09 to 6/30/11

R01DA026530 National Institute on Drug Abuse (NIDA) NIH Grant
Principal Investigator: C. K. Surratt, Ph.D.
Co-investigators: J. D. Madura, Ph.D. and D. J. Lapinsky, Ph.D.
Dopamine Transporter Structure and Function
$627,250
7/1/09 to 6/30/11

R01DA027806 NIDA NIH/NSF Grant
Principal Investigator: J. D. Madura, Ph.D.
Co-investigators: C. K. Surratt, Ph.D. and D. J. Lapinsky, Ph.D.
CRCNS: Computational and Experimental Study of Dopamine and Serotonin Transporters
$1,545,450
7/1/09 to 6/30/14

Publications

Evolution of a compact photoprobe for the dopamine transporter based on threo-methylphenidate.  By Lapinsky, David J.; Yarravarapu, Nageswari; Nolan, Tammy L.; Surratt, Christopher K.; Lever, John R.; Tomlinson, Michael; Vaughan, Roxanne A.; Deutsch, Howard M.  From ACS Medicinal Chemistry Letters (2012), dx.doi.org/10.1021/ml3000098.

Bupropion binds to two sites in the Torpedo nicotinic acetylcholine receptor transmembrane domain: A photoaffinity labeling study with the bupropion analogue [125I]-SADU-3.72.  By Pandhare, Akash; Hamouda, Ayman K.; Staggs, Brandon; Aggarwal, Shaili; Duddempudi, Phaneendra K.; Lever, John R.; Lapinsky, David J.; Jansen, Michaela; Cohen, Jonathan B.; Blanton, Michael P.  From Biochemistry (2012), 51, 2425-2435.

2-(N-tert-butylamino)-3'-[125I]-iodo-4'-azidopropiophenone: A dopamine transporter and nicotinic acetylcholine receptor photoaffinity ligand based on bupropion (Wellbutrin, Zyban).  By Lapinsky, David J.; Aggarwal, Shaili; Nolan, Tammy L.; Surratt, Christopher K.; Lever, John R.; Acharya, Rejwi; Vaughan, Roxanne A.; Pandhare, Akash; Blanton, Michael P.  From Bioorganic & Medicinal Chemistry Letters (2012), 22, 523-526.

Identification of a novel selective serotonin reuptake inhibitor by coupling monoamine transporter-based virtual screening and rational molecular hybridization.  By Nolan, Tammy L.; Lapinsky, David J.; Talbot, Jeffery N.; Indarte, Martin; Liu, Yi; Manepalli, Sankar; Geffert, Laura M.; Amos, Mary Ellen; Taylor, Philip N.; Madura, Jeffry D.; Surratt, Christopher K. From ACS Chemical Neuroscience (2011), 2, 544-552.

Azido-iodo-N-benzyl derivatives of threo-methylphenidate (Ritalin, Concerta): Rational design, synthesis, pharmacological evaluation, and dopamine transporter photoaffinity labeling.  By Lapinsky, David J.; Velagaleti, Ranganadh; Yarravarapu, Nageswari; Liu, Yi; Huang, Yurong; Surratt, Christopher K.; Lever, John R.; Foster, James D.; Acharya, Rejwi; Vaughan, Roxanne A.; Deutsch, Howard M.  From Bioorganic & Medicinal Chemistry (2011), 19, 504-512.

A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.  By Lapinsky, David J.; Aggarwal, Shaili; Huang, Yurong; Surratt, Christopher K.; Lever, John R.; Foster, James D.; Vaughan, Roxanne A.  From Bioorganic & Medicinal Chemistry (2009), 17, 3770-3774.

Substitution effects in intramolecular aziridine-allylsilane cyclizations.  By Lapinsky, David J.; Pulipaka, Aravinda B.; Bergmeier, Stephen C.  From Tetrahedron (2009), 65, 741-747.

Presentations

Structure-based virtual screening for monoamine transporter inhibitors.  By Madura, Jeffry D.; Manepalli, Sankar; Nolan, Tammy L.; Geffert Laura; Lapinsky, David J.; Surratt, Christopher K.  From Abstracts of Papers, 243rd ACS National Meeting, San Diego, CA, United States, March 25-29, 2009 (2012), COMP-627.

Development of novel photoaffinity ligands for the dopamine transporter based on pyrovalerone.  By Aggarwal, Shaili; Lapinsky, David J.; Huang, Yurong; Surratt, Christopher K.; Lever, John R.; Foster, James D.; Vaughan, Roxanne A.; Manepalli, Sankar; Madura, Jeffry D. From Abstracts of Papers, 238th ACS National Meeting, Washington, DC, United States, August 16-20, 2009 (2009), MEDI-325.

Elucidation of binding profile similarities across structurally diverse ligands using a 3D dopamine transporter model.  By Manepalli, Sankar; Madura, Jeffry D.; Lapinsky, David J.; Surratt, Christopher K. From Abstracts of Papers, 238th ACS National Meeting, Washington, DC, United States, August 16-20, 2009 (2009), COMP-235.

Courses

PHBM 423 Biomedical Sciences & Therapeutics II (Inflammation / Pain / Rheumatology / Gastrointestinal Diseases / Geriatrics / Pediatrics)

PHBM 425 Biomedical Sciences & Therapeutics IV (Endocrinology / Nutrition)

PHBM 426 Biomedical Sciences & Therapeutics V (Infectious Disease)

PHBM 427 Biomedical Sciences & Therapeutics VI (Hematology / Oncology / Transplant / Pulmonary)

GPSC 523 Advanced Medicinal Chemistry I

GPSC 527 Advanced Medicinal Chemistry II

GPSC 623 Selected Topics in Medicinal Chemistry

GPSC 691/692 Medicinal Chemistry Seminar