Division of Pharmaceutical Sciences

Faculty

David J. Lapinsky, Ph.D. Assistant Professor of Medicinal Chemistry 422 B Mellon T 412.396.6069 L 412.396.1973 (450 Mellon) F 412.396.5593 lapinskyd@duq.edu

Educational Background

B.S. (cum laude, Pharmacy) – Duquesne University
Ph.D. (Medicinal Chemistry) – The Ohio State University
Postdoctoral Fellow – Johns Hopkins University
Wiess Instructor of Chemistry – Rice University

Courses

• PHBM 423 – Biomedical Sciences & Therapeutics II (Inflammation / Pain / Rheumatology / Gastrointestinal Diseases / Geriatrics / Pediatrics)
• PHBM 425 – Biomedical Sciences & Therapeutics IV (Endocrinology / Nutrition)
• PHBM 427 – Biomedical Sciences & Therapeutics VI (Hematology / Oncology / Transplant / Pulmonary) (Coursemaster)
• GPSC 523 – Advanced Medicinal Chemistry I (Coursemaster)
• GPSC 527 – Advanced Medicinal Chemistry II
• GPSC 623 – Selected Topics in Medicinal Chemistry
• GPSC 691/692 – Medicinal Chemistry Seminar

Active Grants

• 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 – 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 – 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 – 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 – 6/30/14

Research Interests

- My research group primarily focuses on the design and synthesis of molecular probes as tools for mapping drug-binding pockets within plasma membrane monoamine (dopamine, norepinephrine, and serotonin) transporter (MAT) proteins. Such probes are tremendously valuable for carrying out structure-function studies of these important proteins. Collaborative efforts featuring computer molecular modeling-guided site-directed mutagenesis of transporter amino acid residues and molecular pharmacology of the obtained mutant transporters are employed in elucidating binding sites for abused psychostimulants (e.g., cocaine, amphetamine), antidepressants, and other CNS drugs. These molecular models are also used in virtual screening of small molecule structural libraries in search of novel MAT ligands. Such ligands are then tested as candidate “lead compound” therapeutics for a variety of CNS disorders or become the subject for additional drug design. Our research team consists of molecular pharmacologists, computational chemists, synthetic organic medicinal chemists, biophysical chemists, and behavioral neuropharmacologists at Duquesne University, the University of Pittsburgh, NIH, and several other research institutes.

 

Representative Partial List of Publications and Presentations

• “Three-membered ring systems.” By Bergmeier, Stephen C.; Lapinsky, David J. From Progress in Heterocyclic Chemistry (2009), 21, 69-93.
• “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.
• “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(11), 3770-3774.
• “Substitution effects in intramolecular aziridine-allylsilane cyclizations.” By Lapinsky, David J.; Pulipaka, Aravinda B.; Bergmeier, Stephen C. From Tetrahedron (2009), 65(4), 741-747.
• “Effects of methyllycaconitine and related analogues on bovine adrenal α3β4* nicotinic acetylcholine receptors.” By Bryant, Darrell L.; Free, R. Benjamin; Thomasy, Sara M.; Lapinsky, David J.; Ismail, K. A.; Arason, K. M.; Bergmeier, Stephen C.; McKay, Dennis B. From Annals of the New York Academy of Sciences (2002), 971(Chromaffin Cell), 139-141.
• “Aziridine-allylsilane-mediated synthesis of exocyclic γ-amino olefins and azabicyclo[x.y.1]-systems.” By Lapinsky, David J.; Bergmeier, Stephen C. From Tetrahedron (2002), 58(35), 7109-7117.
• “A Suzuki cross-coupling route to substituted aziridines.” By Lapinsky, David J.; Bergmeier, Stephen C. From Tetrahedron Letters (2001), 42(49), 8583-8586.