Kenner C. Rice, Ph.D.

Senior Investigator

Molecular Targets and Medications Discovery Branch, Drug Design and Synthesis Section

NIDA

9800 Medical Center Drive
MSC-3373, Room 228A
Bethesda, MD 20892

301-217-5200

kennerr@mail.nih.gov

Research Topics

Our major research direction is the elucidation of the structure and function of neurotransmitter systems in the mammalian central nervous system (CNS) in normal, drug-altered, and pathological states and the molecular mechanism of action of CNS active drugs. Organic/medicinal chemistry is the foundation of the multidisciplinary approach utilized in these studies that requires the rational design and chemical synthesis of novel agonists, antagonists, imaging agents, affinity ligands, and other drugs for particular applications. Our principal focus is the application of these techniques to study the mechanism of action of abused drugs and the development of medications for the treatment and prevention of drug abuse. Our present research areas are: (1) opioid receptor subtypes and bifunctional ligands, (2) design and synthesis of highly G-protein biased opioid agonists as potential replacements for medical narcotics presently in use (3) design and synthesis of haptens for vaccine construction for treatment and prevention of drug abuse (4) design and synthesis of Toll-4 receptor antagonists (5) synthesis and pharmacology of new clandestine designer drugs. The multidisciplinary nature of this program requires extensive collaboration with other groups with diverse pharmacological and biological expertise from within and outside of NIH. These studies also require complex, multistep chemical synthesis of multigram and larger quantities of target compounds. Our program has provided potential medications, many new research tools, and much valuable technology for drug abuse research. The latter includes the development of the NIH Opiate Total Synthesis that offers synthetic production of both enantiomers of medical opiates and their antagonists and thus independence from foreign sources of opium.

Selected Publications

  1. Sulima A, Jalah R, Antoline JFG, Torres OB, Imler GH, Deschamps JR, Beck Z, Alving CR, Jacobson AE, Rice KC, Matyas GR. A Stable Heroin Analogue That Can Serve as a Vaccine Hapten to Induce Antibodies That Block the Effects of Heroin and Its Metabolites in Rodents and That Cross-React Immunologically with Related Drugs of Abuse. J Med Chem. 2018;61(1):329-343.

  2. Barrientos RC, Bow EW, Whalen C, Torres OB, Sulima A, Beck Z, Jacobson AE, Rice KC, Matyas GR. Novel Vaccine That Blunts Fentanyl Effects and Sequesters Ultrapotent Fentanyl Analogues. Mol Pharm. 2020.

  3. Wang M, Irvin TC, Herdman CA, Hanna RD, Hassan SA, Lee YS, Kaska S, Crowley RS, Prisinzano TE, Withey SL, Paronis CA, Bergman J, Inan S, Geller EB, Adler MW, Kopajtic TA, Katz JL, Chadderdon AM, Traynor JR, Jacobson AE, Rice KC. The Intriguing Effects of Substituents in the <i>N</i>-Phenethyl Moiety of Norhydromorphone: A Bifunctional Opioid from a Set of "Tail Wags Dog" Experiments. Molecules. 2020;25(11).

  4. Selfridge BR, Deschamps JR, Jacobson AE, Rice KC. Synthesis of enantiopure 10-nornaltrexones in the search for Toll-like receptor 4 antagonists and opioid ligands. J Org Chem. 2014;79(11):5007-18.

  5. Selfridge BR, Wang X, Zhang Y, Yin H, Grace PM, Watkins LR, Jacobson AE, Rice KC. Structure-Activity Relationships of (+)-Naltrexone-Inspired Toll-like Receptor 4 (TLR4) Antagonists. J Med Chem. 2015;58(12):5038-52.


This page was last updated on November 2nd, 2018