Malgorzata Dukat, Ph.D. Associate Professor of Medicinal Chemistry mdukat@vcu.edu (804) 828-5256 Smith Bldg. 554B

Research Interests:

The central nervous system (CNS), and drugs with emphasis on novel mechanisms in pain and drug abuse treatment. Our tools are classical (synthesis of neurotransmitter receptor selective ligands) and computational medicinal chemistry (modeling of neurotransmitter receptors, QSAR studies) as well as pharmacology (animal behavioral assays). Main interests stress a2-adrenoceptors, nicotinic cholinergic (nACh) receptors, and serotonin (5-HT) receptors, and the role of their subtype-selective agonists and antagonists in pain and drug addiction therapy.

Selected Publications:

81. Khorana, N; Pullagurla, M. R.; Dukat, M.; Young, R.; Glennon, R. A. Stimulus effects of three sulfur- containing psychoactive agents. Pharmacol. Biochem. Behav. 2004, 78, 821-826.

82. Prisinzano, T.; Dukat, M.; Law, H.; Slassi, A.; MacLean, N. A.; DeLannoy, I.; Glennon, R. A. 2- (Anilino)imidazolines and 2-(benzyl)imidazolines derivatives as h5-HT1D serotonin receptor ligands. Bioorg. Med. Chem. Lett. 2004, 14, 4697-4699.

83. Shelton, K. L.; Dukat, M.; Allan, A. M. Consequences of 5-HT3 receptor over-expression to the discriminative stimulus effects of ethanol. Alcohol. Clin. Exp. Res., 2004, 8, 1161-1171.

84. Wesolowska, A.; Young, S.; Dukat, M.; MD-354 potentiates the antinociceptive effect of clonidine in the mouse tail-flick but not hot-plate assay. Eur. J. Pharmacol. 2004, 495, 129-136.

85. Dukat, M.; Taroua, M.; Dahdouh, A.; Siripurapu, U.; Damaj, I. M.; Martin, B. R.; Glennon, R. A. (±)8-Amino- 5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. Bioorg. Med. Chem. Lett. 2004, 14, 3651- 3654.

86. Lee, M.; Rangisetty, J. B.; Pullagurla, M. R.; Dukat, M.; Setola, V.; Roth, B, L.; Glennon, R. A. 1-(1- Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands. Bioorg. Med. Chem. Lett. 2005, 15, 1707-1711.

87. Kolanos, R.; Siripurapu, U.; Pullagurla, M.; Riaz, M.; Setola, V.; Roth, B. L.; Dukat, M.; Glennon, R. A. Binding of isotryptamines and indenes at h5-HT6 serotonin receptors. Bioorg. Med. Chem. Lett. 2005, 15, 1987-1991.

88. Setola, V.; Dukat, M.; Glennon, R. A.; Roth, B. L. Molecular determinants for the interaction of the valvulopathic anorexigen norfenfluramine with the 5-HT2B receptor. Mol. Pharmacol. 2005, 68, 20-33.

89. Ramunno, A.; Dukat, M.; Lee, M.; Young, R.; El-Zahabi, M.; Damaj, I.; Martin, B.; Glennon, R. A. 6-(2- Phenylethyl)nicotine: A novel nicotinic cholinergic receptor ligand. Bioorg. Med. Chem. Lett. 2005, 15, 3237-3240.

90. Abate, C.; Kolanos, R.; Dukat, M.; Setola, V.; Roth, B. L.; Glennon, R. A. Interaction of chiral MS-245 analogs at h5-HT6 receptors. Bioorg. Med. Chem. Lett. 2005, 15, 3510-3513.

91. Dukat, M.; Ramunno, A.; Banzi, R.; Damaj, M. I.; Martin, B.; Glennon, R. A. 3-(2-Aminoethyl)pyridine analogs as a4b2 nicotinic cholinergic receptor ligands. Bioorg. Med. Chem. Lett. 2005, 15, 4308-4312.

92. Bondareva, T.; Wesolowska, A.; Dukat, M.; Lee, M.; Young, R.; Glennon, R. A. S(+) and R(-)N-methyl-1- (3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) as discriminative stimuli: effect of cocaine. Pharmacol. Biochem. Behav. 2005, 82, 531-538.

93. Pullagurla, M.; Dukat, M.; Roth, B. L.; Setola, V.; Glennon, R. A. 5-Azatryptamine analogs as h5-HT6 receptor ligands. Med. Chem. Res. 2005, 14, 1-18.

94. Pullagurla, M.; Siripurapu, U.; Kolanos, R.; Bondarev, M.; Dukat, M.; Setola, V.; Roth, B. L.; Glennon, R. A. Binding of amine-substituted N1-benzenesulfonylindoles at human 5-HT6 serotonin receptor. Bioorg. Med. Chem. Lett. 2005, 15, 5298-5302.

95. Dukat, M.; Wesolowska, A. Antinociception: Mechanistic studies on the action of MD-354 and clonidine. Part 1. The 5-HT3 component. Eur. J. Pharmacol. 2005, 528, 59-64.

96. Young, R.; Rothamn, R.; Rangisetty, J. B.; Dukat, M.; Glennon, R. A. TDIQ (5,6,7,8-tetrahydro-1,3- dioxolo[4,5-g]isoquinoline) inhibits the consumption of between-meals “snaks” in mice. Pharmacol. Biochem. Behav. 2006, 84, 74-83.

97. Siripurapu, U.; Kolanos, R.; Dukat, M.; Roth, B.L.; Glennon, R.A, Binding of methoxy-substituted N1- benzenesulfonylindole analogs at human 5-HT6 serotonin receptors. Bioorg. Med. Chem. Lett. 2006, 16, 3793-3796.

98. Ragab, H.M.; Kim, J.S.; Dukat, M.; Navarro, H.; Glennon, R.A. Aryloxyethylamines: Binding at a7 nicotinic acetylcholine receptors. Bioorg. Med. Chem. Lett. 2006,16, 4283-4286.

99. Sikazwe, D.M.N.; Bondarev, M.L.; Dukat, M.; Rangisetty, J.B.; Roth, B.L.; Glennon, R.A. Binding of Sulfonyl-Containing Arylalkylamines at Human 5-HT6 Serotonin receptors. J. Med. Chem. 2006, 49, 5217- 5225.

100. Kolanos, R.; Dukat, M.; Roth, B.L.; Glennon, R.A. Interaction of N1-unsubstituted and N1- benzenesulfonyltryptamines at h5-HT6 receptors. Bioorg. Med. Chem. Lett. 2006, 16, 5832-5835.