Search Results - "Lovell, Kimberly M."

Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics by Schmid, Cullen L., Kennedy, Nicole M., Ross, Nicolette C., Lovell, Kimberly M., Yue, Zhizhou, Morgenweck, Jenny, Cameron, Michael D., Bannister, Thomas D., Bohn, Laura M.

“…Biased agonism has been proposed as a means to separate desirable and adverse drug responses downstream of G protein-coupled receptor (GPCR) targets. Herein,…”
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Development of Functionally Selective, Small Molecule Agonists at Kappa Opioid Receptors by Zhou, Lei, Lovell, Kimberly M., Frankowski, Kevin J., Slauson, Stephen R., Phillips, Angela M., Streicher, John M., Stahl, Edward, Schmid, Cullen L., Hodder, Peter, Madoux, Franck, Cameron, Michael D., Prisinzano, Thomas E., Aubé, Jeffrey, Bohn, Laura M.

“…The kappa opioid receptor (KOR) is widely expressed in the CNS and can serve as a means to modulate pain perception, stress responses, and affective reward…”
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Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier potassium channels by Raphemot, Rene, Rouhier, Matthew F, Swale, Daniel R, Days, Emily, Weaver, C David, Lovell, Kimberly M, Konkel, Leah C, Engers, Darren W, Bollinger, Sean R, Bollinger, Sean F, Hopkins, Corey, Piermarini, Peter M, Denton, Jerod S

“…Vector-borne diseases such as dengue fever and malaria, which are transmitted by infected female mosquitoes, affect nearly half of the world's population. The…”
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Eliciting renal failure in mosquitoes with a small-molecule inhibitor of inward-rectifying potassium channels by Raphemot, Rene, Rouhier, Matthew F, Hopkins, Corey R, Gogliotti, Rocco D, Lovell, Kimberly M, Hine, Rebecca M, Ghosalkar, Dhairyasheel, Longo, Anthony, Beyenbach, Klaus W, Denton, Jerod S, Piermarini, Peter M

“…Mosquito-borne diseases such as malaria and dengue fever take a large toll on global health. The primary chemical agents used for controlling mosquitoes are…”
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Fragment-based screening by X-ray crystallography, MS and isothermal titration calorimetry to identify PNMT (phenylethanolamine N-methyltransferase) inhibitors by Drinkwater, Nyssa, Vu, Hoan, Lovell, Kimberly M, Criscione, Kevin R, Collins, Brett M, Prisinzano, Thomas E, Poulsen, Sally-Ann, McLeish, Michael J, Grunewald, Gary L, Martin, Jennifer L

“…CNS (central nervous system) adrenaline (epinephrine) is implicated in a wide range of physiological and pathological conditions. PNMT (phenylethanolamine…”
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Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias by Kennedy, Nicole M, Schmid, Cullen L, Ross, Nicolette C, Lovell, Kimberly M, Yue, Zhizhou, Chen, Yen Ting, Cameron, Michael D, Bohn, Laura M, Bannister, Thomas D

“…While mu opioid receptor (MOR) agonists are especially effective as broad-spectrum pain relievers, it has been exceptionally difficult to achieve a clear…”
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Trimethylsilyl Trifluoromethanesulfonate (TMSOTf) Assisted Facile Deprotection of N,O-Acetonides by Poon, Kevin W. C, Lovell, Kimberly M, Dresner, Kendra N, Datta, Apurba

“…Employing TMSOTf as an easily available reagent, we have developed a mild and efficient method for the deprotection of both terminal and internal N,O-acetonide…”
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Synthetic studies of neoclerodane diterpenes from Salvia divinorum: role of the furan in affinity for opioid receptors by Simpson, Denise S, Lovell, Kimberly M, Lozama, Anthony, Han, Nina, Day, Victor W, Dersch, Christina M, Rothman, Richard B, Prisinzano, Thomas E

“…Further synthetic modification of the furan ring of salvinorin A (1), the major active component of Salvia divinorum, has resulted in novel neoclerodane…”
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Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting by Zhou, Lei, Stahl, Edward L., Lovell, Kimberly M., Frankowski, Kevin J., Prisinzano, Thomas E., Aubé, Jeffrey, Bohn, Laura M.

“…Differential modulation of kappa opioid receptor (KOR) signaling has been a proposed strategy for developing therapies for drug addiction and depression by…”
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Advances in Sulfonamide Kappa Opioid Receptor Antagonists: Structural Refinement and Evaluation of CNS Clearance by Ma, Huiyong, Brust, Tarsis, Frankowski, Kevin J, Lovell, Kimberly M, Cameron, Michael D, Bohn, Laura M, Aubé, Jeffrey

“…Focused modification of a sulfonamide-based kappa opioid receptor (KOR) antagonist series previously reported by this laboratory was investigated. A total of…”
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Synthesis of Kappa Opioid Antagonists Based On Pyrrolo[1,2-α]quinoxalinones Using an N‑Arylation/Condensation/Oxidation Reaction Sequence by Scarry, Sarah M, Lovell, Kimberly M, Frankowski, Kevin J, Bohn, Laura M, Aubé, Jeffrey

“…The quinoxaline and quinoxalinone family of nitrogen heterocycles is present in molecules of therapeutic relevance for diverse applications ranging from…”
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Structure–activity relationship investigation of triazole-based kappa opioid receptor agonists by Frankowski, Kevin J., Brust, Tarsis, Lovell, Kimberly M., Yoo, Euna, Bohn, Laura M., Aubé, Jeffrey

“…Select triazole-based small molecules possess potent and selective kappa opioid receptor (KOR) agonism. Here, we designed twenty new analogs to investigate the…”
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Structure–Activity Relationship Studies of Functionally Selective Kappa Opioid Receptor Agonists that Modulate ERK 1/2 Phosphorylation While Preserving G Protein Over βArrestin2 Signaling Bias by Lovell, Kimberly M, Frankowski, Kevin J, Stahl, Edward L, Slauson, Stephen R, Yoo, Euna, Prisinzano, Thomas E, Aubé, Jeffrey, Bohn, Laura M

“…Kappa opioid receptor (KOR) modulation is a promising target for drug discovery efforts due to KOR involvement in pain, depression, and addiction behaviors. We…”
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Behavioral effects and central nervous system levels of the broadly available κ-agonist hallucinogen salvinorin A are affected by P-glycoprotein modulation in vivo by Butelman, Eduardo R, Caspers, Michael, Lovell, Kimberly M, Kreek, Mary Jeanne, Prisinzano, Thomas E

“…Active blood-brain barrier mechanisms, such as the major efflux transporter P-glycoprotein (mdr1), modulate the in vivo/central nervous system (CNS) effects of…”
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Semisynthetic neoclerodanes as kappa opioid receptor probes by Lovell, Kimberly M., Vasiljevik, Tamara, Araya, Juan J., Lozama, Anthony, Prevatt-Smith, Katherine M., Day, Victor W., Dersch, Christina M., Rothman, Richard B., Butelman, Eduardo R., Kreek, Mary Jeanne, Prisinzano, Thomas E.

“…Modification of the furan ring of salvinorin A (1), the main active component of Salvia divinorum, has resulted in novel neoclerodane diterpenes with opioid…”
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Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif by Frankowski, Kevin J., Slauson, Stephen R., Lovell, Kimberly M., Phillips, Angela M., Streicher, John M., Zhou, Lei, Whipple, David A., Schoenen, Frank J., Prisinzano, Thomas E., Bohn, Laura M., Aubé, Jeffrey

“…[Display omitted] Optimization of the sulfonamide-based kappa opioid receptor (KOR) antagonist probe molecule ML140 through constraint of the sulfonamide…”
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N-Acyl-N′-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats by Lovell, Kimberly M., Felts, Andrew S., Rodriguez, Alice L., Venable, Daryl F., Cho, Hyekyung P., Morrison, Ryan D., Byers, Frank W., Daniels, J. Scott, Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W., Emmitte, Kyle A.

“…Development of SAR in an N-acyl-N′-arylpiperazine series of negative allosteric modulators of mGlu1 using a functional cell-based assay is described in this…”
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Correction to “Structure–Activity Relationship Studies of Functionally Selective Kappa Opioid Receptor Agonists that Modulate ERK 1/2 Phosphorylation While Preserving G Protein Over βArrestin2 Signaling Bias” by Lovell, Kimberly M, Frankowski, Kevin J, Stahl, Edward L, Slauson, Stephen R, Yoo, Euna, Prisinzano, Thomas E, Aubé, Jeffrey, Bohn, Laura M

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Further exploration of M1 allosteric agonists: Subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism by Sheffler, Douglas J., Sevel, Christian, Le, Uyen, Lovell, Kimberly M., Tarr, James C., Carrington, Sheridan J.S., Cho, Hyekyung P., Digby, Gregory J., Niswender, Colleen M., Conn, P. Jeffrey, Hopkins, Corey R., Wood, Michael R., Lindsley, Craig W.

“…This letter describes the further exploration of two series of M1 allosteric agonists, TBPB and VU0357017, previously reported from our lab. Within the TPBP…”
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Synthesis of neoclerodane diterpenes and their pharmacological effects by Lovell, Kimberly M, Prevatt-Smith, Katherine M, Lozama, Anthony, Prisinzano, Thomas E

“…Salvinorin A is a neoclerodane diterpene that has been shown to be an agonist at kappa opioid receptors. Its unique structure makes it an attractive target for…”
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