Search Results - "Wasicak, James"

Novel 3-Pyridyl Ethers with Subnanomolar Affinity for Central Neuronal Nicotinic Acetylcholine Receptors by Abreo, Melwyn A, Lin, Nan-Horng, Garvey, David S, Gunn, David E, Hettinger, Ann-Marie, Wasicak, James T, Pavlik, Patricia A, Martin, Yvonne C, Donnelly-Roberts, Diana L, Anderson, David J, Sullivan, James P, Williams, Michael, Arneric, Stephen P, Holladay, Mark W

“…Recent evidence indicating the therapeutic potential of cholinergic channel modulators for the treatment of central nervous system (CNS) disorders as well as…”
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Identification and Initial Structure−Activity Relationships of (R)-5-(2-Azetidinylmethoxy)-2-chloropyridine (ABT-594), a Potent, Orally Active, Non-Opiate Analgesic Agent Acting via Neuronal Nicotinic Acetylcholine Receptors by Holladay, Mark W, Wasicak, James T, Lin, Nan-Horng, He, Yun, Ryther, Keith B, Bannon, Anthony W, Buckley, Michael J, Kim, David J. B, Decker, Michael W, Anderson, David J, Campbell, Jeffrey E, Kuntzweiler, Theresa A, Donnelly-Roberts, Diana L, Piattoni-Kaplan, Marietta, Briggs, Clark A, Williams, Michael, Arneric, Stephen P

“…New members of a previously reported series of 3-pyridyl ether compounds are disclosed as novel, potent analgesic agents acting through neuronal nicotinic…”
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Antinociceptive effects of the novel neuronal nicotinic acetylcholine receptor agonist, ABT-594, in mice by Decker, Michael W, Bannon, Anthony W, Buckley, Michael J, Kim, David J.B, Holladay, Mark W, Ryther, Keith B, Lin, Nan-Horng, Wasicak, James T, Williams, Michael, Arneric, Stephen P

“…ABT-594 [5-((2 R)-azetidinylmethoxy)-2-chloropyridine], a novel neuronal nicotinic acetylcholine receptor agonist, produced significant antinociceptive effects…”
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Novel Isoxazoles which Interact with Brain Cholinergic Channel Receptors Have Intrinsic Cognitive Enhancing and Anxiolytic Activities by Garvey, David S, Wasicak, James T, Decker, Michael W, Brioni, Jorge D, Buckley, Michael J, Sullivan, James P, Carrera, George M, Holladay, Mark W, Arneric, Stephen P, Williams, Michael

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Ligands for Brain Cholinergic Channel Receptors: Synthesis and in Vitro Characterization of Novel Isoxazoles and Isothiazoles as Bioisosteric Replacements for the Pyridine Ring in Nicotine by Garvey, David S, Wasicak, James T, Elliott, Richard L, Lebold, Suzanne, Hettinger, Ann-Marie, Carrera, George M, Lin, Nan-Horng, He, Yun, Holladay, Mark W

“…Ligands which activate neuronal nicotinic acetylcholine receptors (nAChRs) represent a potential approach for the palliative treatment for the symptoms of…”
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A-85380 [3-(2( S)-azetidinylmethoxy) pyridine]: In Vitro pharmacological properties of a novel, high affinity α4β2 nicotinic acetylcholine receptor ligand by Sullivan, James P., Donnelly-Roberts, Diana, Briggs, Clark A., Anderson, David J., Gopalakrishnan, Murali, Piattoni-Kaplan, Marietta, Campbell, Jeffrey E., McKenna, David G., Molinari, Edwardo, Hettinger, Ann-Marie, Garvey, David S., Wasicak, James T., Holladay, Mark W., Williams, Michael, Arneric, Stephen P.

“…The in vitro pharmacological properties of a novel cholinergic channel ligand, A-85380 [3-(2( S)-azetidinylmethoxy) pyridine], were examined using tissue…”
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Conformationally constrained amino acids. Synthesis and optical resolution of 3-substituted proline derivatives by Chung, John Y. L, Wasicak, James T, Arnold, William A, May, Catherine S, Nadzan, Alex M, Holladay, Mark W

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Alkylation of tricarbonyl(diene)iron complexes: Model studies for the preparation of protomycinolide IV by Wasicak, James T., Craig, Richard A., Henry, Rodger, Dasgupta, Bireshwar, Li, Huameng, Donaldson, William A.

“…The alkylation of (4,6-heptadien-3-one)- and (methyl 3,5-hexadienoate)Fe(CO)3 (1 and 2) were examined (0–42% de and 69–92% de respectively). Optically active…”
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Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors by Garvey, David S, Wasicak, James T, Chung, John Y. L, Shue, Youe Kong, Carrera, George M, May, Paul D, McKinney, Michael M, Anderson, David, Cadman, Evelyn

“…A series of novel 2-substituted acetylenic pyrrolidines and piperidines related to oxotremorine (1) were prepared and evaluated in vitro as muscarinic…”
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ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective analgesic acting via neuronal nicotinic acetylcholine receptors: I. In vitro characterization by Donnelly-Roberts, D L, Puttfarcken, P S, Kuntzweiler, T A, Briggs, C A, Anderson, D J, Campbell, J E, Piattoni-Kaplan, M, McKenna, D G, Wasicak, J T, Holladay, M W, Williams, M, Arneric, S P

“…The discovery of (+/-)-epibatidine, a naturally occurring neuronal nicotinic acetylcholine receptor (nAChR) agonist with antinociceptive activity 200-fold more…”
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ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors: II. In vivo characterization by Bannon, A W, Decker, M W, Curzon, P, Buckley, M J, Kim, D J, Radek, R J, Lynch, J K, Wasicak, J T, Lin, N H, Arnold, W H, Holladay, M W, Williams, M, Arneric, S P

“…The antinociceptive effects of ABT-594, a novel nicotinic acetylcholine receptor (nAChR) ligand, were examined in rats in models of acute thermal (hot box) and…”
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Pyrrolidine-3-carboxylic Acids as Endothelin Antagonists. 3. Discovery of a Potent, 2-Nonaryl, Highly Selective ET A Antagonist (A-216546) by Liu, Gang, Henry, Kenneth J., Szczepankiewicz, Bruce G., Winn, Martin, Kozmina, Natasha S., Boyd, Steven A., Wasicak, James, von Geldern, Thomas W., Wu-Wong, Jinshyun R., Chiou, William J., Dixon, Douglas B., Nguyen, Bach, Marsh, Kennan C., Opgenorth, Terry J.

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Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: Effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice by Holladay, Mark W., Bai, Hao, Li, Yihong, Lin, Nan-Horng, Daanen, Jerome F., Ryther, Keith B., Wasicak, James T., Kincaid, John F., He, Yun, Hettinger, Anne-Marie, Huang, Peggy, Anderson, David J., Bannon, Anthony W., Buckley, Michael J., Campbell, Jeffrey E., Donnelly-Roberts, Diana L., Gunther, Karen L., Kim, David J.B., Kuntzweiler, Theresa A., Sullivan, James P., Decker, Michael W., Arneric, Stephen P.

“…Analogs of A-98593 ( 1) and its enantiomer ABT-594 ( 2) with diverse substituents on the pyridine ring were prepared and tested for affinity to nicotinic…”
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Discovery of a Series of Cyclohexylethylamine-Containing Protein Farnesyltransferase Inhibitors Exhibiting Potent Cellular Activity by Henry, Kenneth J, Wasicak, James, Tasker, Andrew S, Cohen, Jerome, Ewing, Patricia, Mitten, Michael, Larsen, John J, Kalvin, Douglas M, Swenson, Rolf, Ng, Shi-Chung, Saeed, Badr, Cherian, Sajeev, Sham, Hing, Rosenberg, Saul H

“…Synthesis of a library of secondary benzylic amines based on the Sebti−Hamilton type peptidomimetic farnesyltransferase (FTase) inhibitor FTI-276 (1) led to…”
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Structural aspects of high affinity ligands for the α4β2 neuronal nicotinic receptor by Dart, Michael J., Wasicak, James T., Ryther, Keith B., Schrimpf, Michael R., Kim, Ki H., Anderson, David J., Sullivan, James P., Meyer, Michael D.

“…Neuronal nicotinic acetylcholine receptors (nAChRs) are a heterogeneous family of related ion channels that are widely distributed throughout the central and…”
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Studies on the preparation of protomycinolide IV: Enantioselective synthesis of the C3–C9 segment by Wasicak, James T., Donaldson, William A.

“…The C3–C9 segment, (−)- 16, of the polyene macrolide antibiotic protomycinolide IV ( 1a) was prepared in optically pure form from commercially available methyl…”
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Structure-activity studies on a novel series of cholinergic channel activators based on a heteroaryl ether framework by Lin, Nan-Horng, Abreo, Melwyn A., Gunn, David E., Lebold, Suzanne A., Lee, Edmund L., Wasicak, James T., Hettinger, Ann-Marie, Daanen, Jerome F., Garvey, David S., Campbell, Jeffrey E., Sullivan, James P., Williams, Michael, Arneric, Stephen P.

“…Analogs of compound 1 with a variety of azacycles and heteroaryl groups were synthesized. These analogs exhibited K i values ranging from 0.15 to > 10,000 nM…”
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Pyrrolidine-3-carboxylic Acids as Endothelin Antagonists. 3. Discovery of a Potent, 2-Nonaryl, Highly Selective ETA Antagonist (A-216546) by Liu, Gang, Henry, Kenneth J, Szczepankiewicz, Bruce G, Winn, Martin, Kozmina, Natasha S, Boyd, Steven A, Wasicak, James, von Geldern, Thomas W, Wu-Wong, Jinshyun R, Chiou, William J, Dixon, Douglas B, Nguyen, Bach, Marsh, Kennan C, Opgenorth, Terry J

“…Previously we have reported the discovery of ABT-627 (1, A-147627, active enantiomer of A-127722), a 2,4-diaryl substituted pyrrolidine-3-carboxylic acid based…”
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