Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Karla Kopec"'
Publikováno v:
Chemical Biology & Drug Design. 83:666-669
A series of non-sulfonamide/non-sulfone derived potent 5-HT6 receptor inverse agonists has been disclosed. Representative compound 9 (Ki = 14 nm) displayed selectivity against a set of family members as well as brain permeability 6 h post-oral admini
Publikováno v:
Chemical Biology & Drug Design. 83:149-153
A series of potent 5-hydroxytryptamine 6 (5-HT₆) receptor antagonists based on 1-thia-4,7-diaza-spiro[4.4]nonane-3,6-dione motif has been disclosed. Enantiomers of potent racemate compound 8a (K(i) = 26 nM) displayed difference in activity (K(i) of
Autor:
Thomas J. Connors, Jie Qian, Zeck Huang, Joanne R. Mathiasen, Edward R. Bacon, Thelma S. Angeles, Mark J. Huffman, Emir Duzic, Joseph M. Salvino, Beth Ann McKenna, Hervé Schaffhauser, Robert J. McHugh, Lily D. Lu, George C. Morton, Beverly P. Holskin, Karla Kopec, Amy DiCamillo, Gerard C. Rosse, Chrysanthe Spais, Rabindranath Tripathy, Lisa D. Aimone
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1421-1426
Serotoninergic neurotransmission has been implicated in modulation of learning and memory. It has been demonstrated that 5-hydroxytryptamine(6) (5-HT(6)) receptor antagonists show beneficial effect on cognition in several animal models. Based on a ph
Autor:
Beverly P. Holskin, Karla Kopec, Joanne R. Mathiasen, Amy DiCamillo, Babu G. Sundar, Thomas J. Connors, Emir Duzic, Edward R. Bacon, Gerard C. Rosse, Chrysanthe Spais, Thomas R. Bailey, Beth Ann McKenna, Rebecca A. Brown, Jie Qian, Derek Dunn, Mark J. Huffman, Joseph M. Salvino, Huang Zeqi, Lisa D. Aimone, Hervé Schaffhauser, Deborah Galinis, Thelma S. Angeles, Lily D. Lu, George C. Morton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:120-123
7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel scaffold for 5HT(6) receptor antagonists. Optimization by substitution at C-1 position led to identification of selective, orally bioavailable, brain penetrant antagonists with
Publikováno v:
Biochemical Pharmacology. 69:1133-1139
Proteomics, the study of cellular protein expression, is an evolving technology platform that has the potential to identify novel proteins involved in key biological processes in the cell that may serve as potential drug targets. While proteomics has
Autor:
Rabindranath, Tripathy, Robert J, McHugh, Edward R, Bacon, Joseph M, Salvino, George C, Morton, Lisa D, Aimone, Zeck, Huang, Joanne R, Mathiasen, Amy, DiCamillo, Mark J, Huffman, Beth A, McKenna, Karla, Kopec, Lily D, Lu, Jie, Qian, Thelma S, Angeles, Thomas, Connors, Chrysanthe, Spais, Beverly, Holskin, Emir, Duzic, Hervé, Schaffhauser, Gerard C, Rossé
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(3)
Serotoninergic neurotransmission has been implicated in modulation of learning and memory. It has been demonstrated that 5-hydroxytryptamine(6) (5-HT(6)) receptor antagonists show beneficial effect on cognition in several animal models. Based on a ph
Autor:
Babu G, Sundar, Thomas R, Bailey, Derek D, Dunn, Edward R, Bacon, Joseph M, Salvino, George C, Morton, Lisa D, Aimone, Huang, Zeqi, Joanne R, Mathiasen, Amy, Dicamillo, Mark J, Huffman, Beth A, McKenna, Karla, Kopec, Lily D, Lu, Rebecca, Brown, Jie, Qian, Thelma, Angeles, Thomas, Connors, Chrysanthe, Spais, Beverly, Holskin, Deborah, Galinis, Emir, Duzic, Herve, Schaffhauser, Gerard C, Rosse
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(1)
7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel scaffold for 5HT(6) receptor antagonists. Optimization by substitution at C-1 position led to identification of selective, orally bioavailable, brain penetrant antagonists with
Publikováno v:
Current Protocols in Pharmacology
This unit describes a convenient functional uptake assay for GABA transport into cell lines transiently transfected with GABA transporter-1 (GAT-1) and other GAT isoforms. This facile, homogeneous assay allows for the determination of Km, Vmax, and K
Comparison of organophosphorous acid anhydrolases from different species using monoclonal antibodies
Autor:
Karla Kopec-Smyth, Jennifer L. Poppino, Susan L. Futrovsky, Jeffrey R. Deschamps, Keith B. Ward
Publikováno v:
Comparative Biochemistry and Physiology Part C: Pharmacology, Toxicology and Endocrinology. 106:765-768
1. Monoclonal antibodies were raised against squid hepatopancreas organophosphorous acid (OPA) anhydrolase (EC 3.1.8.2) and were used to study structural similarities with OPA anhydrolases isolated from different sources. 2. Common epitopes were iden
Publikováno v:
Brain research. 1374
Alternative promoter usage and mRNA precursor splicing produce three amino-terminal isoforms of the human glycine transporter type 1 (GlyT1). To enable discovery of pharmacological tools that might distinguish them, each of these isoforms was stably