Zobrazeno 1 - 10
of 59
pro vyhledávání: '"Boyd L, Harrison"'
Autor:
Matthew D. Hill, Maria-Jesus Blanco, Francesco G. Salituro, Zhu Bai, Jacob T. Beckley, Michael A. Ackley, Jing Dai, James J. Doherty, Boyd L. Harrison, Ethan C. Hoffmann, Tatiana M. Kazdoba, David Lanzetta, Michael Lewis, Michael C. Quirk, Albert J. Robichaud
Publikováno v:
Journal of Medicinal Chemistry. 65:9063-9075
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::55c17424c1aec1450e3aa6abf75d1774
https://doi.org/10.1021/acs.jmedchem.2c00313
https://doi.org/10.1021/acs.jmedchem.2c00313
Autor:
James J. Doherty, Michael A. Ackley, Ethan Hoffmann, Tatiana M. Kazdoba, Zhu Bai, Boyd L. Harrison, Albert J. Robichaud, Andrew Griffin, Mike Lewis, Gabriel Martinez Botella, Francesco G. Salituro, Daniel S. La, Jing Dai, Michael Quirk
Publikováno v:
Journal of Medicinal Chemistry. 62:7526-7542
Neuroactive steroids (NASs) play a pivotal role in maintaining homeostasis is the CNS. We have discovered that one NAS in particular, 24(S)-hydroxycholesterol (24(S)-HC), is a positive allosteric modulator (PAM) of NMDA receptors. Using 24(S)-HC as a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d85c93f6e01f9e02e46c0fd48ba0202c
https://doi.org/10.1021/acs.jmedchem.9b00591
https://doi.org/10.1021/acs.jmedchem.9b00591
Autor:
Francesco G. Salituro, Caitlin A. Newman, Maria-Jesus Blanco, Boyd L. Harrison, Quinn Coughlin, Daniel La, Andrew Griffin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:61-70
Endogenous and synthetic neuroactive steroids (NASs) or neurosteroids are effective modulators of multiple signaling pathways including receptors for the γ-aminobutyric acid A (GABAA) and glutamate, in particular N-methyl-d-aspartate (NMDA). These r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8d135b8adc8e1a60374c554f57b2196
https://doi.org/10.1016/j.bmcl.2017.11.043
https://doi.org/10.1016/j.bmcl.2017.11.043
Autor:
Daniel S, La, Francesco G, Salituro, Gabriel, Martinez Botella, Andrew M, Griffin, Zhu, Bai, Michael A, Ackley, Jing, Dai, James J, Doherty, Boyd L, Harrison, Ethan C, Hoffmann, Tatiana M, Kazdoba, Michael C, Lewis, Michael C, Quirk, Albert J, Robichaud
Publikováno v:
Journal of medicinal chemistry. 62(16)
Neuroactive steroids (NASs) play a pivotal role in maintaining homeostasis is the CNS. We have discovered that one NAS in particular, 24(
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::8edd1a5945ab2bc16424985f2d7c6fb6
https://pubmed.ncbi.nlm.nih.gov/31390523
https://pubmed.ncbi.nlm.nih.gov/31390523
Autor:
Zhu Bai, Scott J. Grossman, Jiamiao Wang, Richard Thomas Beresis, Ethan Hoffmann, Gabriel Martinez Botella, Carlos M. Loya, Kaisheng Shen, Francesco G. Salituro, Albert J. Robichaud, Boyd L. Harrison, Michael A. Ackley, Shiling Jia, Gabriel M. Belfort, James J. Doherty
Publikováno v:
Journal of Medicinal Chemistry. 58:3500-3511
Neuroactive steroids (NASs) have been shown to impact central nervous system (CNS) function through positive allosteric modulation of the GABA(A) receptor (GABA(A)-R). Herein we report the effects on the activity and pharmacokinetic properties of a s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::526fcbe06be37d20a154344dc5f6e61e
https://doi.org/10.1021/acs.jmedchem.5b00032
https://doi.org/10.1021/acs.jmedchem.5b00032
Autor:
Ethan Hoffmann, Carlos M. Loya, Albert J. Robichaud, Boyd L. Harrison, Richard Thomas Beresis, Jing Dai, Gabriel M. Belfort, Alison L. Althaus, Michael A. Ackley, James J. Doherty, Maria-Jesus Blanco, Zhu Bai, Scott J. Grossman, Francesco G. Salituro, Gabriel Martinez Botella
Publikováno v:
Journal of medicinal chemistry. 60(18)
Certain classes of neuroactive steroids (NASs) are positive allosteric modulators (PAM) of synaptic and extrasynaptic GABAA receptors. Herein, we report new SAR insights in a series of 5β-nor-19-pregnan-20-one analogues bearing substituted pyrazoles
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92adadab7380c7344ed988b15618ea47
https://pubmed.ncbi.nlm.nih.gov/28753313
https://pubmed.ncbi.nlm.nih.gov/28753313
Autor:
Albert J. Robichaud, Norbert Hoefgen, Karen L. Marquis, Steven M. Grauer, Hans Stange, Radka Graf, Ute Egerland, Thorsten Hage, Christian Grunwald, Julie A. Brennan, Michael S. Malamas, Boyd L. Harrison, Menelas N. Pangalos, Kevin Parris, Thomas Kronbach, Yike Ni, Kristi Fan, Rudolf Schindler, Rachel Navarra, Hans-Joachim Lankau, Nicholas J. Brandon, James Joseph Erdei, Barbara Langen
Publikováno v:
Journal of Medicinal Chemistry. 54:7621-7638
The identification of highly potent and orally active phenylpyrazines for the inhibition of PDE10A is reported. The new analogues exhibit subnanomolar potency for PDE10A, demonstrate high selectivity against all other members of the PDE family, and s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c3f324255336d82f4fabd618b4bcef3
https://doi.org/10.1021/jm2009138
https://doi.org/10.1021/jm2009138
Autor:
Shen Z, Tom A. Comery, David Smith, Brian J. Platt, Terrance H. Andree, Zhang Minsheng, Magid Abou-Gharbia, Sukoff-Rizzo Sj, Havran Lm, Chong Dc, Natasha Kagan, Zoë A. Hughes, Kelly Sullivan, Bach Ac rd, Boyd L. Harrison, Wayne E. Childers, Magda Asselin, Sharon Rosenzweig-Lipson, Claudine Pulicicchio, Steven M. Grauer, Marathias, George Theodore Grosu, Mark Day, Bicksler Jj, Chad E. Beyer, Adedayo Adedoyin, Christine Huselton, Sabb Al, Suzan Aschmies, Ronald L. Magolda, Warren D. Hirst, Kleintop T, Albert J. Robichaud
Publikováno v:
Journal of Medicinal Chemistry. 53:4066-4084
As part of an effort to identify 5-HT(1A) antagonists that did not possess typical arylalkylamine or keto/amido-alkyl aryl piperazine scaffolds, prototype compound 10a was identified from earlier work in a combined 5-HT(1A) antagonist/SSRI program. T
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8128f3b71923ae4c75a96a7c24e6d62e
https://doi.org/10.1021/jm1000908
https://doi.org/10.1021/jm1000908
Autor:
Thorsten Hage, Nicholas J. Brandon, Norbert Höfgen, Hans-Joachim Lankau, Menelas N. Pangalos, Christian Grunwald, Karen L. Marquis, Michael S. Malamas, Rudolf Schindler, Thomas Kronbach, Hans Stange, Peter Tremmel, Barbara Langen, Ute Egerland, Boyd L. Harrison
Publikováno v:
Journal of Medicinal Chemistry. 53:4399-4411
Novel imidazo[1,5-a]pyrido[3,2-e]pyrazines have been synthesized and characterized as both potent and selective phosphodiesterase 10A (PDE10A) inhibitors. For in vitro characterization, inhibition of PDE10A mediated cAMP hydrolysis was used and a QSA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::313deec27a347216a6685b7564af2754
https://doi.org/10.1021/jm1002793
https://doi.org/10.1021/jm1002793
Autor:
Ping Chen, Rajesh A. Shenoy, Albert J. Robichaud, Deborah F. Smith, Schuyler Adam Antane, Boyd L. Harrison, Van-Duc Le, Ronald C. Bernotas, Guo Ming Zhang, Lee E. Schechter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1657-1660
Novel 3-(arylsulfonyl)-1-(azacyclyl)-1H-indoles 6 were synthesized as potential 5-HT(6) receptor ligands, based on constraining a basic side chain as either a piperidine or a pyrrolidine. Many of these compounds had good 5-HT(6) binding affinity with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bbd37cbf938ab1c1710fbc022465ce6
https://doi.org/10.1016/j.bmcl.2010.01.073
https://doi.org/10.1016/j.bmcl.2010.01.073