Výsledky vyhledávání - "Kevin A. Serpa"

Discovery of a novel Kv7 channel opener as a treatment for epilepsy

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:4941-4944

Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures. In an effort to identify a compound with suc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47d5703f96a7e503af07e95a710ca422
https://doi.org/10.1016/j.bmcl.2015.04.074

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Discovery of PF-00217830: Aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder

Autor: Joseph T. Repine, Lorraine Kathleen Fay, Favor David, Hyacinth Akunne, Kim Nicholls, Bradley Snyder, Liming Zhang, Kevin A. Serpa, Douglas S. Johnson, Lawrence W. Fitzgerald, Andrew D. White, Chung Choi, Steven Z. Whetzel

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:2621-2625

The synthesis and structure-activity relationship (SAR) of a novel series of aryl piperazine napthyridinone D(2) partial agonists is described. Our goal was to optimize the affinities for the D(2), 5-HT(2A) and 5-HT(1A) receptors, such that the D(2)/

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a73015fc859258fce499a6bc0925b0a
https://doi.org/10.1016/j.bmcl.2011.01.059

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Activity profile of pregabalin in rodent models of epilepsy and ataxia

Autor: Louis L. Radulovic, Mark G. Vartanian, Jack J. Kinsora, Edward H. Bertram, Charles Taylor, Kevin A. Serpa, M. Vergnes

Publikováno v: Epilepsy Research. 68:189-205

Pregabalin (Lyrica) is a novel amino acid compound that binds with high affinity to the alpha2-delta (alpha2-delta) auxiliary protein of voltage-gated calcium channels. In vivo, it potently prevents seizures, pain-related behaviors and has anxiolytic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::296da83529c9c68836624a40449cd41e
https://doi.org/10.1016/j.eplepsyres.2005.11.001

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Synthesis and Pharmacology of Benzoxazines as Highly Selective Antagonists at M4 Muscarinic Receptors

Autor: T. A. Pugsley, Hussein Hallak, Thomas M. Böhme, Kevin A. Serpa, Corinne E. Augelli-Szafran, Roy D. Schwarz

Publikováno v: Journal of Medicinal Chemistry. 45:3094-3102

Previously, we reported on PD 102807 (41) as being the most selective synthetic M(4) muscarinic antagonist identified to date. Synthesized analogues of 41 showed no improvement in affinity and selectivity at that time. However, several newly synthesi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2202c0c2db7a4f272d0165ed3a30b53
https://doi.org/10.1021/jm011116o

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Subtype-Selective N-Methyl-d-aspartate Receptor Antagonists: Benzimidazalone and Hydantoin as Phenol Replacements

Autor: Lawrence D. Wise, Po-Wai Yuen, Leonard T. Meltzer, Schelkun Robert Michael, Edward R. Whittemore, Kevin A. Serpa, Richard M. Woodward

Publikováno v: Journal of Medicinal Chemistry. 43:1892-1897

Previous work in our laboratories investigating compounds with structural similarity to ifenprodil (5) and 6 (CP101,606) resulted in compound 7 as a potent and selective antagonist of the NR1/2B subtype of the NMDA receptors. Replacement of the pheno

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e35cc8fe32ce57e06aa96dcbad34f80a
https://doi.org/10.1021/jm990537r

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Metabotropic glutamate receptor-mediated inhibition and excitation of substantia nigra dopamine neurons

Autor: Kevin A. Serpa, Leonard T. Meltzer, C L Christoffersen

Publikováno v: Synapse. 26:184-193

Microiontophoretic drug application and extracellular recording techniques were used to evaluate the effects of the selective metabotropic glutamate receptor (mGluR) agonist (1S,3R)-1-aminocyclopentane-1,3-dicarboxylate (1S,3R-ACPD) on dopamine (DA)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e88eb47864a746867e7aceb9a1e4da51
https://doi.org/10.1002/(sici)1098-2396(199706)26:2<184::aid-syn9>3.0.co

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Modulation of dopamine neuronal activity by glutamate receptor subtypes

Autor: Kevin A. Serpa, C L Christoffersen, Leonard T. Meltzer

Publikováno v: Neuroscience & Biobehavioral Reviews. 21:511-518

In vitro and in vivo electrophysiological studies have been used to assess the effects of glutamate, as well as specific agonists and antagonists for ionotropic, N-methyl-D-aspartate (NMDA), (R,S)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81921b1a6ebd301ac7ccc69f38ed311e
https://doi.org/10.1016/s0149-7634(96)00030-9

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6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics

Autor: Lawrence W. Fitzgerald, Favor David, Vincent E. Groppi, Andrew D. White, James J. Powers, Kevin A. Serpa

Publikováno v: Bioorganicmedicinal chemistry letters. 20(19)

A series of 6-alkoxyisoindolin-1-ones with a magic shotgun pharmacological profile are presented as potential antipsychotics. The in vitro pharmacological profile includes D2 partial agonism (30–55%), 5-HT1A partial agonism (60–90%), and 5-HT2A a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::27c592ef4709fcdd3e293f25c74f12c4
https://pubmed.ncbi.nlm.nih.gov/20801650

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ChemInform Abstract: Parallel Synthesis of a Series of Subtype-Selective NMDA Receptor Antagonists

Autor: Richard M. Woodward, Edward R. Whittemore, Kevin A. Serpa, Lawrence D. Wise, Christopher S. Konkoy, Tracy F. Gregory, Jon Wright, Leonard T. Meltzer

Publikováno v: ChemInform. 31

A series of 1-(heteroarylthioalkyl)-4-benzylpiperidines was rapidly synthesized through the use of parallel synthesis to investigate the binding affinity for the NR1 a /2B receptor subtype.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c68dca9bb8c17fd4d7b0ff62e53abcc2
https://doi.org/10.1002/chin.200026240

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