Výsledky vyhledávání - "Karine Fabio"

Pharmacokinetics and Metabolism of SRX246: A Potent and Selective Vasopressin 1a Antagonist

Autor: Karine Fabio, Michael J. Brownstein, Shi-fang Lu, Christophe Guillon, Carrie Garippa, Carl Jeffrey Lacey, Neal G. Simon, Ned D. Heindel

Publikováno v: Journal of Pharmaceutical Sciences. 102:2033-2043

SRX246 is a potent, highly selective, orally bioavailable vasopressin 1a receptor antagonist that represents a novel mechanism of action for the treatment of mood disorders. The compound previously showed efficacy in animal models of mood disorders a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9f4efb839e92eac3417ca281c41a8d2
https://doi.org/10.1002/jps.23495

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Investigation of anticholinergic and non-steroidal anti-inflammatory prodrugs which reduce chemically induced skin inflammation

Autor: Christophe Guillon, Karine Fabio, Jaya Saxena, Sherri C. Young, Ned D. Heindel, Anna M. Vetrano, Diane E. Heck, Meredith P. Harman, Jeffrey D. Laskin, Mou-Tuan Huang, Robert A. Flowers

Publikováno v: Journal of Applied Toxicology. 32:135-141

As part of a continuous effort to develop efficient counter measures against sulfur mustard injuries, several unique NSAID prodrugs have been developed and screened for anti-inflammatory properties. Presented herein are three classes of prodrugs whic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2d9044099749d47342427de2b1e89113
https://doi.org/10.1002/jat.1645

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Vasopressin Antagonists as Anxiolytics and Antidepressants: Recent Developments

Autor: Michael J. Brownstein, Shi-fang Lu, Karine Fabio, Gary A. Koppel, Marvin J. Miller, Neal G. Simon, Craig F. Ferris, Ned D. Heindel, Carrie Garripa, Christophe Guillon

Publikováno v: Recent Patents on CNS Drug Discovery. 3:77-93

A compelling case for the potential utility of vasopressin (AVP) antagonists as a novel therapeutic class for the treatment of stress-related affective illness has emerged based on observations in depressed individuals, findings in animal models of a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::227adc08a3c68d6f77e000555eb575c6
https://doi.org/10.2174/157488908784534586

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Azetidinones as vasopressin V1a antagonists

Autor: Jeffrey J. Skelton, Karine Fabio, Robin D. G. Cooper, Robert F. Bruns, Gary A. Koppel, Stephen W. Kaldor, David C. Hunden, Bruce A. Dressman, Michael P. Clay, Mitchell I. Steinberg, Michael J. Brownstein, Neal G. Simon, Christophe Guillon, Craig F. Ferris, Marvin J. Miller, Michael O. Chaney, Shi-fang Lu, Ned D. Heindel

Publikováno v: Bioorganic & Medicinal Chemistry. 15:2054-2080

The azetidinone LY307174 (1) was identified as a screening lead for the vasopressin V1a receptor (IC50 45 nM at the human V1a receptor) based on molecular similarity to ketoconazole (2), a known antagonist of the luteinizing hormone releasing hormone

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fcea47a4dc266c2aa7647f92ba4147e5
https://doi.org/10.1016/j.bmc.2006.12.031

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Heat-Stable Dry Powder Oxytocin Formulations for Delivery by Oral Inhalation

Autor: Benoit Adamo, Kelly Kraft, Brendan Laurenzi, Joseph J. Guarneri, Andrea Leone-Bay, Marshall Grant, Kieran Curley, Karine Fabio, Robin Offord

Publikováno v: AAPS PharmSciTech. 16(6)

In this work, heat stable dry powders of oxytocin (OT) suitable for delivery by oral inhalation were prepared. The OT dry powders were prepared by spray drying using excipients chosen to promote OT stability including trehalose, isoleucine, polyvinyl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eab558b18cfdb80397256bdeb3128ecf
https://pubmed.ncbi.nlm.nih.gov/25776985

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New perfluorinated polycationic dimerizable detergents for the formulation of monomolecular DNA nanoparticles and their in vitro transfection efficiency

Autor: Christophe Di Giorgio, Pierre Vierling, Karine Fabio

Publikováno v: Biochimica et Biophysica Acta (BBA) - General Subjects. 1724:203-214

We describe the synthesis of new perfluorinated dimerizable detergents which contain a tricationic or tetracationic (linear or branched spermine, respectively) polar head, and report on their cmc, their ability to condense DNA into cationic monomolec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69e55e8a20267a97e0dcd3f78dc7edf5
https://doi.org/10.1016/j.bbagen.2005.03.007

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Synthesis and evaluation of potent and selective human V1a receptor antagonists as potential ligands for PET or SPECT imaging

Autor: Karine Fabio, Neal G. Simon, Graham B. Jones, Christophe Guillon, Ned D. Heindel, Michael J. Brownstein, Shi-fang Lu, Michael S. Placzek, Carl Jeffrey Lacey, Craig F. Ferris

Publikováno v: Bioorganicmedicinal chemistry. 20(3)

SRX246 is a potent, highly selective human vasopressin V1a antagonist that crosses the blood–brain barrier in rats. CNS penetration makes SRX246 an ideal candidate for potential radiolabeling and use in visualization and characterization of the rol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac231336e36bac3fbd34b4ecd5d2ba4f
https://pubmed.ncbi.nlm.nih.gov/22249122

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Vasopressin Antagonists as Anxiolytics and Antidepressants: Recent Developments

Autor: null Karine Fabio, null Christophe Guillon, null Shi-fang Lu, null Ned D. Heindel, null Marvin Miller, null Craig F. Ferris, null Michael J. Brownstein, null Carrie Gar

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1981d4d948070bdfdc02b5b4ec6ae62f
https://doi.org/10.2174/978160805159511001010156

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Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction

Autor: Ned D. Heindel, Sherri Young, Diane E. Heck, Jeffrey D. Laskin, Christophe Guillon, Pramod K. Mohanta, Robert A. Flowers, Timothy A. Halton, Karine Fabio

Publikováno v: Bioorganicmedicinal chemistry letters. 20(9)

The design and study of two classes of noncompetitive acetylcholinesterase inhibitors (AChEIs) which also function as NSAID prodrugs are reported. The most potent AChEIs disclosed contain an aromatic alkyl-aryl linker between an NSAID and a lipophili

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a072bba2f3d8668a836926cbcfd95baa
https://pubmed.ncbi.nlm.nih.gov/20347302

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Novel galactosylated polyamine bolaamphiphiles for gene delivery

Autor: Pierre Vierling, Karine Fabio, Jérôme Gaucheron, Christophe Di Giorgio

Publikováno v: Bioconjugate chemistry. 14(2)

We describe the synthesis of a series of alpha-galacto-omega-polyamine double-chain bolaamphiphiles (Gal-CL) and report on the gene transfer mediated with lipoplexes they form either when used in conjunction with DOPE or with pcTG90:DOPE. Lipofection

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::143270e4768302413a3a0f71d4b487c9
https://pubmed.ncbi.nlm.nih.gov/12643746

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