Výsledky vyhledávání - "Stephane St-Onge"

Discovery of Agonists of Cannabinoid Receptor 1 with Restricted Central Nervous System Penetration Aimed for Treatment of Gastroesophageal Reflux Disease

Autor: Wei Zhongyong, Johan Broddefalk, Madeleine Antonsson, Kosrat Amin, Jörgen Jensen, Johan Ulander, Maxime Tremblay, Stephane St-Onge, Karolina Nilsson, Shujuan Jin, Anders Lehmann, Alleyn T. Plowright, Christopher Walpole, Tomaszewski Miroslaw, Hua Yang

Publikováno v: Journal of Medicinal Chemistry. 56:220-240

Agonists of the cannabinoid receptor 1 (CB1) have been suggested as possible treatments for a range of medical disorders including gastroesophageal reflux disease (GERD). While centrally acting cannabinoid agonists are known to produce psychotropic e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7e05819466ec51f70ae07e9321387a5
https://doi.org/10.1021/jm301511h

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γ-Carbolines: A novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration

Autor: Xuehong Luo, Xiao Hong Yu, Pourashraf Mehrnaz, Sanjay Srivastava, Dominic Salois, Cheng Yun-Xing, Kemal Payza, Christopher Walpole, Etienne Lessard, Stephane St-Onge, Tomaszewski Miroslaw

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:1619-1624

An oral, peripherally restricted CB1/CB2 agonist could provide an interesting approach to treat chronic pain by harnessing the analgesic properties of cannabinoids but without the well-known central side effects. γ-Carbolines are a novel class of po

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a70c2a778db169330114c41d0ed05f33
https://doi.org/10.1016/j.bmcl.2011.12.124

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N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: The development of diaryl amino piperidines as potent δ opioid receptor agonists with in vivo anti-nociceptive activity in rodent models

Autor: Martin Coupal, Paul Jones, Lejla Hodzic, Wenhau Xiao, Edward Roberts, Andrew Griffin, Daniel Delorme, Dominic Salois, Maryse Labarre, Stephane St-Onge, Christopher Walpole, Jamie Boulet, Lars Gawell, Rico Lavoie, Joanne Butterworth, William Brown

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:5994-5998

We have investigated a series of phenolic diaryl amino piperidine delta opioid receptor agonists, establishing the importance of the phenol functional group and substitution on the piperdine nitrogen for delta agonist activity and selectivity versus

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::309cc40e144f4ea22f0ebf8874c89c2d
https://doi.org/10.1016/j.bmcl.2009.09.072

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N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration

Autor: William Brown, Tomaszewski Miroslaw, Etienne Lessard, Christopher Walpole, Wei Zhongyong, Hua Yang, Beha Sara, Sanjay Srivastava, Maxime Tremblay, Shi Yi Yue, Shawn Johnstone, Stephane St-Onge, Thierry Groblewski, Anne-Julie Archambault, Ziping Liu, Page Daniel

Publikováno v: Bioorganicmedicinal chemistry letters. 22(12)

Cannabinoid CB1 receptor agonists exhibit potent analgesic effects in rodents and humans, but their clinical utility as analgesic drugs is often limited by centrally mediated side effects. We report herein the preparation of N-methyl-3-(tetrahydro-2H

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8398b5e47f84620dc49296ccdf8d606e
https://pubmed.ncbi.nlm.nih.gov/22607668

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A peripherally restricted cannabinoid receptor agonist produces robust anti-nociceptive effects in rodent models of inflammatory and neuropathic pain

Autor: Jennifer M. A. Laird, Giovanni Martino, Anne Morinville, Stephane St-Onge, Chang Qing Cao, Carole Puma, Etienne Lessard, Xiao Hong Yu, Martin N. Perkins

Publikováno v: PainReferences. 151(2)

Cannabinoids are analgesic in man, but their use is limited by their psychoactive properties. One way to avoid cannabinoid receptor subtype 1 (CB1R)-mediated central side-effects is to develop CB1R agonists with limited CNS penetration. Activation of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99590df3616f980bb68625bdcd9e35a4
https://pubmed.ncbi.nlm.nih.gov/20696525

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New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists

Autor: Page Daniel, Christopher Walpole, François Gaudreault, Meredith Fyfe, Hua Yang, Manon Fleurent, Stephane St-Onge, William Brown

Publikováno v: Bioorganicmedicinal chemistry letters. 17(22)

The preparation and evaluation of a novel class of CB2 agonists based on a 1,2,3,4-tetrahydropyrrolo[3,4-b]indole moiety are reported. They showed binding affinities up to 4.2 nM toward CB2 with sub-nanomolar EC50 values. They also showed moderate to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13002dd9d03208d0da7bfdc7ac12b204
https://pubmed.ncbi.nlm.nih.gov/17884494

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New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability

Publikováno v: Journal of medicinal chemistry. 43(21)

Nonpeptide delta opioid agonists are analgesics with a potentially improved side-effect and abuse liability profile, compared to classical opioids. Andrews analysis of the NIH nonpeptide lead SNC-80 suggested the removal of substituents not predicted

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9712a1e21e6971a34a29440bf30ca9be
https://pubmed.ncbi.nlm.nih.gov/11052793

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