Search Results - "Greig, Iain R"

The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB1 Receptor Positive Allosteric Modulators by Tseng, Chih-Chung, Baillie, Gemma, Donvito, Giulia, Mustafa, Mohammed A, Juola, Sophie E, Zanato, Chiara, Massarenti, Chiara, Dall’Angelo, Sergio, Harrison, William T. A, Lichtman, Aron H, Ross, Ruth A, Zanda, Matteo, Greig, Iain R

“…The first generation of CB1 positive allosteric modulators (e.g., ZCZ011) featured a 3-nitroalkyl-2-phenyl-indole structure. Although a small number of drugs…”
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Genomic and non-genomic pathways are both crucial for peak induction of neurite outgrowth by retinoids by Khatib, Thabat, Marini, Pietro, Nunna, Sudheer, Chisholm, David R, Whiting, Andrew, Redfern, Christopher, Greig, Iain R, McCaffery, Peter

“…Retinoic acid (RA) is the active metabolite of vitamin A and essential for many physiological processes, particularly the induction of cell differentiation. In…”
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Regulation of bone mass, bone loss and osteoclast activity by cannabinoid receptors by Ralston, Stuart H, Idris, Aymen I, van 't Hof, Robert J, Greig, Iain R, Ridge, Susan A, Baker, David, Ross, Ruth A

“…Accelerated osteoclastic bone resorption has a central role in the pathogenesis of osteoporosis and other bone diseases. Identifying the molecular pathways…”
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A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects by Ignatowska-Jankowska, Bogna M, Baillie, Gemma L, Kinsey, Steven, Crowe, Molly, Ghosh, Sudeshna, Owens, Robert A, Damaj, Imad M, Poklis, Justin, Wiley, Jenny L, Zanda, Matteo, Zanato, Chiara, Greig, Iain R, Lichtman, Aron H, Ross, Ruth A

“…The CB1 receptor represents a promising target for the treatment of several disorders including pain-related disease states. However, therapeutic applications…”
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Effects of glycol-split low molecular weight heparin on placental, endothelial, and anti-inflammatory pathways relevant to preeclampsia by Wat, Jovian M, Hawrylyshyn, Krista, Baczyk, Dora, Greig, Iain R, Kingdom, John C

“…Low molecular weight heparin (LMWH) is being investigated as a potential preventative therapy against preeclampsia. There is evidence suggesting that LMWH may…”
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Modulation of l-α-Lysophosphatidylinositol/GPR55 Mitogen-activated Protein Kinase (MAPK) Signaling by Cannabinoids by Anavi-Goffer, Sharon, Baillie, Gemma, Irving, Andrew J., Gertsch, Jürg, Greig, Iain R., Pertwee, Roger G., Ross, Ruth A.

“…GPR55 is activated by l-α-lysophosphatidylinositol (LPI) but also by certain cannabinoids. In this study, we investigated the GPR55 pharmacology of various…”
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Motor-like Tics are Mediated by CB2 Cannabinoid Receptor-dependent and Independent Mechanisms Associated with Age and Sex by Gorberg, Victoria, Borisov, Veronika, Greig, Iain R., Pertwee, Roger G., McCaffery, Peter, Anavi-Goffer, Sharon

“…Δ 9 -Tetrahydrocannabinol (Δ 9 -THC) inhibits tics in individuals with Tourette syndrome (TS). Δ 9 -THC has similar affinities for CB 1 /CB 2 cannabinoid…”
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Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators by Greig, Iain R., Baillie, Gemma L., Abdelrahman, Mostafa, Trembleau, Laurent, Ross, Ruth A.

“…[Display omitted] Existing CB1 negative allosteric modulators (NAMs) fall into a limited range of structural classes. In spite of the theoretical potential of…”
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Antidepressant activity of pharmacological and genetic deactivation of the small-conductance calcium-activated potassium channel subtype-3 by Nashed, Mina G., Waye, Shannon, Hasan, S. M. Nageeb, Nguyen, Diana, Wiseman, Micaela, Zhang, Jing, Lau, Harry, Dinesh, O. Chandani, Raymond, Roger, Greig, Iain R., Bambico, Francis Rodriguez, Nobrega, José N.

“…Rationale The voltage-insensitive, small-conductance calcium-activated potassium (SK) channel is a key regulator of neuronal depolarization and is implicated…”
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Aminobisphosphonates Cause Osteoblast Apoptosis and Inhibit Bone Nodule Formation In Vitro by Idris, Aymen I., Rojas, Javier, Greig, Iain R., van’t Hof, Rob J., Ralston, Stuart H.

“…Bisphosphonates are widely used for the treatment of bone diseases associated with increased osteoclastic bone resorption. Bisphosphonates are known to inhibit…”
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A novel allosteric modulator of the cannabinoid CB1 receptor ameliorates hyperdopaminergia endophenotypes in rodent models by Mielnik, Catharine A., Sugamori, Kim S., Finlay, David B., Thorpe, Hayley H. A., Schapira, Matthieu, Sivananthan, Nirunthan, Li, Chun Kit, Lam, Vincent M., Harrington, Sean, Abdelrahman, Mostafa H., Trembleau, Laurent A., McIntyre Burnham, W., Khokhar, Jibran Y., Salahpour, Ali, Ramsey, Amy J., Glass, Michelle, Greig, Iain R., Ross, Ruth A.

“…Abstract The endocannabinoid system (eCBs) encompasses the endocannabinoids, their synthetic and degradative enzymes, and cannabinoid (CB) receptors. The eCBs…”
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Development of Fluorinated Analogues of Perhexiline with Improved Pharmacokinetic Properties and Retained Efficacy by Tseng, Chih-Chung, Noordali, Hannah, Sani, Monica, Madhani, Melanie, Grant, Denis M, Frenneaux, Michael P, Zanda, Matteo, Greig, Iain R

“…We designed and synthesized perhexiline analogues that have the same therapeutic profile as the parent cardiovascular drug but lacking its metabolic liability…”
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In-vivo pharmacological evaluation of the CB1-receptor allosteric modulator Org-27569 by Gamage, Thomas F, Ignatowska-Jankowska, Bogna M, Wiley, Jenny L, Abdelrahman, Mostafa, Trembleau, Laurent, Greig, Iain R, Thakur, Ganesh A, Tichkule, Ritesh, Poklis, Justin, Ross, Ruth A, Pertwee, Roger G, Lichtman, Aron H

“…Several allosteric modulators (AMs) of the CB1 receptor have been characterized in vitro, including Org27569, which enhances CB1-specific binding of…”
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Synthesis and structure-activity relationship studies of novel tubulysin U analogues--effect on cytotoxicity of structural variations in the tubuvaline fragment by Shankar, Sreejith P, Jagodzinska, Monika, Malpezzi, Luciana, Lazzari, Paolo, Manca, Ilaria, Greig, Iain R, Sani, Monica, Zanda, Matteo

“…Tubulysins are cytotoxic natural products with promising anti-cancer properties, originally isolated from myxobacterial cultures. Structurally, tubulysins are…”
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The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB 1 Receptor Positive Allosteric Modulators by Tseng, Chih-Chung, Baillie, Gemma, Donvito, Giulia, Mustafa, Mohammed A, Juola, Sophie E, Zanato, Chiara, Massarenti, Chiara, Dall'Angelo, Sergio, Harrison, William T A, Lichtman, Aron H, Ross, Ruth A, Zanda, Matteo, Greig, Iain R

“…The first generation of CB positive allosteric modulators (e.g., ZCZ011) featured a 3-nitroalkyl-2-phenyl-indole structure. Although a small number of drugs…”
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In Vitro Characterization of 6‑Methyl-3-(2-nitro-1-(thiophen-2-yl)ethyl)-2-phenyl‑1H‑indole (ZCZ011) at the Type 1 Cannabinoid Receptor: Allosteric Agonist or Allosteric Modulator? by Green, Hayley M., Finlay, David B., Ross, Ruth A., Greig, Iain R., Duffull, Stephen B., Glass, Michelle

“…Orthosteric activation of CB1 is known to cause a plethora of adverse side effects in vivo. Allosteric modulation is an exciting therapeutic approach and is…”
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Identification of small molecule inhibitors of RANKL and TNF signalling as anti-inflammatory and antiresorptive agents in mice by Coste, Emmanuel, Greig, Iain R, Mollat, Patrick, Rose, Lorraine, Gray, Mohini, Ralston, Stuart H, van 't Hof, Rob J

“…Inflammatory joint diseases such as rheumatoid arthritis are associated with local bone erosions and systemic bone loss, mediated by increased osteoclastic…”
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Small-molecule targeting AMPA-mediated excitotoxicity has therapeutic effects in mouse models for multiple sclerosis by Zhai, Dongxu, Yan, Shuxin, Samsom, James, Wang, Le, Su, Ping, Jiang, Anlong, Zhang, Haorui, Jia, Zhengping, Wallach, Izhar, Heifets, Abraham, Zanato, Chiara, Tseng, Chih-Chung, Wong, Albert H C, Greig, Iain R, Liu, Fang

“…While most research and treatments for multiple sclerosis (MS) focus on autoimmune reactions causing demyelination, it is possible that neurodegeneration…”
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In Vitro Characterization of 6-Methyl-3-(2-nitro-1-(thiophen-2-yl)ethyl)-2-phenyl-1 H -indole (ZCZ011) at the Type 1 Cannabinoid Receptor: Allosteric Agonist or Allosteric Modulator? by Green, Hayley M, Finlay, David B, Ross, Ruth A, Greig, Iain R, Duffull, Stephen B, Glass, Michelle

“…Orthosteric activation of CB is known to cause a plethora of adverse side effects . Allosteric modulation is an exciting therapeutic approach and is hoped to…”
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Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics by Tyagi, Rahul, Maddirala, Amarendar Reddy, Elfawal, Mostafa, Fischer, Chelsea, Bulman, Christina A, Rosa, Bruce A, Gao, Xin, Chugani, Ryan, Zhou, Mingzhou, Helander, Jon, Brindley, Paul J, Tseng, Chih-Chung, Greig, Iain R, Sakanari, Judy, Wildman, Scott A, Aroian, Raffi, Janetka, James W, Mitreva, Makedonka

“…The enormous prevalence of infections caused by parasitic nematodes worldwide, coupled to the rapid emergence of their resistance to commonly used anthelmintic…”
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