Selective orexin receptor antagonists
TP Lebold, P Bonaventure, BT Shireman - Bioorganic & medicinal …, 2013 - Elsevier
The orexin, or hypocretin, neuropeptides (orexin-A and orexin-B) are produced on neurons
in the hypothalamus which project to key areas of the brain that control sleep–wake states, …
in the hypothalamus which project to key areas of the brain that control sleep–wake states, …
Copper-mediated synthesis of drug-like bicyclopentanes
Multicomponent reactions are relied on in both academic and industrial synthetic organic
chemistry owing to their step- and atom-economy advantages over traditional synthetic …
chemistry owing to their step- and atom-economy advantages over traditional synthetic …
Direct catalytic asymmetric aldol additions of methyl ynones. Spontaneous reversal in the sense of enantioinduction
BM Trost, A Fettes, BT Shireman - Journal of the American …, 2004 - ACS Publications
In this Communication, we report the direct, catalytic, asymmetric aldol addition of methyl
ynones using our dinuclear zinc catalyst. A spontaneous reversal in the sense of …
ynones using our dinuclear zinc catalyst. A spontaneous reversal in the sense of …
Dinuclear asymmetric Zn aldol additions: formal asymmetric synthesis of fostriecin
…, PE Harrington, S Shin, BT Shireman - Journal of the …, 2005 - ACS Publications
Direct asymmetric aldol reactions constitute a powerful methodology for the efficient synthesis
of complex natural products. Herein we report the first application of our recently reported …
of complex natural products. Herein we report the first application of our recently reported …
A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects
…, PL Johnson, A Shekhar, SD Fitz, BT Shireman… - … of Pharmacology and …, 2015 - ASPET
Orexins (OXs) are peptides produced by perifornical (PeF) and lateral hypothalamic neurons
that exert a prominent role in arousal-related processes, including stress. A critical role for …
that exert a prominent role in arousal-related processes, including stress. A critical role for …
Identification of small-molecule protein–protein interaction inhibitors for NKG2D
…, ML Rives, S Sharma, BT Shireman… - Proceedings of the …, 2023 - National Acad Sciences
NKG2D (natural-killer group 2, member D) is a homodimeric transmembrane receptor that
plays an important role in NK, γδ + , and CD8 + T cell-mediated immune responses to …
plays an important role in NK, γδ + , and CD8 + T cell-mediated immune responses to …
[HTML][HTML] Orexin-1 receptor blockade dysregulates REM sleep in the presence of orexin-2 receptor antagonism
…, S Yun, P Bonaventure, BT Shireman… - Frontiers in …, 2014 - frontiersin.org
… Shireman provided compounds; Timothy W. Lovenberg participated in research design. …
Copyright © 2014 Dugovic, Shelton, Yun, Bonaventure, Shireman and Lovenberg. This is an …
Copyright © 2014 Dugovic, Shelton, Yun, Bonaventure, Shireman and Lovenberg. This is an …
[HTML][HTML] Translational evaluation of novel selective orexin-1 receptor antagonist JNJ-61393215 in an experimental model for panic in rodents and humans
…, A Shekhar, PL Johnson, B Lord, BT Shireman… - Translational …, 2020 - nature.com
Orexin neurons originating in the perifornical and lateral hypothalamic area project to
anxiety- and panic-associated neural circuitry, and are highly reactive to anxiogenic stimuli. …
anxiety- and panic-associated neural circuitry, and are highly reactive to anxiogenic stimuli. …
Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate
…, JE Shelton, CR Shah, BT Shireman… - Journal of medicinal …, 2015 - ACS Publications
The preclinical characterization of novel octahydropyrrolo[3,4-c]pyrroles that are potent and
selective orexin-2 antagonists is described. Optimization of physicochemical and DMPK …
selective orexin-2 antagonists is described. Optimization of physicochemical and DMPK …
[HTML][HTML] Selective inhibition of orexin-2 receptors prevents stress-induced ACTH release in mice
…, P Bonaventure, MA Letavic, BT Shireman… - Frontiers in Behavioral …, 2017 - frontiersin.org
Orexins peptides exert a prominent role in arousal-related processes including stress
responding, by activating orexin-1 (OX1R) and orexin-2 (OX2R) receptors located widely …
responding, by activating orexin-1 (OX1R) and orexin-2 (OX2R) receptors located widely …