scholarly journals Pharmacophore‐guided Virtual Screening to Identify New β3‐Adrenergic Receptor Agonists

2021 ◽  
Author(s):  
Navista Sri Octa Ujiantari ◽  
Seungmin Ham ◽  
Chisae Nagiri ◽  
Wataru Shihoya ◽  
Osamu Nureki ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Adrenergic Receptor ◽  
Receptor Agonists

620 β-Adrenergic receptor agonists- and cAMP-mediated suppression of the proliferation of microglial cells in culture

1997 ◽  
Vol 28 ◽  
pp. S89
Author(s):  
Masahiro Sakanaka ◽  
Hiroko Fujita ◽  
Junya Tanaka ◽  
Seiji Matsuda ◽  
Nobuji Maeda
Keyword(s):  
Adrenergic Receptor ◽  
Microglial Cells ◽  
Receptor Agonists ◽  
Cells In Culture

Guanabenz and Clonidine, α2-Adrenergic Receptor Agonists, Inhibit Choroidal Neovascularization

2021 ◽  
Vol 18 ◽  
Author(s):  
Miruto Tanaka ◽  
Yuki Inoue ◽  
Takahiko Imai ◽  
Norifumi Tanida ◽  
Koichi Takahashi ◽  
...  
Keyword(s):  
Choroidal Neovascularization ◽  
Adrenergic Receptor ◽  
Intraperitoneal Administration ◽  
Age Related Macular Degeneration ◽  
High Dose ◽  
Adrenergic Agonists ◽  
Continuous Administration ◽  
Cell Growth And Migration ◽  
Receptor Agonists ◽  
Age Related

Background: Neovascular age-related macular degeneration (AMD) with choroidal neovascularization (CNV) is a leading cause of blindness in elderly people. Anti-vascular endothelial growth factor (anti-VEGF)-drugs are used to treat AMD patients; however, some patients are resistant to these therapies. Objective: The purpose of this study was to investigate the anti-angiogenic effects of α2-adrenergic agonists, including guanabenz and clonidine. Methods: We evaluated the anti-angiogenic effects of α2-adrenergic agonists in human retinal microvascular endothelial cells (HRMECs). A proliferation assay was conducted, and the migration ratio was evaluated. In a laser-induced CNV model, guanabenz and clonidine were delivered via intraperitoneal injection or implantation of an osmotic pump device. Fourteen days following CNV induction, CNV lesion size and fundus fluorescein angiography (FFA) were evaluated. Results: Guanabenz and clonidine inhibited VEGF-induced retinal endothelial cell growth and migration. In the CNV model mice, CNV lesion sizes were reduced by intraperitoneal administration of guanabenz or clonidine. Data, including body weight, systolic blood pressure, and heart rate showed that guanabenz (0.5 and 2.0 mg/kg/day) had little effect on these parameters; conversely, a high dose of clonidine (1.0 mg/kg/day) did affect these parameters. Additionally, clonidine did not affect CNV size, but continuous administration of guanabenz attenuated both CNV size and leakage from neovessels. Conclusion: Our study suggests a key role for α2-adrenergic receptors during CNV formation. Therefore, we suggest that α2-adrenergic receptor agonists may represent novel therapeutic drugs for patients with neovascular AMD.

3-pyridylethanolamines: Potent and selective human β3 adrenergic receptor agonists

1998 ◽  
Vol 8 (21) ◽  
pp. 3087-3092 ◽  
Author(s):  
Elizabeth M. Naylor ◽  
Vincent J. Colandrea ◽  
Mari R. Candelore ◽  
Margaret A. Cascieri ◽  
Lawrence F. Colwell ◽  
...  
Keyword(s):  
Adrenergic Receptor ◽  
Receptor Agonists

scholarly journals Adrenergic receptor agonists induce the differentiation of pluripotent stem cell-derived hepatoblasts into hepatocyte-like cells

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Maki Kotaka ◽  
Taro Toyoda ◽  
Katsutaro Yasuda ◽  
Yuko Kitano ◽  
Chihiro Okada ◽  
...  
Keyword(s):  
Stem Cell ◽  
Adrenergic Receptor ◽  
Pluripotent Stem Cell ◽  
Receptor Agonists

Rat Carotid Artery Responses to ?-Adrenergic Receptor Agonists and 5-HT After Ovariectomy and Hormone Replacement

2007 ◽  
Vol 47 (2) ◽  
pp. 236-246 ◽  
Author(s):  
Suneet Mehrotra ◽  
Saurabh Gupta ◽  
Carlos M. Villalón ◽  
Frans Boomsma ◽  
Pramod R. Saxena ◽  
...  
Keyword(s):  
Carotid Artery ◽  
Adrenergic Receptor ◽  
Hormone Replacement ◽  
Receptor Agonists

Tryptamine-based human β3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives

2004 ◽  
Vol 14 (24) ◽  
pp. 5963-5966 ◽  
Author(s):  
Masaaki Sawa ◽  
Hirotaka Tateishi ◽  
Kazuhiro Mizuno ◽  
Hiroshi Harada ◽  
Mayumi Oue ◽  
...  
Keyword(s):  
Adrenergic Receptor ◽  
Receptor Agonists
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