Retinoid Receptor-Selective Agonists and Their Action in Skin

1999 ◽  
pp. 539-559 ◽  
Author(s):  
B. Shroot ◽  
D. F. C. Gibson ◽  
X.-P. Lu
Keyword(s):  
Retinoid Receptor ◽  
Selective Agonists

Influence of selective agonists of retinoid receptor X (RXR) and retinoid acid receptor (RAR) on bone metabolism in rats

2013 ◽  
Vol 65 ◽  
pp. 71
Author(s):  
Beata Nowak ◽  
Agnieszka Matuszewska ◽  
Anna Merwid-Ląd ◽  
Małgorzata Pieśniewska ◽  
Lidia Fereniec-Gołębiewska ◽  
...  
Keyword(s):  
Bone Metabolism ◽  
Retinoid Receptor ◽  
Acid Receptor ◽  
Selective Agonists ◽  
Retinoid Acid

scholarly journals Role of retinoid receptors in the regulation of mucin gene expression by retinoic acid in human tracheobronchial epithelial cells

1999 ◽  
Vol 338 (2) ◽  
pp. 351-357 ◽  
Author(s):  
Ja Seok KOO ◽  
Anton M. JETTEN ◽  
Paula BELLONI ◽  
Joo-Heon YOON ◽  
Yong-Dae KIM ◽  
...  
Keyword(s):  
Gene Expression ◽  
Retinoic Acid ◽  
Cell Differentiation ◽  
Mucous Cell ◽  
Dependent Manner ◽  
Retinoid Receptor ◽  
Retinoid Receptors ◽  
Mucin Gene ◽  
Mucin Genes ◽  
Selective Agonists

To investigate which retinoid receptors are critical in the regulation by all-trans-retinoic acid (RA) of the mucin genes MUC2, MUC5AC and MUC5B in cultured normal human tracheobronchial epithelial (NHTBE) cells, we used pan-RAR-, pan-RXR- and RAR- isotype (α, β and γ)-selective agonists and RARα- and RARγ-selective antagonists (RAR is RA receptor and RXR is retinoid X receptor). RAR-, RARα- and RARγ-selective agonists strongly induced mucin mRNAs in a dose-dependent manner, while the RARβ-selective retinoid only weakly induced mucin gene expression at very high concentrations (1 µM). The pan-RXR-selective agonist by itself did not induce mucin gene expression, but acted synergistically with suboptimal concentrations of the pan-RAR agonist. A retinoid with selective anti-activator-protein-1 activity only marginally induced mucin gene expression. The RARα antagonist strongly inhibited mucin gene induction and mucous cell differentiation caused by RA and by the RARα- and RARγ-selective retinoids. In contrast, the RARγ antagonist only weakly inhibited RARα-selective-retinoid-induced mucin gene expression, but completely blocked mucin gene expression induced by the RARγ-selective retinoid. Our studies indicate that RARα is the major retinoid receptor subtype mediating RA-dependent mucin gene expression and mucous cell differentiation, but that the RARγ isotype can also induce mucin genes. Furthermore these studies suggest that RARβ is probably not (directly) involved in RA-induced mucin gene expression.

Effect of opioid peptides on liver function after patial hepatectomy

2018 ◽  
pp. 67-71
Author(s):  
А.В. Солин ◽  
А.Ю. Ляшев ◽  
Ю.Д. Ляшев
Keyword(s):  
Lactate Dehydrogenase ◽  
Liver Failure ◽  
Partial Hepatectomy ◽  
Opioid Receptors ◽  
Total Protein ◽  
Pronounced Effect ◽  
Male Rats ◽  
Control Group ◽  
Peptide Molecule ◽  
Selective Agonists

Цель исследования - сравнительный анализ влияния селективных агонистов отдельных классов опиоидных рецепторов на белковосинтетическую функцию печени, развитие цитолитического и холестатического синдромов у крыс, подвергшихся частичной гепатэктомии. Методика. Работа выполнена на 152 крысах-самцах Вистар массой 200-250 г. Частичную гепатэктомию выполняли по методу, описанному Higgins G.M. и Anderson R.M. с удалением 70% ткани печени. В плазме крови определяли концентрации общего белка, альбуминов, общего билирубина, активность аланинтрансаминазы (АЛТ), аспартаттрансаминазы (АСТ), лактатдегидрогеназы (ЛДГ) традиционными методами. Опиоиды: DAGO в дозе 6,3 мкг/кг, DSLET в дозе 10,0 мкг/кг, динорфин А (1-13) в дозе 20,1 мкг/кг, вводили внутрибрюшинно ежедневно 1 раз в сутки в течение 5 сут. эксперимента в объеме 0,2 мл. Контрольным животным аналогично вводили физраствор. Результаты. Удаление 70% ткани печени у крыс-самцов Вистар сопровождается развитием печеночной недостаточности, проявляющейся гипербилирубинемией, гипоальбуминемией, гипопротеинемией, повышением активности трансаминаз и лактатдегидрогеназы. Применение селективных агонистов опиоидных рецепторов у крыс, которым моделировали частичную гепатэктомию, оказывало гепатопротективное действие и снижало выраженность проявлений печеночной недостаточности, начиная с 3-х сут. после резекции. Активность трансаминаз, лактатдегидрогеназы и концентрация общего билирубина у животных, которым вводили опиоиды, были существенно ниже, чем в контрольной группе. Содержание общего белка и альбуминов было статистически значимо выше в группах, которые получали исследованные пептиды, по сравнению с контрольной группой на 7-е сут. после частичной гепатэктомии. Наиболее выраженное действие проявлял селективный агонист опиоидных мю-рецепторов DAGO. По нашему мнению, такое влияние пептидов объясняется присущими им антиоксидантным и антигипоксическим эффектами, что снижает повреждающее действие оперативного вмешательства на печень. Более выраженное влияние DAGO связано, по-видимому, с особенностями распределения опиоидных рецепторов или устойчивостью пептида к действию эндопептидаз благодаря модификациям в молекуле пептида. Заключение. Применение опиоидов стимулирует восстановление функциональной активности печени после частичной гепатэктомии. Наибольший эффект отмечается при введении мю-агониста DAGO. Aim. The aim of the study was to compare effects of selective agonists of opioid receptors from different classes on the protein-synthesizing function of liver and development of cytolytic and cholestatic syndromes in rats after partial hepatectomy. Methods. The study was conducted on 152 Wistar male rats weighing 200-250 g. The animals were subjected to partial hepatectomy according to the Higgins and Anderson method. Concentrations of total protein, albumin, total bilirubin, and activities of alanine aminotransferase, aspartate aminotransferase, and lactate dehydrogenase were measured in plasma using standard methods. The opioids, DAGO (6.3 mg/kg), DSLET (10.0 mg/kg), and dynorphin A (1-13) (20.1 mg/kg), were injected in 0.2 ml of saline daily for 5 days. Control animals were injected with 0.2 ml of saline for 5 days. Results. Resection of 70% of liver tissue resulted in development of liver failure as evidenced by hyperbilirubinemia, hypoalbuminemia, hypoproteinemia, and increased transaminase and lactate dehydrogenase activities. Selective agonists of opioid receptors administered to the rats after partial hepatectomy exerted a hepatoprotective effect and alleviated the signs of liver failure beginning from the 3 day after resection. Transaminase and lactate dehydrogenase activities were significantly lower in opioid-treated rats than in the control group. Levels of total protein and albumins were significantly higher in the groups injected with the study peptides compared to the control group on the 7 day after partial hepatectomy. The selective agonist of opioid m-receptors, DAGO, exerted the most pronounced effect. Apparently, the similar effects of peptides were due to their antioxidant and anti-hypoxic action, which alleviated the detrimental effect of liver surgery. The more pronounced effect of DAGO apparently resulted from peculiarities of opioid receptors distribution or peptide resistance to endopeptidase action due to modifications of the peptide molecule. Conclusion. Administration of opioids stimulated restoration of liver functional activity after partial hepatectomy. Injections of the m-agonist, DAGO, produced the most pronounced effect.

Retinoid X Receptor Selective Agonists and their Synthetic Methods

2017 ◽  
Vol 17 (6) ◽  
pp. 742-767 ◽  
Author(s):  
Carl E. Wagner ◽  
Peter W. Jurutka ◽  
Pamela A. Marshall ◽  
Michael C. Heck
Keyword(s):  
Retinoid X Receptor ◽  
Synthetic Methods ◽  
Selective Agonists

The melanocortin system

2003 ◽  
Vol 284 (3) ◽  
pp. E468-E474 ◽  
Author(s):  
Ira Gantz ◽  
Tung M. Fong
Keyword(s):  
Sexual Function ◽  
Energy Homeostasis ◽  
Melanocortin Receptors ◽  
Experimental Basis ◽  
Melanocortin System ◽  
Genetic Studies ◽  
Melanocortin Peptides ◽  
Selective Agonists ◽  
Made In

The melanocortin system consists of melanocortin peptides derived from the proopiomelanocortin gene, five melanocortin receptors, two endogenous antagonists, and two ancillary proteins. This review provides an abbreviated account of the basic biochemistry, pharmacology, and physiology of the melanocortin system and highlights progress made in four areas. In particular, recent pharmacological and genetic studies have affirmed the role of melanocortins in pigmentation, inflammation, energy homeostasis, and sexual function. Development of selective agonists and antagonists is expected to further facilitate the investigation of these complex physiological functions and provide an experimental basis for new pharmacotherapies.

Novel four selective agonists for prostaglandin E receptor subtypes

1999 ◽  
Vol 59 (1-6) ◽  
pp. 150 ◽  
Author(s):  
Hiroshi Yamamoto ◽  
Takayuki Maruyama ◽  
Kiyoto Sakata ◽  
Masatoshi Koketsu ◽  
Michiyoshi Kobayashi ◽  
...  
Keyword(s):  
Prostaglandin E ◽  
Receptor Subtypes ◽  
Selective Agonists
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