Evidence that membrane-bound G protein-coupled melatonin receptors MT1 and MT2 are not involved in the neuroprotective effects of melatonin in focal cerebral ischemia

2011 ◽  
Vol 52 (2) ◽  
pp. 228-235 ◽  
Author(s):  
Ulkan Kilic ◽  
Bayram Yilmaz ◽  
Milas Ugur ◽  
Adnan Yüksel ◽  
Russel J. Reiter ◽  
...  
Keyword(s):  
Cerebral Ischemia ◽  
G Protein ◽  
Focal Cerebral Ischemia ◽  
Melatonin Receptors ◽  
Neuroprotective Effects ◽  
Membrane Bound ◽  
G Protein Coupled

scholarly journals Cyclical Regulation of GnRH Gene Expression in GT1–7 GnRH-Secreting Neurons by Melatonin

Endocrinology ◽  
2001 ◽  
Vol 142 (11) ◽  
pp. 4711-4720 ◽  
Author(s):  
Deboleena Roy ◽  
Nadia L. Angelini ◽  
Hiroki Fujieda ◽  
Gregory M. Brown ◽  
Denise D. Belsham
Keyword(s):  
Gene Expression ◽  
G Protein ◽  
Reproductive Physiology ◽  
Melatonin Receptors ◽  
Mrna Levels ◽  
Orphan Nuclear Receptors ◽  
Neuroendocrine Control ◽  
Gnrh Neurons ◽  
Membrane Bound ◽  
G Protein Coupled

Abstract The pineal hormone melatonin plays an important role in the neuroendocrine control of reproductive physiology, but its effects on hypothalamic GnRH neurons are not yet known. We have found that GT1–7 GnRH-secreting neurons express membrane-bound G protein-coupled melatonin receptors, mt1 (Mel-1a) and MT2 (Mel-1b) as well as the orphan nuclear receptors RORα and RZRβ. Melatonin (1 nm) significantly downregulates GnRH mRNA levels in a 24-h cyclical manner, an effect that is specifically inhibited by the melatonin receptor antagonist luzindole (10 μm). Repression of GnRH gene expression by melatonin appears to occur at the transcriptional level and can be mapped to the GnRH neuron-specific enhancer located within the 5′ regulatory region of the GnRH gene. Using transient transfection of GT1–7 cells, downregulation of GnRH gene expression by melatonin was further localized to five specific regions within the GnRH enhancer including −1827/−1819,− 1780/−1772, −1746/−1738, −1736/−1728, and −1697/−1689. Interestingly, the region located at −1736/−1728 includes sequences that correspond to two direct repeats of hexameric consensus binding sites for members of the ROR/RZR orphan nuclear receptor family. To begin to dissect the mechanisms involved in the 24-h cyclical regulation of GnRH transcription, we have found that melatonin (10 nm) induces rapid internalization of membrane-bound mt1 receptors through a β-arrestin 1-mediated mechanism. These results provide the first evidence that melatonin may mediate its neuroendocrine control on reproductive physiology through direct actions on the GnRH neurons of the hypothalamus, both at the level of GnRH gene expression and through the regulation of G protein-coupled melatonin receptors.

scholarly journals Molecular Targets of Cannabidiol in Experimental Models of Neurological Disease

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5186 ◽  
Author(s):  
Serena Silvestro ◽  
Giovanni Schepici ◽  
Placido Bramanti ◽  
Emanuela Mazzon
Keyword(s):  
G Protein ◽  
Serotonin Receptor ◽  
Molecular Mechanisms ◽  
Transient Receptor Potential ◽  
Neurological Diseases ◽  
In Vivo Studies ◽  
Receptor Subtype ◽  
Transient Receptor Potential Vanilloid ◽  
Neuroprotective Effects ◽  
G Protein Coupled

Cannabidiol (CBD) is a non-psychoactive phytocannabinoid known for its beneficial effects including antioxidant and anti-inflammatory properties. Moreover, CBD is a compound with antidepressant, anxiolytic, anticonvulsant and antipsychotic effects. Thanks to all these properties, the interest of the scientific community for it has grown. Indeed, CBD is a great candidate for the management of neurological diseases. The purpose of our review is to summarize the in vitro and in vivo studies published in the last 15 years that describe the biochemical and molecular mechanisms underlying the effects of CBD and its therapeutic application in neurological diseases. CBD exerts its neuroprotective effects through three G protein coupled-receptors (adenosine receptor subtype 2A, serotonin receptor subtype 1A and G protein-coupled receptor 55), one ligand-gated ion channel (transient receptor potential vanilloid channel-1) and one nuclear factor (peroxisome proliferator-activated receptor γ). Moreover, the therapeutical properties of CBD are also due to GABAergic modulation. In conclusion, CBD, through multi-target mechanisms, represents a valid therapeutic tool for the management of epilepsy, Alzheimer’s disease, multiple sclerosis and Parkinson’s disease.

Therapeutic Neuroprotective Effects of XQ-1H in a Rat Model of Permanent Focal Cerebral Ischemia

Pharmacology ◽  
2012 ◽  
Vol 89 (1-2) ◽  
pp. 1-6 ◽  
Author(s):  
Qichuan Yang ◽  
Weirong Fang ◽  
Peng Lv ◽  
Xiaohan Geng ◽  
Yunman Li ◽  
...  
Keyword(s):  
Cerebral Ischemia ◽  
Rat Model ◽  
Focal Cerebral Ischemia ◽  
Neuroprotective Effects

scholarly journals Perspectives on the Role of Non-Coding RNAs in the Regulation of Expression and Function of the Estrogen Receptor

Cancers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 2162
Author(s):  
Mohammad Taheri ◽  
Hamed Shoorei ◽  
Marcel E. Dinger ◽  
Soudeh Ghafouri-Fard
Keyword(s):  
Estrogen Receptor ◽  
G Protein ◽  
Reproductive System ◽  
Estrogen Regulation ◽  
Tissue Specific ◽  
Membrane Bound ◽  
Non Coding Rnas ◽  
And Function ◽  
G Protein Coupled

Estrogen receptors (ERs) comprise several nuclear and membrane-bound receptors with different tissue-specific functions. ERα and ERβ are two nuclear members of this family, whereas G protein-coupled estrogen receptor (GPER), ER-X, and Gq-coupled membrane estrogen receptor (Gq-mER) are membrane-bound G protein-coupled proteins. ERα participates in the development and function of several body organs such as the reproductive system, brain, heart and musculoskeletal systems. ERβ has a highly tissue-specific expression pattern, particularly in the female reproductive system, and exerts tumor-suppressive roles in some tissues. Recent studies have revealed functional links between both nuclear and membrane-bound ERs and non-coding RNAs. Several oncogenic lncRNAs and miRNAs have been shown to exert their effects through the modulation of the expression of ERs. Moreover, treatment with estradiol has been shown to alter the malignant behavior of cancer cells through functional axes composed of non-coding RNAs and ERs. The interaction between ERs and non-coding RNAs has functional relevance in several human pathologies associated with estrogen regulation, such as cancers, intervertebral disc degeneration, coronary heart disease and diabetes. In the current review, we summarize scientific literature on the role of miRNAs and lncRNAs on ER-associated signaling and related disorders.

Neuroprotective effects of neuregulin-1 in rat models of focal cerebral ischemia

2006 ◽  
Vol 1087 (1) ◽  
pp. 180-185 ◽  
Author(s):  
Wen-Ping Guo ◽  
Jie Wang ◽  
Rui-Xi Li ◽  
Yu-Wen Peng
Keyword(s):  
Cerebral Ischemia ◽  
Focal Cerebral Ischemia ◽  
Neuroprotective Effects ◽  
Neuregulin 1 ◽  
Rat Models
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