Heteromerization of Dopaminergic Receptors in the Brain: Pharmacological Implications

2021 ◽  
pp. 105600
Author(s):  
Desye Misganaw
2015 ◽  
Vol 13 (2) ◽  
pp. 10-13 ◽  
Author(s):  
Marat Igorevich Airapetov ◽  
Platon Platonovich Khokhlov ◽  
Eugeny Rudolfovich Bychkov ◽  
Edgar Arturovich Sekste ◽  
Natalia Dmitrievna Yakushina ◽  
...  

The purpose of the paper was to study both the desacylghrelin (unacylated ghrelin) level in the blood serum and expression of mRNA ghrelin receptor in the brain structures in ontogeny after chronic alcoholization in rats. The results proved that the prenatal effect of ethanol negatively affected the maturation of dopaminergic and ghrelin systems of the brain as well as involvement of ghrelin system in mechanisms of alcohol dependence formation. The decrease of COMT mRNA expression simultaneoully with the increase of expression of D2 long and short isoforms of dopaminergic receptors and misbalance of ghrelin system were observed. Alcoholization of mothers reduced desacylghrelin level in the blood serum in early postnatal period in offsprings although mRNA expression of ghrelin receptor in the brain was elevated. Chronic alcoholization of adult rats also affected the ghrelin system. In the alcoholiztion process, the reduced contents of desacylghrelin in the blood serum with compensatory increase of ghrelin receptor expression in the brain were registered. After withdrawal of ethanol, the recovery of desacylghrelin level (tendency to normalization) was observed.


2017 ◽  
Vol 67 (2) ◽  
pp. 215-226 ◽  
Author(s):  
Lourdes A. Vega Rasgado ◽  
Iván Villanueva ◽  
Fernando Vega Díaz

Abstractγ-Ethyl-γ-phenyl-butyrolactone (EFBL) is a structural combination of the anticonvulsant γ-hydroxy-γ-ethyl-γ-phenylbutyramide (HEPB) and the hypnotic γ-butyrolactone (GBL), which inherits both properties. To clarify its mechanism of action, the effects of EFBL, GBL and HEPB on dopamine (DA) and noradrenaline (NA) brain levels were investigated. Influences of chlorpromazine, phenelzine and aminooxyacetic acid were also studied. EFBL increased DA in a dose-dependent manner, remaining enhanced by 80 % over a period of 24 h and augmented NA by 54 % one hour after treatment. HEPB increased DA and NA approximately 2-fold after the first hour. GBL raised DA and NA after three and 24 h, resp. EFBL reversed chlorpromazine effects but potentiated those of phenelzine on DA. Amino-oxyacetic modified neither DA nor NA brain levels, not even in the presence of EFBL. The anticonvulsant and hypnotic properties of EFBL are attributed to its effect on presynaptic dopaminergic receptors and its lasting effect on ethyl and phenyl radicals that hinder its degradation. The results support the role of DA and NA in regulating seizure activity in the brain and indicate that EFBL offers a potential treatment for refractory epilepsy without complementary drugs and Parkinson’s disease, without the drawbacks of oral therapies.


1979 ◽  
Vol 31 (1) ◽  
pp. 91-93 ◽  
Author(s):  
FREDERICK N. MINARD ◽  
JOHN C. CAIN ◽  
DENNIS S. GRANT ◽  
ANTHONY T. DREN

2019 ◽  
Vol 12 (12) ◽  
pp. 714-719
Author(s):  
Robert West

Restless legs syndrome is a common, often debilitating disorder, which is under-recognised and under-diagnosed. Patients typically describe an uncomfortable urge to move their legs, this occurs mainly at night. It often has a significant impact on the quality of sleep, and hence, daily functioning. The pathophysiology of the disorder is well known, it relates to iron depletion and dopaminergic receptors in the brain, and this has aided the development of effective treatment. This article will cover the recognition, pathophysiology and management of the condition.


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