Methods for the Evaluation of Drug Action at the Human Melatonin Receptor Subtypes

Neurosignals ◽  
1999 ◽  
Vol 8 (1-2) ◽  
pp. 32-40 ◽  
Author(s):  
Romolo Nonno ◽  
Franco Fraschini ◽  
BojidarM. Stankov
Keyword(s):  
Drug Action ◽  
Receptor Subtypes ◽  
Melatonin Receptor

Expression analysis of melatonin receptor subtypes in the ovary of domestic chicken

2008 ◽  
Vol 33 (1) ◽  
pp. 49-56 ◽  
Author(s):  
N. R. Sundaresan ◽  
M. D. Marcus Leo ◽  
J. Subramani ◽  
D. Anish ◽  
M. Sudhagar ◽  
...  
Keyword(s):  
Expression Analysis ◽  
Domestic Chicken ◽  
Receptor Subtypes ◽  
Melatonin Receptor

scholarly journals Differential Expression of Melatonin Receptor Subtypes MelIa, MelIb and MelIc in Relation to Melatonin Binding in the Male Songbird Brain

2014 ◽  
Vol 85 (1) ◽  
pp. 4-14 ◽  
Author(s):  
Leonida Fusani ◽  
Manfred Gahr
Keyword(s):  
Expression Patterns ◽  
General Pattern ◽  
Passerine Bird ◽  
Brain Regions ◽  
Receptor Expression ◽  
Receptor Subtype ◽  
Receptor Subtypes ◽  
Melatonin Receptor ◽  
Brain Areas ◽  
Specific Expression

Previous autoradiography studies illustrated that several areas of the avian brain can bind the pineal hormone melatonin. In birds, there are three melatonin receptor (MelR) subtypes: MelIa, MelIb and MelIc. To date, their brain distribution has not been studied in any passerine bird. Therefore, we investigated mRNA distribution of MelR subtypes in adjacent sections of the brain of two songbirds, the blackcap and the zebra finch, in parallel with that of 2-[125I]-iodomelatonin (IMEL) binding sites in the same brains. The general pattern of receptor expression shown by in situ hybridization of species-specific probes matched well with that of IMEL binding. However, the expression of the three subtypes was area specific with similar patterns in the two species. Some brain areas expressed only one receptor subtype, most brain regions co-expressed either MelIa with MelIb or MelIa with MelIc, whereas few areas expressed MelIb and MelIc or all three receptor subtypes. Since many sensory areas, most thalamic areas and subareas of the neopallium, a cortex analogue, express MelR, it is likely that most sensory motor integration functions are melatonin sensitive. Further, the area-specific expression patterns suggest that the regulatory role of melatonin differs among different brain areas. Since subareas of well-defined neural circuits, such as the visual system or the song control system, are equipped with different receptor types, we hypothesize a diversity of functions for melatonin in the control of sensory integration and behavior.

scholarly journals Probing Cortical Sites of Antipsychotic Drug Action within vivoReceptor Imaging

2000 ◽  
Vol 12 (1-2) ◽  
pp. 3-9 ◽  
Author(s):  
P. Shaw ◽  
L. S. Pilowsky
Keyword(s):  
Antipsychotic Drug ◽  
Antipsychotic Drugs ◽  
Temporal Cortex ◽  
Direct Determination ◽  
Drug Action ◽  
Receptor Subtypes ◽  
Initial Finding ◽  
Main Site ◽  
Dopamine D2 ◽  
Sites Of Action

Imaging receptors using radioactive ligands has allowed direct determination of the sites of action of antipsychotic drugs. Initial studies relating antipsychotic drug efficacy to action at striatal dopamine D2-like receptors have recently been undermined. Developments in imaging extrastriatal dopamine D2-like receptors suggest rather that antagonism of these receptors in the temporal cortex is the common site of action for antipsychotic drugs, with occupancy at striatal receptors relating more closely to extrapyramidal side effects. Further work into dopamine receptor subtypes and other receptor groups such as serotonin and GABA neurotransmitters awaits the development of suitable probes, but there are some initial finding. Again a main site of antipsychotic drug action is at cortical levels with high degrees of cortical D1 and 5HT2areceptor occupancy attained particularly by atypical antipsychotic drugs.

The α1a and α1b-adrenergic receptor subtypes: molecular mechanisms of receptor activation and of drug action

2000 ◽  
Vol 74 (2-3) ◽  
pp. 173-179 ◽  
Author(s):  
Susanna Cotecchia ◽  
Olivier Rossier ◽  
Francesca Fanelli ◽  
Amedeo Leonardi ◽  
Pier G De Benedetti
Keyword(s):  
Adrenergic Receptor ◽  
Molecular Mechanisms ◽  
Receptor Activation ◽  
Drug Action ◽  
Receptor Subtypes

scholarly journals Targeted Disruption of the Mouse Mel1b Melatonin Receptor

2003 ◽  
Vol 23 (3) ◽  
pp. 1054-1060 ◽  
Author(s):  
Xiaowei Jin ◽  
Charlotte von Gall ◽  
Rick L. Pieschl ◽  
Valentin K. Gribkoff ◽  
Jorg H. Stehle ◽  
...  
Keyword(s):  
Functional Redundancy ◽  
Inhibitory Response ◽  
Receptor Subtype ◽  
Receptor Subtypes ◽  
Melatonin Receptor ◽  
Targeted Disruption ◽  
High Affinity ◽  
C3h Mice ◽  
Element Binding Protein ◽  
Residual Response

ABSTRACT Two high-affinity, G protein-coupled melatonin receptor subtypes have been identified in mammals. Targeted disruption of the Mel1a melatonin receptor prevents some, but not all, responses to the hormone, suggesting functional redundancy among receptor subtypes (Liu et al., Neuron 19:91-102, 1997). In the present work, the mouse Mel1b melatonin receptor cDNA was isolated and characterized, and the gene has been disrupted. The cDNA encodes a receptor with high affinity for melatonin and a pharmacological profile consistent with its assignment as encoding a melatonin receptor. Mice with targeted disruption of the Mel1b receptor have no obvious circadian phenotype. Melatonin suppressed multiunit electrical activity in the suprachiasmatic nucleus (SCN) in Mel1b receptor-deficient mice as effectively as in wild-type controls. The neuropeptide, pituitary adenylyl cyclase activating peptide, increases the level of phosphorylated cyclic AMP response element binding protein (CREB) in SCN slices, and melatonin reduces this effect. The Mel1a receptor subtype mediates this inhibitory response at moderate ligand concentrations (1 nM). A residual response apparent in Mel1a receptor-deficient C3H mice at higher melatonin concentrations (100 nM) is absent in Mel1a-Mel1b double-mutant mice, indicating that the Mel1b receptor mediates this effect of melatonin. These data indicate that there is a limited functional redundancy between the receptor subtypes in the SCN. Mice with targeted disruption of melatonin receptor subtypes will allow molecular dissection of other melatonin receptor-mediated responses.

Influence of moonlight on mRNA expression patterns of melatonin receptor subtypes in the pineal organ of a tropical fish

2014 ◽  
Vol 14 ◽  
pp. 67-70 ◽  
Author(s):  
Yong-Ju Park ◽  
Ji-Gweon Park ◽  
Yuki Takeuchi ◽  
Sung-Pyo Hur ◽  
Young-Don Lee ◽  
...  
Keyword(s):  
Mrna Expression ◽  
Pineal Organ ◽  
Expression Patterns ◽  
Tropical Fish ◽  
Receptor Subtypes ◽  
Melatonin Receptor
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