Distribution of 2-[125I]iodomelatonin binding sites in the brain of the pied flycatcher (Ficedula hypoleuca) and the zebra finch (Taeniopygia guttata)

1995 ◽  
Vol 198 (9) ◽  
pp. 1943-1949
Author(s):  
T Schneider

Using in vitro autoradiography, the distribution of 2-[125I]iodomelatonin (IMEL) binding sites in the brain of the pied flycatcher and the zebra finch was examined. The results show IMEL binding in retinofugal, tectofugal and thalamofugal brain areas of the visual system. Additionally, IMEL binding sites were detected in the ectostriatum, the thalamus, the mesencephalon and the limbic system. No IMEL binding could be demonstrated in the pineal gland, the hippocampus, the nucleus suprachiasmaticus, the visual wulst or the pituitary.

1989 ◽  
Vol 256 (4) ◽  
pp. R858-R866 ◽  
Author(s):  
C. Koseki ◽  
M. Imai ◽  
Y. Hirata ◽  
M. Yanagisawa ◽  
T. Masaki

Endothelin (ET) is a potent and long-acting vasoconstrictor peptide consisting of 21 amino acids and recently isolated from a medium of cultured porcine endothelial cells. To determine the possible sites of ET action, we have conducted autoradiography and receptor binding assays with 125I-labeled ET in rat tissues. The displaceable binding sites of the ligand were widely distributed, not only in the arteries and heart but also in various other organs, e.g., brain, kidney, lung, adrenal gland, and intestine. The systemically injected ET did not cross the blood-brain barrier, whereas the ligand, applied in vitro, was mainly located in the hypothalamic and thalamic areas, lateral ventricular region, subfornical organ, globus pallidus, and caudate putamen. Both membrane preparations from the brain stem including diencephalon and from the heart ventricle had similar, specific, and high-affinity binding sites for 125I-ET. We suggest that ET is involved in the regulation of a large variety of organ functions and may also act as a neuropeptide.


Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1532
Author(s):  
Víctor Fernández-Dueñas ◽  
Mingcheng Qian ◽  
Josep Argerich ◽  
Carolina Amaral ◽  
Martijn D.P. Risseeuw ◽  
...  

In recent years, new drug discovery approaches based on novel pharmacological concepts have emerged. Allosteric modulators, for example, target receptors at sites other than the orthosteric binding sites and can modulate agonist-mediated activation. Interestingly, allosteric regulation may allow a fine-tuned regulation of unbalanced neurotransmitter’ systems, thus providing safe and effective treatments for a number of central nervous system diseases. The metabotropic glutamate type 5 receptor (mGlu5R) has been shown to possess a druggable allosteric binding domain. Accordingly, novel allosteric ligands are being explored in order to finely regulate glutamate neurotransmission, especially in the brain. However, before testing the activity of these new ligands in the clinic or even in animal disease models, it is common to characterize their ability to bind mGlu5Rs in vitro. Here, we have developed a new series of fluorescent ligands that, when used in a new NanoBRET-based binding assay, will facilitate screening for novel mGlu5R allosteric modulators.


1991 ◽  
Vol 133 (1) ◽  
pp. 68-72 ◽  
Author(s):  
Bojidar Stankov ◽  
Bruno Cozzi ◽  
Valeria Lucini ◽  
Simona Capsoni ◽  
Jan Fauteck ◽  
...  

2016 ◽  
Vol 524 (18) ◽  
pp. 3747-3773 ◽  
Author(s):  
Cristian Gutierrez-Ibanez ◽  
Andrew N. Iwaniuk ◽  
Megan Jensen ◽  
David J. Graham ◽  
Ákos Pogány ◽  
...  

1989 ◽  
Vol 123 (2) ◽  
pp. 205-211 ◽  
Author(s):  
L. M. E. Finocchiaro ◽  
A. Scheucher ◽  
S. Finkielman ◽  
V. E. Nahmod ◽  
C. J. Pirola

ABSTRACT [3H]Quinuclidinyl benzylate ([3H]QNB)-binding sites, showing similar properties to cholinergic muscarinic receptors in other tissues, were disclosed in the rat pineal gland. Functionality of these receptors was demonstrated, as in-vitro muscarinic activation by pilocarpine increased the pineal metabolic production of the hydroxyindole derivatives 5-hydroxytryptophan and serotonin, with a slight effect on melatonin biosynthesis. Electric-field stimulation of pineal slices caused similar metabolic effects. These effects were inhibited by muscarinic blockade with atropine and enhanced by neostigmine inactivation of acetylcholinesterase. These results suggest that acetyl-choline is the neurotransmitter involved. Cholinergic activity may, therefore, regulate indole metabolism in the pineal gland. Journal of Endocrinology (1989) 123, 205–211


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