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Structure of the BoNT/A1 – receptor complex

Toxicon, 2015
Botulinum neurotoxin A causes botulism but is also used for medical and cosmetic applications. A detailed molecular understanding of BoNT/A--host receptor interactions is therefore fundamental for improving current clinical applications and for developing new medical strategies targeting human disorders.
Roger M, Benoit   +6 more
openaire   +2 more sources

Adenosine A1 receptor antagonists and the kidney

Current Opinion in Nephrology and Hypertension, 2003
This review will examine the most recent evidence that adenosine receptors in the kidney can alter kidney function. Adenosine A(1)-receptors located in the afferent arteriole and proximal tubule can contribute to fluid retaining disorders by mediating tubuloglomerular feedback, afferent arteriole vasoconstriction or direct sodium absorption.
Paul S, Modlinger, William J, Welch
openaire   +2 more sources

Medicinal Chemistry of Adenosine A1 Receptor Ligands

Current Topics in Medicinal Chemistry, 2003
In this review the latest developments in ligand design for the adenosine A(1) receptor are summarized. Novel series of agonists and antagonists are discussed, leading to the conclusion that ligands truly selective for the human adenosine A(1) receptor are still scarce.
Willem, Soudijn   +2 more
openaire   +2 more sources

Binding of an adenosine A1 receptor agonist and adenosine A1 receptor antagonist to sheep pineal membranes

European Journal of Pharmacology, 1997
The pineal organ of vertebrates produces melatonin and adenosine. In lower vertebrates, adenosine modulates melatonin production. We report herein that 2-chloro-cyclopentyl-[3H]-adenosine ([3H]CCPA: adenosine A1 receptor agonist) and [3H]-cyclopentyl-1,3-dipropylxanthine ([3H]DPCPX: adenosine A1 receptor antagonist), bind specifically to sheep pineal ...
Falcon, J., Privat, K., Ravault, J.P.
openaire   +3 more sources

Repetitive stimulation of adenosine A1 receptors in vivo: Changes in receptor numbers, G-proteins and A1 receptor agonist-induced hypothermia

Brain Research, 2008
Adenosine is an important neuromodulator and neuroprotective molecule, which is produced in the brain as a function of neuronal activity, coupling energy expenditure to energy supply. Under conditions of increased need and reduced availability of energy, including hypoxia and prolonged wakefulness, there is an increase in adenosine turnover and ...
Roman, Viktor   +3 more
openaire   +3 more sources

Binding thermodynamics at A1 and A2a adenosine receptors

Life Sciences, 1996
Only recently the binding equilibrium of a number of ligands at adenosine A1 and A2a receptors has been analyzed from a thermodynamic point of view. This approach presents the advantage, with respect to usual affinity constant measurements, of a greater capability to give information about the molecular mechanisms underlying the binding process.
BOREA, Pier Andrea   +4 more
openaire   +3 more sources

Allosteric modulation of A1-adenosine receptor: a review

Drug Discovery Today: Technologies, 2013
Allosteric modulators of adenosine receptors represent an alternative to direct-acting adenosine agonists and nucleoside uptake blockers, preferably those can selectively modulate the response to adenosine in only those organs or localized areas of a given organ in which production of adenosine is increased.
M. Kimatrai Salvador   +2 more
openaire   +2 more sources

A1 Receptors Ligands: Past, Present and Future Trends

Current Topics in Medicinal Chemistry, 2010
Adenosine is a neuromodulator that interacting with four receptors, A(1), A(2A), A(2B) and A(3), is involved in the regulation of several biological functions in different organs and tissues, including the central nervous system, the cardiovascular system and the airways; many pathophysiological states are associated with changes of adenosine levels ...
SCHENONE, SILVIA   +4 more
openaire   +4 more sources

Desensitization of A1 Adenosine Receptors

1995
It is well known that exposure of sensitive cells to receptor agonists can cause a progressive reduction in their capacity to respond to this and related agonists. This phenomenon has been observed with cells expressing receptors from different superfamilies, and has been termed desensitization, refractoriness,tolerance, or tachyphylaxis [1].
Edmund Hoppe, Martin J. Lohse
openaire   +1 more source

Cellular localization of adenosine A1 receptors in rat forebrain: Immunohistochemical analysis using adenosine A1 receptor‐specific monoclonal antibody

The Journal of Comparative Neurology, 1999
Monoclonal antibodies were generated against the adenosine A1 receptor (A1R) purified from rat brain. In immunoblot analyses of purified or partially purified A1R preparations from rat brain, these antibodies recognized a solitary band, the size of which corresponded to that expected for A1R.
T, Ochiishi   +7 more
openaire   +2 more sources

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