P Bousquet’s research while affiliated with University of Strasbourg and other places

... Perhaps the most likely of these to be involved is the AIRP antiserum detected 43-kDa imidazoline receptor candidate from human RVLM ( Greney et al., 1994) since it has been put forward as a prime candidate for I 1 imidazo line receptors ( Vonthron et al., 1998). It is known to inhibit 3 H-clonidine labeled imidazoline binding sites ( Dontenwill et al., 1999). ...

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Contribution of imidazoline receptors and α2-adrenoceptors in the rostral ventrolateral medulla to sympathetic baroreflex inhibition by systemic rilmenidine

... In this context, centrally acting antihypertensive drugs, which modulate central sympathetic activity, may be attractive drugs for MS treatment by modulating sympathetic overactivity directly in the central nervous system [25]. This pharmacological group that is represented by clonidine and related compounds with high affinity for a 2 Rs and/or I 1 Rs has potent antihypertensive effects by reducing sympatho-excitatory inputs in the brainstem by activating a 2 Rs in particular within the RVLM [10]. The second generation of centrally acting antihypertensive drugs including rilmenidine and moxonidine, which have higher selectivity for I 1 Rs, is characterized by reduced central side effects such as dizziness and daytime sedation [10,53]. ...

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Central Sympathetic Modulation Reverses Microvascular Alterations in a Rat Model of High-Fat Diet-Induced Metabolic Syndrome

... Određivanje afiniteta vezivanja liganda za I 1 -IR je vršeno primenom metode kompetitivne inhibicije vezivanja radioliganda, kao što su [ [25][26][27][28], na plazma membranama ćelija centralnog dela nadbubrežne žlezde (chromaffin cells) [21,22,29], na plazma membranama ćelija neuroendokrinog tumora chromaffin ćelija (rat pheochromocytoma cells (PC 12)) [23,24,[30][31][32][33], plazma membranama humanih trombocita [34] i plazma membranama ćelija prostate psa [35]. ...

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Imidazoline receptors ligands

... This suggests that losartan had an effect on free fatty acid levels. Previous studies have shown increases in free fatty acids as a result of losartan treatment (Fellmann et al., 2009). ...

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Effect of Combined Drug Therapy and Genetic Modifiers on Hepatosteatosis and Fibrosis in a Mouse Model for Alström Syndrome

... [13][14][15] The nonadrenergic component of the central hypotension induced by imidazoline-like drugs was afterward attributed to their ability to act at specific binding sites, insensitive to catecholamines, called imidazoline binding sites (IBS) and located in the NRL/RVLM region. 16,17 Because relevant animal models and ligands selective for these nonadrenergic sites over ␣ 2 ARs were lacking, it was impossible to clarify how (in the case that these 2 mechanisms should work together) they might affect BP regulation and also how they might account for the overall hypotensive action of imidazoline-like drugs. It may be interesting to note that after central injection, the onset of the hypotensive effect of these drugs is much faster than that of ␣-MNA. ...

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Evidence for Synergy Between alpha2-Adrenergic and Nonadrenergic Mechanisms in Central Blood Pressure Regulation

... Until today three subtypes of imidazoline receptors, I1-IR, I2-IR, and I3-IR, were experimentally characterized (6,7). The I1-IRs were defined as one of the binding sites involved in the control of blood pressure (8). The I1-IRs have high affinity for clonidine, moxonidine, and rilmenidine, while the I2-IRs has high affinity for idazoxan and its analogues (9,10). ...

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Partial Least Square and Hierarchical Clustering in ADMET Modeling: Prediction of Blood – Brain Barrier Permeation of α-Adrenergic and Imidazoline Receptor Ligands

... On this basis, a possible role of I 1 -R in pain modulation can be theoretically suggested although so far unexplored. In the present work we studied the effects of I 1 -R modulation against oxaliplatin-induced neuropathic pain by using the selective I 1 -R agonist compound 2 (in this paper named carbophenyline, highly selective over I 2 , α 2 , and 5-HT 1A receptors [30,31]) (Fig. 1). Its effects on pain threshold were evaluated after single or repeated administrations in the absence or presence of the I 1 -R antagonist 3 [2-(1-methyl-2phenylethyl)-4,5-dihydro-1H-imidazole] (Fig. 1) [32], highly selective over I 2 , α 2 and 5-HT 1A receptor and the well-known I 1 /α 2 receptor antagonist efaroxan [33] which proved to be selective over several other biological targets [33; https:// pubchem.ncbi.nlm.nih.gov/compound/Efaroxan#section= ...

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The Use of the Selective Imidazoline I1 Receptor Agonist Carbophenyline as a Strategy for Neuropathic Pain Relief: Preclinical Evaluation in a Mouse Model of Oxaliplatin-Induced Neurotoxicity

... ; https://doi.org/10.1101/2021.09.29.462492 doi: bioRxiv preprint optical process that two photons are combined to form a new photon with twice the energy, which efficiently occurs in noncentrosymmetric molecules such as the collagen in biological tissue enabling a visualization of collagen without additional labeling(Mostaco-Guidolin, Rosin et al., 2017, Zipfel, Williams et al., 2003. A label-free SHG imaging have been widely used to monitor the fibrillar collagen in specimens of various fibrotic diseases in skin (Chen, Chen et al., 2009), liver (Goh, Leow et al., 2019), lung (Kottmann, Sharp et al., 2015), carotid artery (Megens, oude Egbrink et al., 2008), eye (Tan, Sun et al., 2007), tendon and ligaments (Doras, Taupier et al., 2011). In brain tissue, SHG imaging was used to investigate the structure and polarity of microtubules in neuronal processes (Dombeck, Kasischke et al., 2003, Van Steenbergen, Boesmans et al., 2019, and collagen deposition in glioblastoma (Jiang, Wang et al., 2017). ...

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Intravital imaging of cerebral microinfarct reveals an astrocyte reaction led to glial scar

... Clonidine activates the postsynaptic alpha2-adrenergic receptors of the vasomotor centers, reduces conduction of sympathetic impulses to the heart and blood vessels, which leads to a decrease in cardiac output, heart rate and peripheral vascular resistance. Clonidine penetrates the blood brain barrier and affects the reticular formation, which is manifested by the sedative effect of the drug (Bousquet et al. 1992). Serious or mild overdose of naphazoline induces a similar mechanism of action, stimulating the same receptors as clonidine, and causes a similar effect. ...

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Pathogenetic features of acute naphazoline poisoning in children

... These authors provided evidence that in hypertensive subjects, administration of betablockers potentiates daily life baroreceptor control of HR and that this occurs uniformly throughout the different behavioral conditions. A special mention can be made of the specific imidazoline sensitive binding sites insensitive to catecholamines, which are present in the nucleus reticularis lateralis [70]. The main effect of acute dosing of 1 mg of rilmenidine was a reduction of blood pressure and HR variability in the standing position [71]. ...

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Sympathetic control of short-term heart rate variability and its pharmacological modulation