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Coupling of I(1) imidazoline receptors to the cAMP pathway: studies with a highly selective ligand, benazoline.
TLDR
It is demonstrated that alpha(2)R and I(1)R are definitely different entities because they are expressed independently in different cell lines, and both are both implicated in the cAMP pathway in cells (one is sensitive to pertussis toxin and the other is not).
Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.
The alpha- and beta-methyl derivatives of 2-phenylethylimidazoline (compounds 7 and 8) and the corresponding enantiomers were prepared and tested with the purpose of studying the role played by the
Structure-activity relationships in 1,4-benzodioxan-related compounds. 8.(1) {2-[2-(4-chlorobenzyloxy)phenoxy]ethyl}-[2-(2,6-dimethoxyphenoxy)ethyl]amine (clopenphendioxan) as a tool to highlight the
TLDR
This study highlighted for the first time alpha1D- and alpha1B-AR expression in PC3 cells and also demonstrated the involvement of these subtypes in the modulation of apoptosis and cell proliferation.
Age-related changes in the density of muscarinic cholinergic M1 and M2 receptor subtypes in pyramidal neurons of the rat hippocampus.
TLDR
The findings suggest that the reduction of muscarinic M1 sites noticed between rats of 2- and 12-months of age using radioligand binding techniques is probably dependent on the loss of hippocampal neurons rather than on the reduced receptor density per neuron.
alpha 2-adrenoreceptors profile modulation. 2. Biphenyline analogues as tools for selective activation of the alpha 2C-subtype.
TLDR
Homology modeling and docking studies support experimental data and highlight the crucial role for the hydrogen bond between the pyridine nitrogen in position 3 of 5 and the NH-indole ring of Trp6.48, which is favorably oriented in the alpha(2C)-subtype, only.
α2C-adrenoceptor modulators: a patent review
TLDR
The main results obtained suggest that α2C-AR stimulation may represent a therapeutic strategy to get an analgesic response with reduced sedative effects and undesirable changes in blood pressure due to α2A-AR activation.
Antagonism/Agonism modulation to build novel antihypertensives selectively triggering i1-imidazoline receptor activation.
TLDR
Inspired by the antihypertensive behavior of the selective I1-agonist 4, the designs, prepared, and studied the novel analogues 5-9 confirmed the stereospecific nature of the I1 proteins.
Pharmacophore development and 3D-QSAR study of I1 imidazoline binding site ligands
TLDR
Congruent and significant cross-validated 2D and 3D correlations indicated that electrostatic and steric interactions differently modulate the binding affinities at I 1 /I 2 IBS.
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