Heterocycle-based multicomponent reactions in drug discovery: from hit finding to rational design

P Nadal Rodríguez, O Ghashghaei, A Bagán… - Biomedicines, 2022 - mdpi.com
In the context of the structural complexity necessary for a molecule to selectively display a
therapeutical action and the requirements for suitable pharmacokinetics, a robust synthetic …

Disease‐modifying treatment with I2 imidazoline receptor ligand LSL60101 in an Alzheimer's disease mouse model: a comparative study with donepezil

F Vasilopoulou, S Rodríguez‐Arévalo… - British Journal of …, 2021 - Wiley Online Library
Background and Purpose The development of effective therapeutic strategies against
Alzheimer's disease (AD) remains a challenge. I2 imidazoline receptor ligands have a …

Visualizing reactive astrocytes: Positron emission tomography imaging ligands for imidazoline‐2 binding sites

W Li, Y Qiao, J Chen, Y Li, X Du, SH Liang, H Fu - View, 2023 - Wiley Online Library
Abstract Imidazoline‐2 binding sites (I2BS) exhibit specific expression in reactive astrocytes
of the brain and are implicated in various pathophysiological processes, including …

[HTML][HTML] Benzofuranyl-2-imidazoles as imidazoline I2 receptor ligands for Alzheimer's disease

S Rodriguez-Arevalo, A Bagan, C Grinan-Ferre… - European journal of …, 2021 - Elsevier
Recent findings unveil the pharmacological modulation of imidazoline I 2 receptors (I 2-IR)
as a novel strategy to face unmet medical neurodegenerative diseases. In this work, we …

I2-imidazoline ligand CR4056 improves memory, increases ApoE expression and reduces BBB leakage in 5xFAD mice

BC Mota, N Ashburner, L Abelleira-Hervas… - International Journal of …, 2022 - mdpi.com
Recent evidence suggests that I2-imidazoline ligands have neuroprotective properties in
animal models of neurodegeneration, such as Alzheimer's disease (AD). We recently …

Discovery of (3-Phenylcarbamoyl-3,4-dihydro-2H-pyrrol-2-yl)phosphonates as Imidazoline I2 Receptor Ligands with Anti-Alzheimer and Analgesic Properties

A Bagán, A López-Ruiz, S Abás… - Journal of Medicinal …, 2025 - ACS Publications
Imidazoline I 2 receptors (I2-IRs) are altered in Alzheimer's disease (AD) patients and are
associated with analgesia. I2-IRs are not structurally described, and their pharmacological …

I2 imidazoline receptor modulation protects aged SAMP8 mice against cognitive decline by suppressing the calcineurin pathway

F Vasilopoulou, C Grinan-Ferre, S Rodríguez-Arévalo… - GeroScience, 2021 - Springer
Brain aging and dementia are current problems that must be solved. The levels of
imidazoline 2 receptors (I 2-IRs) are increased in the brain in Alzheimer's disease (AD) and …

Agmatine reverses memory deficits induced by Aβ1–42 peptide in mice: A key role of imidazoline receptors

N Kotagale, M Dixit, H Garmelwar, S Bhondekar… - Pharmacology …, 2020 - Elsevier
Abstracts Agmatine is a biogenic amine synthesized following decarboxylation of L-arginine
by the enzyme arginine decarboxylase and exhibits favourable outcome in …

[HTML][HTML] Sex differences in the antidepressant-like response and molecular events induced by the imidazoline-2 receptor agonist CR4056 in rats

E Hernández-Hernández, S Ledesma-Corvi… - Pharmacology …, 2023 - Elsevier
In searching for novel targets to design antidepressants, among the characterized
imidazoline receptors (IR), I2 receptors are an innovative therapeutical approach since they …

Amelioration of BPSD-Like Phenotype and Cognitive Decline in SAMP8 Mice Model Accompanied by Molecular Changes after Treatment with I2-Imidazoline …

F Vasilopoulou, A Bagan, S Rodriguez-Arevalo… - Pharmaceutics, 2020 - mdpi.com
Behavioural and psychological symptoms of dementia (BPSD), including fear-anxiety-and
depressive-like behaviour, are present in Alzheimer's disease (AD), together with memory …