Rational design, synthesis, and pharmacological evaluation of a cohort of novel beta-adrenergic receptors ligands enables an assessment of structure-activity …

J Tricomi, L Landini, V Nieddu, U Cavallaro… - European Journal of …, 2023 - Elsevier
… Biomedical applications of molecules that are able to … Comparative analysis of their predicted
binding mode within … comprising this moiety (eg carazolol) displayed an almost planar …

Development of covalent antagonists for β1-and β2-adrenergic receptors

T Schwalbe, H Huebner, P Gmeiner - Bioorganic & Medicinal Chemistry, 2019 - Elsevier
… Aiming to apply these ligands in future structural and … 49 (B, receptor in light green and the
inverse agonist carazolol in grey). … analysis was performed by normalizing the receptor bound

Hybridization of β-adrenergic agonists and antagonists confers G protein bias

M Stanek, LP Picard, MF Schmidt… - Journal of medicinal …, 2019 - ACS Publications
Beta adrenergic receptors (β-AR) undoubtedly belong to the … , synthesis, and pharmacological
characterization of novel β-… 1) were compared to carazolol and those of our previously …

[HTML][HTML] A high-resolution description of β1-adrenergic receptor functional dynamics and allosteric coupling from backbone NMR

A Grahl, LA Abiko, S Isogai, T Sharpe… - Nature …, 2020 - nature.com
… To characterize the timescale of receptor motions, we … carazolol (PDB 2RH1). In contrast, in
the ternary complexes of agonist-… the beta-adrenergic receptors upon nanobody or G protein …

Photoswitchable Antagonists for a Precise Spatiotemporal Control of β2-Adrenoceptors

A Duran-Corbera, J Catena… - Journal of Medicinal …, 2020 - ACS Publications
… Results from the photochemical characterization of the … reported here through the application
of intercalated light cycles at … (A) Rigid docking of carazolol in the empty receptor serves …

Radiolabeled adrenergic and muscarinic blockers for in vivo studies

WC Eckelman - Receptor binding radiotracers, 2019 - taylorfrancis.com
… Only in the case of H-3 carazolol were we actually observing … by the analysis of compounds
that are highly protein bound. It … Snyder, SH, Beta adrenergic receptor labeling in intact ani…

Photoswitchable antagonists for a precise spatiotemporal control of ß 2-adrenoceptors

A Duran-Corbera, J Catena, M Otero Viñas, A Llebaria… - 2020 - dspace.uvic.cat
… Results from the photochemical characterization of the … applications that require spatiotemporal
activation of specific … the human β2-AR in complex with carazolol (PDB code 2RH1).This …

Bisoprolol-based 18F-PET tracer: Synthesis and preliminary in vivo validation of β1-blocker selectivity for β1-adrenergic receptors in the heart

J Kang, KN More, A Pyo, Y Jung, DY Kim… - Bioorganic & Medicinal …, 2021 - Elsevier
… with superior decay characteristics (t 1/2 … receptor in the heart and brain by (±)-bisoprolol
leads to faster excretion of labelled (±)-[ 18 F]bisoprolol due to unavailability of receptor binding

Adrenergic receptors in breast cancer

CP Piñero, EM Rivero, L Gargiulo… - Progress in Molecular …, 2022 - Elsevier
bound to a diffusible ligand was β2AR, crystallized bound to a high-affinity inverse agonist,
carazolol, in lipid bicelles bound to … We next described and characterized the α2AR in several …

[PDF][PDF] Characterisation of the α1B-adrenoceptor by modeling, dynamics and virtual screening

K Jain - 2019 - core.ac.uk
… 68 Figure 1-17 Molecular dynamics simulations of inverse agonist (carazolol) and … Beta
adrenergic receptor δ-OR … The availability of multistate structural data facilitates the application of …