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The Isoleucine at Position 118 in Transmembrane 2 Is Responsible for the Selectivity of Xamoterol, Nebivolol, and ICI89406 for the Human β1-Adrenoceptor (2023)
Journal Article
Lim, V. J. Y., Proudman, R. G. W., Monteleone, S., Kolb, P., & Baker, J. G. (2023). The Isoleucine at Position 118 in Transmembrane 2 Is Responsible for the Selectivity of Xamoterol, Nebivolol, and ICI89406 for the Human β1-Adrenoceptor. Molecular Pharmacology, 103(2), 89-99. https://doi.org/10.1124/molpharm.122.000583

Known off-target interactions frequently cause predictable drug side-effects (e.g., β1-antagonists used for heart disease, risk β2-mediated bronchospasm). Computer-aided drug design would improve if the structural basis of existing drug selectivity w... Read More about The Isoleucine at Position 118 in Transmembrane 2 Is Responsible for the Selectivity of Xamoterol, Nebivolol, and ICI89406 for the Human β1-Adrenoceptor.

The signaling and selectivity of α-adrenoceptor agonists for the human α2A, α2B and α2C-adrenoceptors and comparison with human α1 and β-adrenoceptors (2022)
Journal Article
Proudman, R. G. W., Akinaga, J., & Baker, J. G. (2022). The signaling and selectivity of α-adrenoceptor agonists for the human α2A, α2B and α2C-adrenoceptors and comparison with human α1 and β-adrenoceptors. Pharmacology Research and Perspectives, 10(5), Article e01003. https://doi.org/10.1002/prp2.1003

α2-adrenoceptors, (α2A, α2B and α2C-subtypes), are Gi-coupled receptors. Central activation of brain α2A and α2C-adrenoceptors is the main site for α2-agonist mediated clinical responses in hypertension, ADHD, muscle spasm and ITU management of sedat... Read More about The signaling and selectivity of α-adrenoceptor agonists for the human α2A, α2B and α2C-adrenoceptors and comparison with human α1 and β-adrenoceptors.

The affinity and selectivity of α-adrenoceptor antagonists, antidepressants and antipsychotics for the human α2A, α2B, and α2C-adrenoceptors and comparison with human α1 and β-adrenoceptors (2022)
Journal Article
Proudman, R. G. W., Akinaga, J., & Baker, J. G. (2022). The affinity and selectivity of α-adrenoceptor antagonists, antidepressants and antipsychotics for the human α2A, α2B, and α2C-adrenoceptors and comparison with human α1 and β-adrenoceptors. Pharmacology Research and Perspectives, 10(2), Article e00936. https://doi.org/10.1002/prp2.936

α2-Adrenoceptors, subdivided into α2A, α2B, and α2C subtypes and expressed in heart, blood vessels, kidney, platelets and brain, are important for blood pressure, sedation, analgesia, and platelet aggregation. Brain α2C-adrenoceptor blockade has also... Read More about The affinity and selectivity of α-adrenoceptor antagonists, antidepressants and antipsychotics for the human α2A, α2B, and α2C-adrenoceptors and comparison with human α1 and β-adrenoceptors.

The selectivity of α‐adrenoceptor agonists for the human α1A, α1B, and α1D‐adrenoceptors (2021)
Journal Article
Proudman, R. G. W., & Baker, J. G. (2021). The selectivity of α‐adrenoceptor agonists for the human α1A, α1B, and α1D‐adrenoceptors. Pharmacology Research and Perspectives, 9(4), Article e00799. https://doi.org/10.1002/prp2.799

Highly selective drugs offer a way to minimize side-effects. For agonist ligands, this could be through highly selective affinity or highly selective efficacy, but this requires careful measurements of intrinsic efficacy. The α1-adrenoceptors are imp... Read More about The selectivity of α‐adrenoceptor agonists for the human α1A, α1B, and α1D‐adrenoceptors.