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A Quantitative Analysis of Beta-Adrenergic Receptor Interactions: Resolution of High and Low Affinity States of the Receptor by Computer Modeling of Ligand Binding Data
Abstract
The properties of ligand binding to the beta-adrenergic receptor have been studied using a computer modeling technique to analyze data obtained by indirect binding methods. Antagonists are shown to bind to the receptor with one homogeneous state of uniform affinity, while agonists manifest heterogeneous binding. For agonists, two distinct binding states are apparent; one of high and one of low affinity. Affinity states of the receptor are characterized by specific macroscopic dissociation constants, and the proportion of total receptors in each state can be determined. The ability of an agonist to activate adenylate cyclase (intrinsic activity) correlates closely with the amount of high affinity state formed in the presence of the agonist (p
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Cited by
Operational models of pharmacological agonism
Black, J. W., & Leff, P. (1983) · Proceedings of the Royal Society of London. Series B. Biological Sciences · doi:10.1098/rspb.1983.0093 · Cited by 951
Raval, N. R., Johansen, A., Donovan, L. L., Ros, N. F., Ozenne, B., Hansen, H. D., & Knudsen, G. M. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22020835 · Cited by 200
Park, P. S.-H., Lodowski, D. T., & Palczewski, K. (2008) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.48.113006.094630 · Cited by 131
Finnema, S. J., Stepanov, V., Ettrup, A., Nakao, R., Amini, N., Svedberg, M., Lehmann, C., Hansen, M., Knudsen, G. M., & Halldin, C. (2014) · NeuroImage · doi:10.1016/j.neuroimage.2013.08.035 · Cited by 72
Gurguis, G. N. M., Andrews, R., Antai-Otong, D., Vo, S. P., Blakeley, J. E., Orsulak, P. J., & Rush, A. J. (1999) · Psychopharmacology · doi:10.1007/s002130050928 · Cited by 24
Metadata
- Authors
- KENT, R. S., DE LEAN, A., & LEFKOWITZ, R. J.
- Venue
- Molecular Pharmacology
- Publisher
- Elsevier BV
- Published
- 1980-01
- Volume
- 17
- Issue
- 1
- Pages
- 14-23
- ISSN
- 0026-895X (ISSN-L)
- OpenAlex
- W2186676367
- Cited by
- 553
- References
- 0
- FWCI
- 24.40
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: A Quantitative Analysis of Beta-Adrenergic Receptor Interactions: Resolution of High and Low Affinity States of the Receptor by Computer Modeling of Ligand Binding Data. https://app.cochat.ai/papers/10.1016/s0026-895x(25)14062-5
- The paper
- KENT, R. S., DE LEAN, A., & LEFKOWITZ, R. J. (1980). A Quantitative Analysis of Beta-Adrenergic Receptor Interactions: Resolution of High and Low Affinity States of the Receptor by Computer Modeling of Ligand Binding Data. Molecular Pharmacology. https://doi.org/10.1016/s0026-895x(25)14062-5
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
