Abstract
The biophysical chemistry of ligand-receptor interactions imposes some restrictions on the characteristics of a radioligand if it is to be a useful tracer for accurately measuring the in vivo concentration of a specific cellular membrane receptor. This review discusses thermodynamic and kinetic rate constant considerations in selecting a ligand for radiolabeling and imaging. When radioligands of only modest specific activity are injected, one is able to use kinetic analysis to calculate the rate constant for the bimolecular binding reaction as well as the receptor concentration. Images of regional receptor density can be constructed from analysis of emission imaging data when the binding occurs at a rate that is slower than the collision frequency. A tracer that reacts with each collision cannot distinguish receptor density from blood flow. The theory of diffusion-limited reactions is reviewed and individual ligand-receptor examples are presented to demonstrate conditions where, even for very fast forward reactions, the binding of radioligand to receptor is controlled by local biochemistry rather than by the purely physical process of diffusion.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 477-483 |
| Number of pages | 7 |
| Journal | Nuclear Medicine and Biology |
| Volume | 28 |
| Issue number | 5 |
| DOIs | |
| State | Published - 2001 |
| Externally published | Yes |
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Keywords
- β-adrenergic ligands
- Diffusion
- Epidermal growth factor
- Kinetic modeling
- Ligand-receptor thermodynamics
- Superoxide dismutase
ASJC Scopus subject areas
- Cancer Research
- Molecular Medicine
- Radiology Nuclear Medicine and imaging
Cite this
The physical chemistry of ligand-receptor binding identifies some limitations to the analysis of receptor images. / Krohn, Kenneth.
In: Nuclear Medicine and Biology, Vol. 28, No. 5, 2001, p. 477-483.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - The physical chemistry of ligand-receptor binding identifies some limitations to the analysis of receptor images
AU - Krohn, Kenneth
PY - 2001
Y1 - 2001
N2 - The biophysical chemistry of ligand-receptor interactions imposes some restrictions on the characteristics of a radioligand if it is to be a useful tracer for accurately measuring the in vivo concentration of a specific cellular membrane receptor. This review discusses thermodynamic and kinetic rate constant considerations in selecting a ligand for radiolabeling and imaging. When radioligands of only modest specific activity are injected, one is able to use kinetic analysis to calculate the rate constant for the bimolecular binding reaction as well as the receptor concentration. Images of regional receptor density can be constructed from analysis of emission imaging data when the binding occurs at a rate that is slower than the collision frequency. A tracer that reacts with each collision cannot distinguish receptor density from blood flow. The theory of diffusion-limited reactions is reviewed and individual ligand-receptor examples are presented to demonstrate conditions where, even for very fast forward reactions, the binding of radioligand to receptor is controlled by local biochemistry rather than by the purely physical process of diffusion.
AB - The biophysical chemistry of ligand-receptor interactions imposes some restrictions on the characteristics of a radioligand if it is to be a useful tracer for accurately measuring the in vivo concentration of a specific cellular membrane receptor. This review discusses thermodynamic and kinetic rate constant considerations in selecting a ligand for radiolabeling and imaging. When radioligands of only modest specific activity are injected, one is able to use kinetic analysis to calculate the rate constant for the bimolecular binding reaction as well as the receptor concentration. Images of regional receptor density can be constructed from analysis of emission imaging data when the binding occurs at a rate that is slower than the collision frequency. A tracer that reacts with each collision cannot distinguish receptor density from blood flow. The theory of diffusion-limited reactions is reviewed and individual ligand-receptor examples are presented to demonstrate conditions where, even for very fast forward reactions, the binding of radioligand to receptor is controlled by local biochemistry rather than by the purely physical process of diffusion.
KW - β-adrenergic ligands
KW - Diffusion
KW - Epidermal growth factor
KW - Kinetic modeling
KW - Ligand-receptor thermodynamics
KW - Superoxide dismutase
UR - http://www.scopus.com/inward/record.url?scp=0034974627&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0034974627&partnerID=8YFLogxK
U2 - 10.1016/S0969-8051(01)00216-5
DO - 10.1016/S0969-8051(01)00216-5
M3 - Article
C2 - 11516691
AN - SCOPUS:0034974627
VL - 28
SP - 477
EP - 483
JO - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
JF - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
SN - 0969-8051
IS - 5
ER -