In pharmacokinetics and receptor–ligand kinetics the binding potential (BP) is a combined measure of the density of "available" neuroreceptors and the affinity of a drug to that neuroreceptor.

Description

Consider a ligand receptor binding system. Ligand with a concentration L associates with a receptor of concentration or availability R to form a ligand-receptor complex with concentration RL. The binding potential is then the ratio ligand-receptor complex to free ligand at equilibrium and in the limit of L tending to 0, and is given symbol BP:

This quantity, originally defined by Mintun, describes the capacity of a receptor to bind ligand. It is a limit (L << Ki) of the general receptor association equation:

and is thus also equivalent to:

These equations apply equally when measuring the total receptor density or the residual receptor density available after binding to second ligand - availability.

BP in Positron Emission Tomography

BP is a pivotal measure in the use of positron emission tomography (PET) to measure the density of "available" receptors, e.g. to assess the occupancy by drugs or to characterize neuropsychiatric diseases (yet, one should keep in mind that binding potential is a combined measure that depends on receptor density as well as on affinity). An overview of the related methodology is e.g. given in Laruelle et al. (2002)..

• : The "specific to nonspecific equilibrium partition coefficient. This is the ratio of specifically bound to nondisplaceable tracer in brain tissue at true equilibrium. It can be calculated without arterial blood sampling. In the two-tissue compartment model is the free fraction of the tracer in the first tissue compartment, i.e. a measure that depends on the nonspecific binding of the ligand in brain tissue

• includes measurements of radioactivity in plasma, including metabolite correction. From the two-tissue compartment model and by assuming there is only passive diffusion finally allows to obtain BP.

Definitions and Symbols

.

. In PET imaging, the amount of radioligand

: Transfer rate constants from the two tissue compartment model.

NEW NOTATIONAL CONVENTIONS: In Innis et al., a large group of researchers who are active in this field agreed to a consensus nomenclature for these terms, with the intent of making the literature in this field more transparent to non-specialists. The convention involves use of the subscripts p for quantities referred to plasma and ND for quantities referred to the free plus nonspecifically bound concentration in brain (NonDisplaceable). Under the consensus nomenclature, the parameters referred to above as f1 and BP1 are now called fp and BPp, while f2 and BP2 are called fND and BPND.

See also

• Volume of distribution

References