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Receptor theories and quantitative effect versus dose-concentration relationship.

Drug Metabolism Reviews

|January 1, 1984

Summary

The dissociation constant (K) differs from D50 in both in vivo and in vitro studies. Pharmacologic methods accurately determine K, enabling receptor subtype discrimination and understanding stimulus-response relationships for drug development.

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Area of Science:

Pharmacology
Biophysics
Drug Discovery

Background:

The dissociation constant (K) is a critical parameter in understanding drug-receptor interactions.
Accurate determination of K is essential for characterizing receptor subtypes and predicting drug efficacy.
Existing methods for determining K have limitations, necessitating refined approaches.

Purpose of the Study:

To investigate the relationship between dissociation constant (K) and D50 in various experimental settings.
To evaluate the reliability of Schild plots and pharmacologic methods for determining K.
To explore novel methods for precise K determination and receptor characterization.

Main Methods:

In vivo and in vitro experiments were conducted using morphine and vasoconstrictors.
Schild plot analysis was employed, with a focus on regression line constraints.
Perturbation of drug-receptor equilibrium and radiolabeled binding assays were utilized.

Main Results:

Dissociation constant (K) was found to be unequal to D50 in both in vivo and in vitro conditions.
Constraining Schild plot regression lines to a slope of -1 is crucial for accurate pA2 and -log KB determination.
Pharmacologic methods provide K values that can discriminate among receptor subtypes.

Conclusions:

Accurate K determination is vital for understanding stimulus-response relationships, a drug-independent property of effector systems.
While radiolabeled binding is precise for K determination, pharmacologic correlation is needed to confirm true receptor identification.
Pharmacologic methods remain indispensable for characterizing receptor subtypes and drug interactions.

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