Mathematical analysis of the kinetics of competitive inhibition in neurotransmitter receptor binding assays

F. J. Ehlert, W. R. Roeske, H. I. Yamamura

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

The kinetics of competitive inhibition was described by first-order differential equations, and the solution to these equations was derived numerically. The results of this analysis showed that the IC50 of a competitive inhibition curve decreases as equilibrium is approached if the dissociation rate constant of the nonlabeled ligand is equal to or less than that of the labeled ligand. The converse was true for competitive inhibition curves of a nonlabeled inhibitor with a dissociation rate constant greater than that of the labeled ligand. Nonequilibrium competitive inhibition experiments were performed using the muscarinic antagonist and agonist ligands, [3H]quinuclidinyl benzilate and [3H]cis-methyldioxolane, and results consistent with the theoretical predictions were observed.

Original languageEnglish (US)
Pages (from-to)367-371
Number of pages5
JournalMolecular Pharmacology
Volume19
Issue number3
StatePublished - 1981
Externally publishedYes

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Neurotransmitter Receptor
Ligands
Quinuclidinyl Benzilate
Muscarinic Agonists
Muscarinic Antagonists
Inhibitory Concentration 50

ASJC Scopus subject areas

  • Pharmacology

Cite this

Mathematical analysis of the kinetics of competitive inhibition in neurotransmitter receptor binding assays. / Ehlert, F. J.; Roeske, W. R.; Yamamura, H. I.

In: Molecular Pharmacology, Vol. 19, No. 3, 1981, p. 367-371.

Research output: Contribution to journalArticle

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