### 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 IC_{50} 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, [^{3}H]quinuclidinyl benzilate and [^{3}H]cis-methyldioxolane, and results consistent with the theoretical predictions were observed.

Original language | English (US) |
---|---|

Pages (from-to) | 367-371 |

Number of pages | 5 |

Journal | Molecular Pharmacology |

Volume | 19 |

Issue number | 3 |

State | Published - 1981 |

Externally published | Yes |

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### ASJC Scopus subject areas

- Pharmacology

### Cite this

*Molecular Pharmacology*,

*19*(3), 367-371.

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

Research output: Contribution to journal › Article

*Molecular Pharmacology*, vol. 19, no. 3, pp. 367-371.

}

TY - JOUR

T1 - Mathematical analysis of the kinetics of competitive inhibition in neurotransmitter receptor binding assays

AU - Ehlert, F. J.

AU - Roeske, W. R.

AU - Yamamura, H. I.

PY - 1981

Y1 - 1981

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=0019495090&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0019495090&partnerID=8YFLogxK

M3 - Article

C2 - 6267444

AN - SCOPUS:0019495090

VL - 19

SP - 367

EP - 371

JO - Molecular Pharmacology

JF - Molecular Pharmacology

SN - 0026-895X

IS - 3

ER -