Unit

UNIT 1.5 Characterization of Adrenoceptors

  1. David B. Bylund

Published Online: 1 MAR 2007

DOI: 10.1002/0471141755.ph0105s36

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

Bylund, D. B. 2007. Characterization of Adrenoceptors. Current Protocols in Pharmacology. 36:1.5:1.5.1–1.5.18.

Author Information

  1. University of Nebraska Medical Center, Omaha, Nebraska

Publication History

  1. Published Online: 1 MAR 2007
  2. Published Print: MAR 2007

Abstract

Norepinephrine and epinephrine are important neurotransmitters in both the peripheral and the central nervous systems. The actions of these neurotransmitters are mediated by adrenoceptors. Three major types of adrenoceptors have been identified on the basis of pharmacological data: α1, α2, and β. Within each major type, at least three receptor subtypes have been identified. Three basic types of radioligand binding experiments are provided in this unit: (1) saturation binding from which the affinity (Kd) of the radioligand for the adrenoceptor and the binding site density (Bmax) can be determined; (2) inhibition experiments from which the affinity (Ki) of a competing, unlabeled compound for the receptor can be determined; and (3) kinetic assays from which the forward and reverse rate constants of the binding process can be determined. Three support protocols are provided covering the preparation of membranes containing the receptor from tissue or cells in culture, calculation of Kd and Bmax from saturation experiments, and calculation of Ki from inhibition experiments.

Keywords:

  • receptor binding;
  • epinephrine;
  • norepinephrine;
  • neurotransmitter;
  • adrenoceptor;
  • adrenergic receptor