Abstract
The Monod-Wyman-Changeux (MWC) cyclic model was described as a kinetic scheme to explain enzyme function and modulation more than 50 years ago and was proposed as a model for understanding activation of transmitter-gated channels soon afterwards. More recently the MWC model has been used to describe the activation of the GABAA receptor by the transmitter, GABA, and drugs that bind to separate sites on the receptor. It is most interesting that the MWC formalism can also describe the interactions among drugs which activate the receptor. In this review we describe properties of the MWC model that have been explored experimentally using the GABAA receptor, summarize analytical expressions for activation and interaction for drugs, and briefly review experimental results.
- The American Society for Pharmacology and Experimental Therapeutics