Allosteric modulation of G protein-coupled receptors.

Allosteric modulation of G protein-coupled receptors is a relatively novel and unexplored pharmacological concept that may lead to more selective and more 'natural' drugs for these receptors. In particular, allosteric enhancers may serve as tools to intensify selectively a weakened hormone or neurotransmitter signal caused by a localized deficit, such as in Alzheimer's or Parkinson's disease. In this paper, attention is paid to the adenosine A1 receptor, for which novel allosteric enhancers were synthesized and characterized that proved superior to the prototypic allosteric enhancer PD 81,723.