Abstract
New modalities providing safe and effective treatment of pain, especially prolonged pathological pain, have not appeared despite much effort. In this mini-review/overview we suggest that new paradigms of drug design are required to counter the underlying changes that occur in the nervous system that may elicit chronic pain states. We illustrate this approach with the example of designing, in a single ligand, molecules that have agonist activity at μ and δ opioid receptors and antagonist activities at cholecystokinin (CCK) receptors. Our findings thus far provide evidence in support of this new approach to drug design. We also report on a new biophysical method, plasmon waveguide resonance (PWR) spectroscopy, which can provide new insights into information transduction in G-protein coupled receptors (GPCRs) as illustrated by the δ opioid receptor.
Original language | English (US) |
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Article number | 53 |
Pages (from-to) | E450-E460 |
Journal | AAPS Journal |
Volume | 8 |
Issue number | 3 |
DOIs | |
State | Published - Jul 14 2006 |
Keywords
- Bifunctional ligands
- Cholecyctokinin receptors
- Drug design
- GPCRs
- Neuropathic pain
- Opioid receptors
- Plasmon waveguide resonance spectroscopy
ASJC Scopus subject areas
- Pharmaceutical Science