Medicinal Chemistry Reviews

Volume 52, Chapter 23

Structure-Activity Relationship (SAR) Studies of Transient Receptor Potential (TRP) Channel Modulators

Christina M. LeGay and Darren J. Derksen

1.          Introduction                                                                                                               443

2.         TRP Channel Structural Features and Gating                                                          444

            2.1        General TRP Architecture                                                                              444

            2.2       Specific Features of TRPV1, TRPA1, and TRPM8                                         445

            2.3       TRP Channel Gating                                                                                      447

            2.4       Ligand Binding Domains of TRPV1, TRPA1, and TRPM8                           447

3.         Modulators of TRPV1, TRPA1, and TRPM8                                                              449

            3.1        Physiological Impacts of Modulating TRPV1, TRPA1, and TRPM8            449

            3.2       Nonselective Natural TRP Channel Modulators                                         450

            3.3       Nonselective Synthetic Modulators                                                            453

            3.4       Selective Synthetic Modulators                                                                   454

4.         Conclusion                                                                                                                 460

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