Recent progress in the development of selective TRPV1 antagonists for pain.
As last year marked the tenth anniversary of the cloning of TRPV1, no attenuation has been observed in the intense interest surrounding this ion channel by both academic labs and pharmaceutical companies alike. Patent searches provide an extensive list of novel TRPV1 antagonists generated within the last 7 years, while literature searches reveal a diverse collection of TRPV1 antagonists that have progressed into pre-clinical in vivo profiling and even clinical development. This review serves to summarize the current knowledge of TRPV1 and TRPV1 antagonists as pain therapeutics and to highlight how use of divergent TRPV1 antagonists is helping to further define the physiological and pathological role of TRPV1 and the scope for TRPV1 antagonist therapies.
Broad
Lisa M
LM
Eli Lilly and Company, Lilly Research Centre, Erl Wood Manor, Sunninghill Road, Windlesham, Surrey, GU20 6PH, UK.
Keding
Stacy J
SJ
Blanco
Maria-Jesus
MJ
D000818:Animals; D006801:Humans; D010146:Pain / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism
D050916:TRPV Cation Channels; C494482:TRPV1 protein, human