PMID- 25060242 OWN - NLM STAT- MEDLINE DCOM- 20150619 LR - 20150418 IS - 1464-410X (Electronic) IS - 1464-4096 (Linking) VI - 115 IP - 5 DP - 2015 May TI - Transient receptor potential channel modulators as pharmacological treatments for lower urinary tract symptoms (LUTS): myth or reality? PG - 686-97 LID - 10.1111/bju.12876 [doi] AB - Transient receptor potential (TRP) channels belong to the most intensely pursued drug targets of the last decade. These ion channels are considered promising targets for the treatment of pain, hypersensitivity disorders and lower urinary tract symptoms (LUTS). The aim of the present review is to discuss to what extent TRP channels have adhered to their promise as new pharmacological targets in the lower urinary tract (LUT) and to outline the challenges that lie ahead. TRP vanilloid 1 (TRPV1) agonists have proven their efficacy in the treatment of neurogenic detrusor overactivity (DO), albeit at the expense of prolonged adverse effects as pelvic 'burning' pain, sensory urgency and haematuria. TRPV1 antagonists have been very successful in preclinical studies to treat pain and DO. However, clinical trials with the first generation TRPV1 antagonists were terminated early due to hyperthermia, a serious, on-target, side-effect. TRP vanilloid 4 (TRPV4), TRP ankyrin 1 (TRPA1) and TRP melastatin 8 (TRPM8) have important sensory functions in the LUT. Antagonists of these channels have shown their potential in pre-clinical studies of LUT dysfunction and are awaiting clinical validation. CI - (c) 2014 The Authors. BJU International (c) 2014 BJU International. FAU - Deruyver, Yves AU - Deruyver Y AD - Laboratory of Experimental Urology, Department of Development and Regeneration, KU Leuven, Leuven, Belgium; University Hospitals Leuven, Leuven, Belgium; TRP Research Platform Leuven (TRPLe), Leuven, Belgium. FAU - Voets, Thomas AU - Voets T FAU - De Ridder, Dirk AU - De Ridder D FAU - Everaerts, Wouter AU - Everaerts W LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review DEP - 20150121 PL - England TA - BJU Int JT - BJU international JID - 100886721 RN - 0 (Transient Receptor Potential Channels) SB - IM CIN - BJU Int. 2015 May;115(5):676-7. PMID: 25885558 MH - Humans MH - Lower Urinary Tract Symptoms/*drug therapy MH - Transient Receptor Potential Channels/*agonists/*antagonists & inhibitors OTO - NOTNLM OT - LUTS OT - TRP channel OT - TRPV1 OT - TRPV4 OT - afferent nerve OT - detrusor overactivity OT - urothelium EDAT- 2014/07/26 06:00 MHDA- 2015/06/20 06:00 CRDT- 2014/07/26 06:00 PHST- 2014/07/26 06:00 [entrez] PHST- 2014/07/26 06:00 [pubmed] PHST- 2015/06/20 06:00 [medline] AID - 10.1111/bju.12876 [doi] PST - ppublish SO - BJU Int. 2015 May;115(5):686-97. doi: 10.1111/bju.12876. Epub 2015 Jan 21.