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Transient receptor potential channels - emerging novel drug targets for the treatment of pain.
Curr Med Chem. 2013; 20(11):1409-36.CM

Abstract

In mammals several members of the Transient Receptor Potential channel family (TRPs), expressed mainly in the sensory neurons and skin keratinocytes, are implicated in relevant physiological functions, including thermosensation,nociception and vision. Since the TRPV1-4, TRPA1 and TRPM8 channels from this family play a pivotal role in both the detection and possibly modulation of painful stimuli, they are regarded as a very promising target of novel analgesic drugs. A few agents acting at TRPs, such as capsaicin or menthol, have a long history of their application as analgesics,whereas others (e.g. SB705498, JTS653, JNJ17203212, AP18, A967079, Chembridge-5861528 or PBMC) are currently being evaluated both in animals and in humans. In this review we discuss pain physiology, as well as the pharmacological properties of the TRPs involved in pain detection as potential critical peripheral analgesic targets. We present one of the most relevant strategies in the search for novel analgesic drugs, namely the TRP channels and their ligands, both agonists and antagonists as potential novel therapeutics for inflammatory and neuropathic pain syndromes. The safety profile of these agents, in particular their impact on thermosensation, is also discussed below.

Authors+Show Affiliations

Department of Pharmacodynamics, Jagiellonian University, Medical College, Medyczna 9, 30-688 Cracow, Poland. salat.kinga@gmail.comNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

23409716

Citation

Sałat, Kinga, et al. "Transient Receptor Potential Channels - Emerging Novel Drug Targets for the Treatment of Pain." Current Medicinal Chemistry, vol. 20, no. 11, 2013, pp. 1409-36.
Sałat K, Moniczewski A, Librowski T. Transient receptor potential channels - emerging novel drug targets for the treatment of pain. Curr Med Chem. 2013;20(11):1409-36.
Sałat, K., Moniczewski, A., & Librowski, T. (2013). Transient receptor potential channels - emerging novel drug targets for the treatment of pain. Current Medicinal Chemistry, 20(11), 1409-36.
Sałat K, Moniczewski A, Librowski T. Transient Receptor Potential Channels - Emerging Novel Drug Targets for the Treatment of Pain. Curr Med Chem. 2013;20(11):1409-36. PubMed PMID: 23409716.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Transient receptor potential channels - emerging novel drug targets for the treatment of pain. AU - Sałat,Kinga, AU - Moniczewski,Andrzej, AU - Librowski,Tadeusz, PY - 2012/10/04/received PY - 2013/01/07/revised PY - 2013/01/26/accepted PY - 2013/2/16/entrez PY - 2013/2/16/pubmed PY - 2013/8/29/medline SP - 1409 EP - 36 JF - Current medicinal chemistry JO - Curr Med Chem VL - 20 IS - 11 N2 - In mammals several members of the Transient Receptor Potential channel family (TRPs), expressed mainly in the sensory neurons and skin keratinocytes, are implicated in relevant physiological functions, including thermosensation,nociception and vision. Since the TRPV1-4, TRPA1 and TRPM8 channels from this family play a pivotal role in both the detection and possibly modulation of painful stimuli, they are regarded as a very promising target of novel analgesic drugs. A few agents acting at TRPs, such as capsaicin or menthol, have a long history of their application as analgesics,whereas others (e.g. SB705498, JTS653, JNJ17203212, AP18, A967079, Chembridge-5861528 or PBMC) are currently being evaluated both in animals and in humans. In this review we discuss pain physiology, as well as the pharmacological properties of the TRPs involved in pain detection as potential critical peripheral analgesic targets. We present one of the most relevant strategies in the search for novel analgesic drugs, namely the TRP channels and their ligands, both agonists and antagonists as potential novel therapeutics for inflammatory and neuropathic pain syndromes. The safety profile of these agents, in particular their impact on thermosensation, is also discussed below. SN - 1875-533X UR - https://www.unboundmedicine.com/medline/citation/23409716/Transient_receptor_potential_channels___emerging_novel_drug_targets_for_the_treatment_of_pain_ L2 - https://www.eurekaselect.com/108054/article DB - PRIME DP - Unbound Medicine ER -