Nociceptive TRP Channels: Sensory Detectors and Transducers in Multiple Pain Pathologies
Abstract
:1. Introduction
2. Nociceptive TRP Channels
2.1. History, Identification and Cloning
2.2. Characterization of Channel Function: Activation by Diverse Physico-Chemical Stimuli
2.3. Similarities and Differences in Channel Expression and Localization
3. Modulation of Nociceptive TRP Channel Activity and Expression
4. Involvement of Nociceptive TRP Channels in Painful Pathologies
4.1. Inflammatory Pain
4.2. Neuropathic Pain
4.3. Visceral Pain
4.4. Pain Associated with Cancers and Other Pathological Conditions
4.4.1. Cancer Pain
4.4.2. Dental Pain
4.4.3. Migraine
5. Nociceptive TRP Channels in Non-Painful Pathologies and Physiological Processes
6. Concluding Remarks
Acknowledgments
Conflicts of Interest
References
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Agonist/Antagonist (Producer/Company) | Channel (Mode of Action) | Current Clinical Use/Trial Status | Specific Painful Pathology | References |
---|---|---|---|---|
AMG517 (Amgen) | TRPV1 (channel blocker) | Phase Ib/Phase II-terminated | Dental pain | [147,148,149,150] |
ABT102 (Abbott) | TRPV1 (channel blocker) | Phase I—completed; Phase II—unknown | Healthy volunteers | [148,149,150,151,152] |
GRC 6211 (Lilly/Glenmark) | TRPV1 (channel blocker) | Phase I-Phase II | Dental pain | [148,149,150] |
SB-705498 (GlaxoSmithKline) | TRPV1 (channel blocker) | Phase II—completed | Dental pain/Toothache | [149,150,153] |
Phase II—terminated | Rectal pain | [154] | ||
MK-2295 (Merck-Neurogen) | TRPV1 (channel blocker) | Phase II—completed | Postoperative dental pain | [149,150,155] |
AZD1386 (Astra-Zeneca) | TRPV1 (channel blocker) | Phase I—completed | Esophageal pain | [149,150,156,157] |
Phase II—completed | Dental pain | [149,158,159] | ||
Phase II—terminated | Osteoarthritis, knee pain | [149,150,160] | ||
Phase II—terminated | Neuropathic pain | [161] | ||
NEO06860 (Neomed Institute) | TRPV1 (blockade of channel activation by capsaicin, but not by heat and protons) | Phase I—completed Phase II—ongoing | Osteoarthritis, knee pain | [162,163] |
NGX 4010 (NeurogesX; Acorda Therapeutics/ Astellas Pharma) | TRPV1 (agonist; capsaicin transdermal patch) | Phase III—completed (launched for clinical use in PHN) | PHN-associated neuropathic pain | [164,165] |
Phase III—completed | HIV-associated neuropathic pain | [165,166,167] | ||
Resiniferatoxin (NIDCR-NIH) | TRPV1 (potent agonist) | Phase I—ongoing | Advanced cancer pain | [168,169,170] |
Zucapsaicin (Sanofi-Aventis; Winston Pharmaceuticals) | TRPV1 (agonist; nasal and topical capsaicin patch & cream) | Phase III—completed (launched for clinical use in osteoarthritis) | Osteoarthritis, knee pain | [171] |
Phase III—completed | Episodic cluster headache | [172] | ||
Phase II—completed | PHN-associated neuropathic pain | [173] | ||
GRC-17536 (Glenmark) | TRPA1 (channel locker) | Phase II—completed | Diabetic peripheral neuropathic pain | [174] |
SAR292833 (Sanofi) | TRPV3 (channel blocker) | Phase II—completed | Neuropathic pain | [175] |
PF-05PR105679 (Pfizer) | TRPM8 (channel blocker) | Phase I—completed | Healthy volunteers | [176,177] |
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Mickle, A.D.; Shepherd, A.J.; Mohapatra, D.P. Nociceptive TRP Channels: Sensory Detectors and Transducers in Multiple Pain Pathologies. Pharmaceuticals 2016, 9, 72. https://doi.org/10.3390/ph9040072
Mickle AD, Shepherd AJ, Mohapatra DP. Nociceptive TRP Channels: Sensory Detectors and Transducers in Multiple Pain Pathologies. Pharmaceuticals. 2016; 9(4):72. https://doi.org/10.3390/ph9040072
Chicago/Turabian StyleMickle, Aaron D., Andrew J. Shepherd, and Durga P. Mohapatra. 2016. "Nociceptive TRP Channels: Sensory Detectors and Transducers in Multiple Pain Pathologies" Pharmaceuticals 9, no. 4: 72. https://doi.org/10.3390/ph9040072