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Abstract
<p class="first" id="d6938424e99">Transient receptor potential vanilloid 1 (TRPV1)
is an ion channel expressed on sensory
neurons triggering an influx of cations. TRPV1 receptors function as homotetramers
responsive to heat, proinflammatory substances, lipoxygenase products, resiniferatoxin,
endocannabinoids, protons, and peptide toxins. Its phosphorylation increases sensitivity
to both chemical and thermal stimuli, while desensitization involves a calcium-dependent
mechanism resulting in receptor dephosphorylation. TRPV1 functions as a sensor of
noxious stimuli and may represent a target to avoid pain and injury. TRPV1 activation
has been associated to chronic inflammatory pain and peripheral neuropathy. Its expression
is also detected in nonneuronal areas such as bladder, lungs, and cochlea where TRPV1
activation is responsible for pathology development of cystitis, asthma, and hearing
loss. This review offers a comprehensive overview about TRPV1 receptor in the pathophysiology
of chronic pain, epilepsy, cough, bladder disorders, diabetes, obesity, and hearing
loss, highlighting how drug development targeting this channel could have a clinical
therapeutic potential. Furthermore, it summarizes the advances of medicinal chemistry
research leading to the identification of highly selective TRPV1 antagonists and their
analysis of structure-activity relationships (SARs) focusing on new strategies to
target this channel.
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