Objective—To examine the effect of Ca 2ϩ store depletion on the translocation of vanilloid transient receptor potential (TRPV) 4-C1 heteromeric channels to the plasma membrane. Methods and Results—Vesicular trafficking is a key mechanism for controlling the surface expression of TRP channels in the plasma membrane, where they perform their function. TRP channels in vivo are often composed of he...

The purpose of this study was to determine if heat inhibits α2-adrenergic vasocontraction, similarly to α1-adrenergic contraction, in isolated human skeletal muscle feed arteries (SMFA) and elucidate the role of the temperature-sensitive vanilloid-type transient receptor potential (TRPV) ion channels in this response. Isolated SMFA from 37 subjects were studied using wire myography. α1 [Phenyle...

Vanilloid receptors of the transient receptor potential family have functions in thermal sensation and nociception. Among them, transient receptor potential vanilloid (TRPV)3 displays a unique property by which the repeated stimulation causes successive increases in its activity. The property has been known as sensitization and is observed in both native cells and cells heterologously expressin...

Holzer, Peter. Neural Injury, Repair, and Adaptation in the GI Tract. II. The elusive action of capsaicin on the vagus nerve. Am. J. Physiol. 275 (Gastrointest. Liver Physiol. 38): G8–G13, 1998.—Capsaicin is an excitotoxin for primary afferent neurons, and perivagal administration of capsaicin is frequently used to ablate afferent fibers from the vagus nerve in an attempt to elucidate the role ...

The ability to avoid noxious extremes of hot and cold is critical for survival and depends on thermal nociception. The TRPV subset of transient receptor potential (TRP) channels is heat activated and proposed to be responsible for heat detection in vertebrates and fruit flies. To gain insight into the genetic and neural basis of thermal nociception, we developed assays that quantify noxious hea...

Understanding the structural and functional complexities of the transient receptor potential vanilloid receptor (TRPV1) is essential to the therapeutic modulation of inflammation and pain. Because of its central role in initiating inflammatory processes and integrating painful stimuli, there is an understandable interest in its pharmacological manipulation (sensitization/desensitization). The p...

Capsaicin, the pungent ingredient in hot pepper, activates and subsequently desensitizes a subset of polymodal nociceptors. Because its initial application to skin produces pain, nonpungent analogs such as olvanil and glyceryl nonivamide (GLNVA) were synthesized to enhance its clinical use. To explore how these nonpungent analogs differ from capsaicin, whole-cell patch-clamp recordings were per...

Whole-cell and single-channel recordings from rat dorsal root ganglion neurones were used to investigate the temperature dependence of currents through the capsaicin receptor (vanilloid receptor 1, VR1). Reducing the temperature from 31 to 148C inhibited the current induced by 0.5 mM capsaicin by 80%. The Q10 (temperature coefficient over a 108C range) of the whole-cell capsaicin-induced curren...