Multiple voltage-gated
calcium channels (VGCCs) contribute to the processing of nociceptive signals in primary afferent fibers. In addition, alteration of
calcium channel activity is associated with a number of
chronic pain conditions. Therefore, VGCCs have emerged as prime target for the management of either neuropathic or inflammatory
pain, and selective
calcium channel blockers have been shown to have efficacy in animal models and in the clinic. However, considering that multiple
calcium channels contribute
pain afferent signaling, broad-spectrum inhibitors of several channel
isoforms may offer a net advantage in modulating
pain. Here, we have analyzed the ability of the compound
surfen to modulate
calcium channels, and assessed its
analgesic potential. We show that
surfen is an equipotent blocker of both low- and high-voltage-activated
calcium channels. Furthermore, spinal (intrathecal) delivery of
surfen to mice produces sustained
analgesia against both acute and
chronic pain. Collectively, our data establish
surfen as a broad-spectrum
calcium channel inhibitor with
analgesic potential, and raise the possibility of using
surfen-derived compounds for the development of new
pain-relieving drugs.