Spider Venom Peptide Pn3a Inhibition of Primary Afferent High Voltage-Activated Calcium Channels.

ABSTRACT: Despite potently inhibiting the nociceptive voltage-gated sodium (Na_v) channel, Na_v1.7, µ-theraphotoxin Pn3a is antinociceptive only upon co-administration with sub-therapeutic opioid agonists, or by itself at doses >3,000-fold greater than its Na_v1.7 IC ₅₀ by a yet undefined mechanism. Na_v channels are structurally related to voltage-gated calcium (Ca_v) channels, Ca_v1 and Ca_v2. These channels mediate the high voltage-activated (HVA) calcium currents (I _Ca ) that orchestrate synaptic transmission in nociceptive dorsal root ganglion (DRG) neurons and are fine-tuned by opioid receptor (OR) activity. Using whole-cell patch clamp recording, we found that Pn3a (1

SUBMITTER: McArthur JR 

PROVIDER: S-EPMC7875911 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature