Selective activation of TRPA1 ion channels by nitrobenzene skin sensitizers DNFB and DNCB

Abstract

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Sophocarpine inhibits TRP channels to produce anti-pruritic and analgesic effects in a mouse model of inflammatory itch and pain

“…Although the amino acid numbers differ, the binding pocket around the S4-S5 linker in TRPV1 of SC competing with AITC or CAP simulated in this study is quite similar to the previously published simulation of CAP binding to TRPV1, referring to the TRPV1 structure identified (42, 43). While the major simulations of AITC and SC demonstrated lower binding energy to the intracellular AR16 or the Linker domain in the N-terminus, the disturbance of SC in the Pre-S1 helix and the TRP-like domain seems more convincing, compared to the simulation of DNCB and DNFB, agonists of TRPA1 to trigger itch as AITC, binding to TRPA1 in protein pockets around the Linker domain and the TRP-like domain (44). Further studies focusing on protein pockets identified to testify whether SC is a competitive inhibitor of TRPV1 and TRPA1 are needed.…”