eprintid: 10164655 rev_number: 16 eprint_status: archive userid: 699 dir: disk0/10/16/46/55 datestamp: 2023-02-10 12:47:24 lastmod: 2023-03-03 11:17:59 status_changed: 2023-02-10 12:47:24 type: article metadata_visibility: show sword_depositor: 699 creators_name: Iseppon, Federico creators_name: Luiz, Ana P creators_name: Linley, John E creators_name: Wood, John N title: Pregabalin silences oxaliplatin-activated sensory neurons to relieve cold allodynia ispublished: pub divisions: UCL divisions: B02 divisions: C10 divisions: D17 divisions: G95 keywords: Oaxliplatin, Pain, Pregabalin, sensory neurons, silent nociceptors note: Copyright © 2023 Iseppon et al. This is an open-access article distributed under the terms of the Creative Commons Attribution 4.0 International license, which permits unrestricted use, distribution and reproduction in any medium provided that the original work is properly attributed. abstract: Oxaliplatin is a platinum-based chemotherapeutic agent that causes cold and mechanical allodynia in up to 90% of patients. Silent Nav1.8-positive nociceptive cold sensors have been shown to be unmasked by oxaliplatin, and this event has been causally linked to the development of cold allodynia. We examined the effects of pregabalin on oxaliplatin-evoked unmasking of cold sensitive neurons using mice expressing GCaMP-3 in all sensory neurons. Intravenous injection of pregabalin significantly ameliorates cold allodynia, while decreasing the number of cold sensitive neurons by altering their excitability and temperature thresholds. The silenced neurons are predominantly medium/large mechano-cold sensitive neurons, corresponding to the 'silent' cold sensors activated during neuropathy. Deletion of α2δ1 subunits abolished the effects of pregabalin on both cold allodynia and the silencing of sensory neurons. Thus, these results define a novel, peripheral inhibitory effect of pregabalin on the excitability of 'silent' cold-sensing neurons in a model of oxaliplatin-dependent cold allodynia.Significance StatementPregabalin is an analgesic drug in the clinic, that is supposed to act by blocking neurotransmitter release. Here we show that silent nociceptors that are activated by chemotherapeutic insults like oxaliplatin are silenced by pregabalin, which blocks the associated pain. This mode of action suggests that peripheral acting pregabalin-like drugs could be very useful for pain during chemotherapy, as they would have no CNS side effects - a problem for many patients with pregabalin. This novel effect of pregabalin is mediated by its interaction with the α2δ1 calcium channel subunit, but how this works is not yet understood. date: 2023-02 date_type: published publisher: Society for Neuroscience official_url: https://doi.org/10.1523/ENEURO.0395-22.2022 oa_status: green full_text_type: pub language: eng primo: open primo_central: open_green verified: verified_manual elements_id: 2004437 doi: 10.1523/ENEURO.0395-22.2022 medium: Print-Electronic pii: ENEURO.0395-22.2022 lyricists_name: Wood, John lyricists_id: JNWOO78 actors_name: Flynn, Bernadette actors_id: BFFLY94 actors_role: owner full_text_status: public publication: eNeuro volume: 10 number: 2 article_number: 0395-22.2022 event_location: United States citation: Iseppon, Federico; Luiz, Ana P; Linley, John E; Wood, John N; (2023) Pregabalin silences oxaliplatin-activated sensory neurons to relieve cold allodynia. eNeuro , 10 (2) , Article 0395-22.2022. 10.1523/ENEURO.0395-22.2022 <https://doi.org/10.1523/ENEURO.0395-22.2022>. Green open access document_url: https://discovery.ucl.ac.uk/id/eprint/10164655/1/Pregabalin%20silences%20oxaliplatin-activated%20sensory%20neurons%20to%20relieve%20cold%20allodynia.pdf