The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels

Abstract T-type calcium channels are known molecular targets of certain phytocannabinoids and endocannabinoids. Here we explored the modulation of Cav3.2 T-type calcium channels by terpenes derived from cannabis plants. A screen of eight commercially available terpenes revealed that camphene and alp...

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Autores principales:	Vinicius M. Gadotti, Sun Huang, Gerald W. Zamponi
Formato:	article
Lenguaje:	EN
Publicado:	BMC 2021
Materias:	Pain Terpenes Bisabolol Camphene T-type Calcium channels Neurology. Diseases of the nervous system RC346-429
Acceso en línea:	https://doaj.org/article/c8c442c2f3654c9896a80bd1601481a9
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spelling	oai:doaj.org-article:c8c442c2f3654c9896a80bd1601481a92021-11-21T12:41:53ZThe terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels10.1186/s13041-021-00876-61756-6606https://doaj.org/article/c8c442c2f3654c9896a80bd1601481a92021-11-01T00:00:00Zhttps://doi.org/10.1186/s13041-021-00876-6https://doaj.org/toc/1756-6606Abstract T-type calcium channels are known molecular targets of certain phytocannabinoids and endocannabinoids. Here we explored the modulation of Cav3.2 T-type calcium channels by terpenes derived from cannabis plants. A screen of eight commercially available terpenes revealed that camphene and alpha-bisabolol mediated partial, but significant inhibition of Cav3.2 channels expressed in tsA-201 cells, as well as native T-type channels in mouse dorsal root ganglion neurons. Both compounds inhibited peak current amplitude with IC50s in the low micromolar range, and mediated an additional small hyperpolarizing shift in half-inactivation voltage. When delivered intrathecally, both terpenes inhibited nocifensive responses in mice that had received an intraplantar injection of formalin, with alpha-bisabolol showing greater efficacy. Both terpenes reduced thermal hyperalgesia in mice injected with Complete Freund’s adjuvant. This effect was independent of sex, and absent in Cav3.2 null mice, indicating that these compounds mediate their analgesic properties by acting on Cav3.2 channels. Both compounds also inhibited mechanical hypersensitivity in a mouse model of neuropathic pain. Hence, camphene and alpha-bisabolol have a wide spectrum of analgesic action by virtue of inhibiting Cav3.2 T-type calcium channels.Vinicius M. GadottiSun HuangGerald W. ZamponiBMCarticlePainTerpenesBisabololCampheneT-typeCalcium channelsNeurology. Diseases of the nervous systemRC346-429ENMolecular Brain, Vol 14, Iss 1, Pp 1-10 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Pain Terpenes Bisabolol Camphene T-type Calcium channels Neurology. Diseases of the nervous system RC346-429
spellingShingle	Pain Terpenes Bisabolol Camphene T-type Calcium channels Neurology. Diseases of the nervous system RC346-429 Vinicius M. Gadotti Sun Huang Gerald W. Zamponi The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels
description	Abstract T-type calcium channels are known molecular targets of certain phytocannabinoids and endocannabinoids. Here we explored the modulation of Cav3.2 T-type calcium channels by terpenes derived from cannabis plants. A screen of eight commercially available terpenes revealed that camphene and alpha-bisabolol mediated partial, but significant inhibition of Cav3.2 channels expressed in tsA-201 cells, as well as native T-type channels in mouse dorsal root ganglion neurons. Both compounds inhibited peak current amplitude with IC50s in the low micromolar range, and mediated an additional small hyperpolarizing shift in half-inactivation voltage. When delivered intrathecally, both terpenes inhibited nocifensive responses in mice that had received an intraplantar injection of formalin, with alpha-bisabolol showing greater efficacy. Both terpenes reduced thermal hyperalgesia in mice injected with Complete Freund’s adjuvant. This effect was independent of sex, and absent in Cav3.2 null mice, indicating that these compounds mediate their analgesic properties by acting on Cav3.2 channels. Both compounds also inhibited mechanical hypersensitivity in a mouse model of neuropathic pain. Hence, camphene and alpha-bisabolol have a wide spectrum of analgesic action by virtue of inhibiting Cav3.2 T-type calcium channels.
format	article
author	Vinicius M. Gadotti Sun Huang Gerald W. Zamponi
author_facet	Vinicius M. Gadotti Sun Huang Gerald W. Zamponi
author_sort	Vinicius M. Gadotti
title	The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels
title_short	The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels
title_full	The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels
title_fullStr	The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels
title_full_unstemmed	The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels
title_sort	terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via cav3.2 t-type calcium channels
publisher	BMC
publishDate	2021
url	https://doaj.org/article/c8c442c2f3654c9896a80bd1601481a9
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The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels

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