TRPV1 activation-modulating complex mixtures of cannabinoids and/or terpenes
Inventors
Small-Howard, Andrea • Turner, Helen
Assignees
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Publication Number
US-11260044-B2
Publication Date
2022-03-01
Expiration Date
Abstract
Described are methods of modulating the activation of the TRPV1 ion channel by administering at least one cannabinoid and/or terpene compound.
Core Innovation
The invention relates to modulating TRPV1 activation by externally contacting TRPV1-expressing cells with predefined cannabinoid/terpene compounds, including cannabigerolic acid (CBGA) and other cannabinoids and terpenes. It provides a state-based framework in which compounds induce distinct TRPV1 state-related agonist properties, including ion selectivity and whether the TRPV1 pore is dilated or remains non-dilated.
The disclosed evidence indicates that capsaicin drives a pore-dilated state (state 2), whereas many cannabinoids and terpenes primarily induce a non-dilated state (state 1) with distinct kinetics. The document reports that myrcene is TRPV1-specific and that different terpenes vary in TRPV1-mediated calcium influx.
The document describes how internal and external calcium affect cannabinoid/terpene-driven TRPV1 responses and includes reported EC50 and kinetic parameters for TRPV1 activation by CBD, CBDV, CBN, and CBG. It also explores state transitions involving pore-dilated versus rectifying behavior with cannabinoids versus capsaicin and outlines pharmaceutical composition and formulation options together with route options and in vivo contacting concepts.
Claims Coverage
The relevant material includes one independent claim and multiple dependent claims. Across the set, the inventive features focus on TRPV1-mediated contacting by a CBGA-containing pharmaceutical composition, selecting specific treated conditions, and optionally extending the cannabinoid/terpene composition or specifying whether contacted cells are killed or not killed.
CBGA-containing pharmaceutical composition for TRPV1 contacting
Administering to a subject with a condition selected from cardiac hypertrophy, urinary cystitis, and hearing loss an effective amount of a pharmaceutical composition comprising cannabigerolic acid (CBGA), wherein after administration CBGA contacts a TRPV1-expressing cell.
Additional cannabinoids in the CBGA pharmaceutical composition
The method further comprises a pharmaceutical composition that includes cannabinol (CBN), cannabidiol (CBD), cannabigerol (CBG), and/or cannabidivarin (CBDV).
Selected terpenes in the CBGA pharmaceutical composition
The method further limits the pharmaceutical composition to include at least one terpene selected from myrcene, beta-caryophyllene, limonene, linalool, phytol, nerolidol, and pinene.
Condition limitation to urinary cystitis
The method is limited to treating urinary cystitis.
Contacting that kills the contacted cell
The method includes contacting a cell such that the contacted cell is killed.
Contacting that does not kill the contacted cell
The method includes contacting a cell such that the contacted cell is not killed.
Overall claim coverage centers on treating cardiac hypertrophy, urinary cystitis, or hearing loss by administering an effective amount of a CBGA-containing pharmaceutical composition such that CBGA contacts TRPV1-expressing cells. Dependent claims then narrow the treated condition, add optional cannabinoid and selected terpene components, and specify whether the contacting is lethal to the contacted cell.
Stated Advantages
Documented Applications
Treating cardiac hypertrophy.
Treating urinary cystitis.
Treating hearing loss.
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