Actions and regulation of ionotropic cannabinoid receptors

L De Petrocellis, M Nabissi, G Santoni… - Advances in …, 2017 - Elsevier
Almost three decades have passed since the identification of the two specific metabotropic
receptors mediating cannabinoid pharmacology. Thereafter, many cannabinoid effects, both …

Transient receptor potential melastatin 8 channel (TRPM8) modulation: cool entryway for treating pain and cancer

MJ Pérez de Vega, I Gómez-Monterrey… - Journal of medicinal …, 2016 - ACS Publications
TRPM8 ion channels, the primary cold sensors in humans, are activated by innocuous
cooling (< 28° C) and cooling compounds (menthol, icilin) and are implicated in sensing …

Behavioral characterization of a CRISPR-generated TRPA1 knockout rat in models of pain, itch, and asthma

RM Reese, M Dourado, K Anderson, S Warming… - Scientific reports, 2020 - nature.com
The transient receptor potential (TRP) superfamily of ion channels has garnered significant
attention by the pharmaceutical industry. In particular, TRP channels showing high levels of …

Effects of curcumin and curcumin analogues on TRP channels

M Nalli, G Ortar, AS Moriello, V Di Marzo… - Fitoterapia, 2017 - Elsevier
A series of 33 curcumin analogues was synthesized and tested on TRPA1, TRPM8, and
TRPV1 channels. Twenty of them acted as good modulators of TRPA1 channels. None was …

Advances in the synthesis of heterocycles bearing an endocyclic urea moiety

AV Smolobochkin, AS Gazizov… - Russian Chemical …, 2021 - iopscience.iop.org
The review systematizes and summarizes data on the synthesis of structurally diverse cyclic
ureas published over the last 10 years. Saturated and unsaturated monocyclic ureas, as well …

Tetrahydroisoquinoline-derived urea and 2, 5-diketopiperazine derivatives as selective antagonists of the transient receptor potential melastatin 8 (TRPM8) channel …

L De Petrocellis, FJ Arroyo, P Orlando… - Journal of medicinal …, 2016 - ACS Publications
Tetrahydroisoquinoline derivatives containing embedded urea functions were identified as
selective TRPM8 channel receptor antagonists. Structure–activity relationships were …

Fluorescence-based assay for TRPV1 channels

AS Moriello, L De Petrocellis, RM Vitale - … Signaling: Methods and …, 2022 - Springer
The transient receptor potential vanilloid 1 ion channel (TRPV1) is a ligand-gated
nonselective calcium-permeant cation channel involved in the detection of a wide variety of …

Assay of TRPV1 receptor signaling

AS Moriello, L De Petrocellis - Endocannabinoid Signaling: Methods and …, 2016 - Springer
The transient receptor potential vanilloid-1 ion channel (TRPV1) is a non-selective ligand-
gated cation channel. It is an integrator of a wide variety of exogenous and endogenous …

Dihydropyrimidin-2 (1H)-one and its analogues as a platform for the design and synthesis of new biologically active compounds

OP Shkurko, TG Tolstikova… - Russian Chemical …, 2016 - iopscience.iop.org
The data published mainly over two past decades on various types of biological activity of 5-
functionally substituted 3, 4-dihydropyrimidin-2-ones and their analogues, 2-thiones and 2 …

Natural compounds and synthetic drugs targeting the ionotropic cannabinoid members of transient receptor potential (TRP) channels

RM Vitale, AS Moriello, L De Petrocellis - 2020 - books.rsc.org
The transient receptor potential (TRP) channels are a superfamily of cation-permeable
channels found in yeast, invertebrates and vertebrates. The name comes from the first TRP …