Cannabinoid-mediated inhibition of recurrent excitatory circuitry in the dentate gyrus in a mouse model of temporal lobe epilepsy. [PDF]
Temporal lobe epilepsy (TLE) is a neurological condition associated with neuron loss, axon sprouting, and hippocampal sclerosis, which results in modified synaptic circuitry. Cannabinoids appear to be anti-convulsive in patients and animal models of TLE,
Muthu D Bhaskaran, Bret N Smith
doaj +1 more source
Highly potent, selective acylguanidine-type histamine H2 receptor agonists: synthesis and structure-activity relationships [PDF]
Potent and selective histamine H2 receptor (H2R) agonists are valuable pharmacological tools and might be of therapeutic value as drugs, for example in the treatment of severe congestive heart failure.
Kraus, Anja
core +1 more source
New Pyridone-Based Derivatives as Cannabinoid Receptor Type 2 Agonists [PDF]
The activation of the human cannabinoid receptor type II (CB2R) is known to mediate analgesic and anti-inflammatory processes without the central adverse effects related to cannabinoid receptor type I (CB1R).
Faundez Parraguez, Manuel +16 more
core +1 more source
Expedient Synthesis of Potent Cannabinoid Receptor Agonist (−)-CP55,940 [PDF]
[reaction: see text] A stereocontrolled synthesis of (-)-CP55,940, a potent cannabinoid receptor agonist, has been attained using a novel aldolization/retro-aldolization interconversion strategy, in which a temporarily generated chiral aldol motif plays essential roles.
Noriaki, Itagaki +2 more
openaire +3 more sources
Objective Amyotrophic lateral sclerosis (ALS) has a markedly distinctive clinical and neuroradiological signature, with the preferential involvement of specific brain networks and the apparent sparing of others. The molecular underpinnings of the strikingly selective anatomical vulnerability have not been fully elucidated to date despite the potential ...
Marlene Tahedl +10 more
wiley +1 more source
Synergistic antinociception by the cannabinoid receptor agonist anandamide and the PPAR-α receptor agonist GW7647 [PDF]
The analgesic properties of cannabinoid receptor agonists are well characterized. However, numerous side effects limit the therapeutic potential of these agents. Here we report a synergistic antinociceptive interaction between the endogenous cannabinoid receptor agonist anandamide and the synthetic peroxisome proliferator-activated receptor-alpha (PPAR-
RUSSO, ROBERTO +6 more
openaire +7 more sources
Aim This report presents a series of 16 patients who were admitted to the emergency department following confirmed intake of the potent synthetic cannabinoid ADB‐CHMINACA. Methods The cases are drawn from a prospective observational study following the recreational use of synthetic cannabinoids.
Maren Hermanns‐Clausen +7 more
wiley +1 more source
The development and therapeutic potential of classical and next-generation cannabinoid ligands
The endogenous cannabinoid system (ECS) is a complex network that plays a crucial role in various physiological processes, and its modulation through cannabinoid ligands has garnered significant interest in pharmacological research. Cannabinoid receptors,
Verónica Muñoz-Canales +4 more
doaj +1 more source
Heterodimerization of apelin receptor and neurotensin receptor 1 induces phosphorylation of ERK1/2and cell proliferationviaGαq-mediated mechanism [PDF]
Dimerization of G protein-coupled receptors (GPCRs) is crucial for receptor function including agonist affinity, efficacy, trafficking and specificity of signal transduction, including G protein coupling.
Cai, X +9 more
core +1 more source
Aim The purpose of this study is to evaluate safety, tolerability, pharmacokinetics (PK), food‐effect (FE) and pharmacodynamics (PD) of an oral tyrosine kinase‐2 (TYK2)/Janus kinase‐1 (JAK1) inhibitor, SDC‐1801, in healthy adult participants. Methods This first‐in‐human study randomized 95 male and female participants.
Chris Brearley +3 more
wiley +1 more source

