The role of (E)-6-chloro-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-2-styrylquinazolin-4(3H)-one in the modulation of cannabinoidergic system. A pilot study

Fabiana Plescia, Fulvio Plescia, Demetrio Raffa, Angela Cavallaro, Gianluca Lavanco, Benedetta Maggio, Maria Valeria Raimondi, Giuseppe Daidone, Anna Brancato, Carla Cannizzaro
Pharmacological Reports. 2018-12-01; 70(6): 1124-1132
DOI: 10.1016/j.pharep.2018.06.004

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BACKGROUND: Compounds acting on endocannabinoid system regulate different
neuronal processes through the cannabinoid receptors activation. The main aim of
this study was determining whether the 2-styrylquinazolin-4(3H)-one 5, a
structural analogue of rimonabant, was able to counteract the behavioural signs
of the activation of the endocannabinoidergic system induced by CP 55.940.

METHODS: Behavioural assessment was carried out using the tetrad task and the
novel object recognition test. The endocannabinoidergic system activation was
possible by the administration of CP 55.940 and 30min after rats were tested in
the tetrad task for the evaluation of the antinociceptive-, cataleptic-,
hypothermic- and locomotor- effects. The evaluation of the declarative memory was
carried out through the novel object recognition test. The administration of the
new compound was made at three different doses, 30min before CP 55.940
administration on a separate group of animals.

RESULTS: Our results demonstrated that compound 5, at the highest dose, was able
to counteract the effects exerted by CP 55.940, shown by an increase in body
temperature, total distance travelled, latency to fall and decrease in tail flick
latency, interfering conjointly in memory impairment.

CONCLUSION: This study shows that compound 5 is able to counteract the
cannabinoid activation induced by the agonist CP 55.940. Further investigations
on its pharmacological profile are mandatory before considering it as a potential
candidate for clinical studies and its possible employment as pharmacological
agent for the management of different pathological conditions such as motor
incoordination, obesity and brain related disorders.

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