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description Publicationkeyboard_double_arrow_right Article , Journal 2016 ItalyPublisher:Elsevier BV Authors:VINCENZI, Fabrizio;
RAVANI, Annalisa;VINCENZI, Fabrizio
VINCENZI, Fabrizio in OpenAIREPASQUINI, Silvia;
PASQUINI, Silvia
PASQUINI, Silvia in OpenAIREMERIGHI, Stefania;
+5 AuthorsMERIGHI, Stefania
MERIGHI, Stefania in OpenAIREVINCENZI, Fabrizio;
RAVANI, Annalisa;VINCENZI, Fabrizio
VINCENZI, Fabrizio in OpenAIREPASQUINI, Silvia;
PASQUINI, Silvia
PASQUINI, Silvia in OpenAIREMERIGHI, Stefania;
MERIGHI, Stefania
MERIGHI, Stefania in OpenAIREGESSI, Stefania;
GESSI, Stefania
GESSI, Stefania in OpenAIREROMAGNOLI, Romeo;
ROMAGNOLI, Romeo
ROMAGNOLI, Romeo in OpenAIREBARALDI, Pier Giovanni;
BOREA, Pier Andrea;BARALDI, Pier Giovanni
BARALDI, Pier Giovanni in OpenAIREVARANI, Katia;
VARANI, Katia
VARANI, Katia in OpenAIREActivation of A1 adenosine receptors (ARs) has been associated with anxiolytic-like effects in different behavioral tests, but development of A1AR agonists for therapeutic use has been hampered, most likely due to the presence of side effects. With the aim to identify a safer approach for the treatment of anxiety, we investigated, in mice, the anxiolytic-like properties of a novel A1AR positive allosteric modulator, TRR469. Acute administration of TRR469 (0.3-3 mg/kg) resulted in robust anxiolytic-like effects in the elevated plus maze, the dark/light box, the open field and the marble burying tests. The magnitude of the anxiolytic action of TRR469 was comparable to that obtained with benzodiazepine diazepam (1 mg/kg). The use of the A1AR antagonist DPCPX (3 mg/kg) suggested that the effects of TRR469 were mediated by this receptor subtype. In contrast to diazepam, the novel positive allosteric modulator did not potentiate the sedative effect of ethanol (3.5 g/kg) evaluated by the loss of righting reflex. While diazepam produced motor coordination impairment in the rotarod test, this effect being enhanced by the presence of ethanol (1.5 g/kg), TRR469 did not elicit locomotor disturbances either when administered alone or in the presence of ethanol. In vitro, TRR469 was able to increase the number of A1AR recognizable by the agonist radioligand [3H]-CCPA in mouse brain regions involved in emotional processes. TRR469 markedly increased the affinity of the agonist CCPA, suggesting the capability, in vivo, to increase the affinity of endogenous adenosine. Taken together, these findings indicate that the positive allosteric modulation of A1AR may represent a promising approach for the treatment of anxiety-related disorders.
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You have already added works in your ORCID record related to the merged Research product.This Research product is the result of merged Research products in OpenAIRE.
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