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Orally active peptide vector allows using cannabis to fight pain while avoiding...

Gallo, Maria; Moreno, Estefanía; Defaus, Sira; Ortega-Alvaro, Antonio; Gonzalez, Angel; Robledo, Patricia; Cavaco, Marco; Neves, Vera

The activation of cannabinoid CB1 receptors (CB1R) by Δ9-tetrahydrocannabinol (THC), the main component of Cannabis sativa, induces analgesia. CB1R activation, however, also causes cognitive impairment via the serotonin 5HT2A receptor (5HT2AR), a component of a CB1R–5HT2AR heteromer, posing a serious drawback for cannabinoid therapeutic use. We have shown that peptides reproducing CB1R transmembrane (TM) helice...


Control of glutamate release by complexes of adenosine and cannabinoid receptors

Köfalvi, Attila; Moreno, Estefanía; Cordomí, Arnau; Cai, Ning-Sheng; Fernández-Dueñas, Victor; Ferreira, Samira G.; Guixà-González, Ramón

It has been hypothesized that heteromers of adenosine A2A receptors (A2AR) and cannabinoid CB1 receptors (CB1R) localized in glutamatergic nerve terminals mediate the integration of adenosine and endocannabinoid signaling involved in the modulation of striatal excitatory neurotransmission. Previous studies have demonstrated the existence of A2AR-CB1R heteromers in artificial cell systems. A dependence of A2AR s...


Control of glutamate release by complexes of adenosine and cannabinoid receptors

Köfalvi, Attila; Moreno, Estefanía; Cordomí, Arnau; Cai, Ning-Sheng; Fernández-Dueñas, Victor; Ferreira, Samira G.; Guixà-González, Ramón

Background: It has been hypothesized that heteromers of adenosine A2A receptors (A2AR) and cannabinoid CB1 receptors (CB1R) localized in glutamatergic nerve terminals mediate the integration of adenosine and endocannabinoid signaling involved in the modulation of striatal excitatory neurotransmission. Previous studies have demonstrated the existence of A2AR-CB1R heteromers in artificial cell systems. A dependen...


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