To determine if eCBs tonically regulate glutamatergic transmission onto PV (+)-INs by presynaptic CB 1 Rs, we first measured 50-ms PPR in the presence of a CB 1 R inverse agonist, AM251 (5 μM).

2023年1月12日 · In this study, we investigated whether LTP alteration acutely caused by CB1 and GABA B receptor antagonists (AM251 and CGP55845, respectively) happens at the postsynaptic or presynaptic regions, or at both. Therefore, the paired-pulse ratio (PPR) was assessed prior to and following the LTP induction in the studied groups.

2010年12月22日 · Application of AM251 blocked the increase in PPR induced by CB 1 R activation (100 ± 4% of baseline; P = 0.98, paired t -test; means ± SE). Antagonism of the CB 1 receptor blocks exogenous eCB-mediated reduction of synaptic strength.

2011年3月30日 · The present study provides experimental evidence that the cellular actions of AM251 involves ERRα, showing not only that AM251 interacts directly with ERRα LBD in vitro, but also that blockade of ERRα signalling with DES, XCT790 or gene knock-down by siRNA elicits an increase in gene expression that is reminiscent of the situation with AM251.

2011年5月1日 · AM251 given at the dose of 1.0 mg/kg, both 15 min before the learning trial (T1) and immediately afterwards, improved recognition memory in rats measured by the difference in time of exploration of a duplicate (A’) of the familiar object A and a new object B in T2 trial (variable B – A’) presented in 2 h delay in comparison with the ...

The cannabinoid CB1 receptor is known to be a negative modulator of synaptic glutamate release [18] and the CB1 antagonist AM251 decreases cocaine-primed reinstatement while also inhibiting the increase in extracellular glutamate that accompanies reinstatement of cocaine-seeking [19••].

Background and purpose: AM251 is an inverse agonist of the cannabinoid 1 receptor (CB (1)R) that can exert 'off-target' effects in vitro and in CB (1)R knock-out mice. AM251 is also potent at modulating tumour cell growth, suggesting that growth factor-mediated oncogenic signalling could be regulated by AM251.

AM-251 is an inverse agonist at the CB 1 cannabinoid receptor. AM-251 is structurally very close to rimonabant; both are biarylpyrazole cannabinoid receptor antagonists. In AM-251, the p - chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p - …

2020年7月7日 · To determine if eCBs tonically regulate glutamatergic transmission onto PV (+)-INs by presynaptic CB 1 Rs, we first measured 50-ms PPR in the presence of a CB 1 R inverse agonist, AM251 (5 μM).

2024年8月15日 · We substantiated the effect of AM251, a cannabinoid receptor-1 (CB1R) antagonist, against β-receptor stimulated myocardial infarction (MI) in streptozotocin (STZ)-induced diabetic mice via modulation- of the NF-kB signaling pathway.