نتایج جستجو برای: am251

تعداد نتایج: 328  

Journal: :PPAR Research 2009
Saoirse E. O'Sullivan David A. Kendall Michael D. Randall

The aim of the present study was to examine whether endocannabinoids cause PPARγ-mediated vascular actions. Functional vascular studies were carried out in rat aortae. Anandamide and N-arachidonoyl-dopamine (NADA), but not palmitoylethanolamide, caused significant vasorelaxation over time (2 hours). Vasorelaxation to NADA, but not anandamide, was inhibited by CB(1) receptor antagonism (AM251, 1...

2014
Agostino Bruno Francesca Lembo Ettore Novellino Mariano Stornaiuolo Luciana Marinelli

Cannabinoid type 1 Receptor (CB1) belongs to the GPCR family and it has been targeted, so far, for the discovery of drugs aimed at the treatment of neuropathic pain, nausea, vomit, and food intake disorders. Here, we present the development of the first fluorescent assay enabling the measurement of kinetic binding constants for CB1 orthosteric ligands. The assay is based on the use of T1117, a ...

Journal: :Neuron 2001
Anatol C Kreitzer Wade G Regehr

Brief depolarization of cerebellar Purkinje cells was found to inhibit parallel fiber and climbing fiber EPSCs for tens of seconds. This depolarization-induced suppression of excitation (DSE) is accompanied by altered paired-pulse plasticity, suggesting a presynaptic locus. Fluorometric imaging revealed that postsynaptic depolarization also reduces presynaptic calcium influx. The inhibition of ...

Journal: :Neuron 2002
Anatol C Kreitzer Adam G Carter Wade G Regehr

Endocannabinoids serve as retrograde messengers in many brain regions. These diffusible lipophilic molecules are released by postsynaptic cells and regulate presynaptic neurotransmitter release. Here we describe an additional mechanism that mediates the spread of endocannabinoid signaling to distant inhibitory synapses. Depolarization of cerebellar Purkinje cells reduced the firing rate of near...

2011
Wei Xia Ning-Ning Chu Jing Liang Yi-Jing Li Rong Zhang Ji-Sheng Han Cai-Lian Cui

Electroacupuncture (EA) has been used to suppress heroin craving in addicts and the conditioned place preference (CPP) for morphine in the rat. The question remained whether EA by itself will produce some rewarding effect. This was investigated using the CPP procedure in the present study. The results indicated that rats showed a significant preference to the 2 Hz EA-paired compartment. This re...

Journal: :Neuropharmacology 2008
Henry H Yin Louise Adermark David M Lovinger

Neurotensin is a peptide that has been suggested to mimic the actions of antipsychotics, but little is known about how it affects synaptic transmission in the striatum, the major input nucleus of the basal ganglia. In this study we measured the effects of neurotensin on EPSCs from medium spiny projection neurons in the sensorimotor striatum, a region implicated in habit formation and control of...

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