Effects of anandamide on cannabinoid receptors in rat brain membranes
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2011, Biochimica et Biophysica Acta - Molecular and Cell Biology of LipidsCitation Excerpt :In clinical studies, containers with EDTA-anticoagulated blood should be immediately put in an ice bath followed by centrifugation in the cold, be portioned (e.g., in 1-mL aliquots), frozen as soon as possible at − 80 °C and stored at this temperature until analysis. Inhibition of unspecific amidases, esterases and proteases through externally added inhibitors such as phenylmethylsulfonyl fluoride (PMSF) has been successfully tested as an approach to prevent EC hydrolysis following blood sampling [115]. However, whole blood incubation with PMSF at 37 °C for 24 h prior to plasma generation by centrifugation produces significantly higher plasma EC concentrations [116].
The endogenous cannabinoid anandamide shares discriminative stimulus effects with △<sup>9</sup>-tetrahydrocannabinol in fatty acid amide hydrolase knockout mice
2011, European Journal of PharmacologyCitation Excerpt :Further, while AEA evoked a transient cannabimimetic profile as assessed through the tetrad (hypolocomotion, hypothermia, antinociception, catalepsy; Smith et al., 1994), AEA failed to influence other behaviors typically altered by cannabinoids, including anxiety-like behavior, memory and food intake (Crawley et al., 1993). Further, significant AEA binding in rat brain homogenate was attained only in the presence of the non-specific serine protease inhibitor phenylmethylsulfonyl fluoride (PMSF; Childers et al., 1994). These results, along with others, strongly suggested that AEA was rapidly metabolized, hence the general lack of cannabinoid activity in vivo.
Chapter 4 Anandamide Receptor Signal Transduction
2009, Vitamins and HormonesCitation Excerpt :For many years, reports of this nature were largely brushed aside as being a result of rapid metabolism. These concerns, although valid, were countered by the use of the metabolically stable derivative, methanandamide, and inhibitors of anandamide degradation coupled with more stringent controls in many publications (Abadji et al., 1994; Breivogel et al., 1998; Childers et al., 1994; Deutsch, 2005; Pinto et al., 1994). In GTPγS assays performed with both rat brain membranes and membranes from CHO cells transfected with human CB1 receptor anandamide acts as a partial agonist (Breivogel et al., 1998; Gonsiorek et al., 2000).
Development of novel tail-modified anandamide analogs
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