Daniele Piomelli
University of California, Irvine
EndocrinologyCannabinoid receptorAnandamideEndocannabinoid systemBiochemistry
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Publications 527
#1Devon Ivy (UCI: University of California, Irvine)
#2Francesca Palese (UCI: University of California, Irvine)H-Index: 1
Last. Daniele Piomelli (UCI: University of California, Irvine)H-Index: 93
view all 9 authors...
The endocannabinoid system is a key regulator of the response to psychological stress. Inhibitors of monoacylglycerol lipase (MGL), the enzyme that deactivates the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG), exert anxiolytic-like effects in rodent models via 2-AG-dependent activation of CB1 cannabinoid receptors. In the present study, we examined whether the MGL inhibitor JZL184 might modulate persistent predator-induced fear in rats, a model that captures features of human post-traumatic...
#1Lorena Macías-Triana (Universidad Anáhuac México Norte)H-Index: 1
#2Karen Romero-Cordero (Universidad Anáhuac México Norte)H-Index: 1
Last. Eric Murillo-Rodríguez (Universidad Anáhuac México Norte)H-Index: 23
view all 8 authors...
Abstract Cannabis and, to a lesser extent, synthetic cannabinoids are used during adolescence, a period in which multiple brain areas are still undergoing development. Among such areas is the hypothalamus, which is implicated in the control of sleep-wake cycle. In the present report, we show that exposing adolescent rats to the cannabinoid receptor agonist WIN 55, 212–2 (0.1, 0.3 or 1.0 mg/kg, i.p) for 14 days during adolescence (i.e., from post-natal day 30–44) resulted in significant sleep dis...
#1Alexa Torrens (UCI: University of California, Irvine)
#2Valentina Vozella (UCI: University of California, Irvine)H-Index: 5
Last. Daniele Piomelli (UCI: University of California, Irvine)H-Index: 93
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We investigated the pharmacokinetic properties of Delta(9)-tetrahydrocannabinol (Delta(9)-THC), the main psychoactive constituent of cannabis, in adolescent and adult male mice. The drug was administered at logarithmically ascending doses (0.5, 1.6 and 5 mg/kg, intraperitoneal) to pubertal adolescent (37-day old) and adult (70-day old) mice. Delta(9)-THC and its first-pass metabolites - 11-hydroxy-Delta(9)-THC (11-OH-THC) and 11-nor-9-carboxy-Delta(9)-THC (11-COOH-THC) - were quantified in plasm...
#1Silvia Carloni (University of Urbino)H-Index: 3
#1Silvia CarloniH-Index: 24
Last. Daniel Alonso-AlconadaH-Index: 12
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The number of functions controlled by the endocannabinoid system in health and disease continues growing over the years. In the brain, these include the modulation of harmful events such as glutama...
#1Daniele PiomelliH-Index: 93
#2Laura ScalviniH-Index: 6
Last. Marco MorH-Index: 43
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N-Acylethanolamine acid amidase (NAAA) is an N-terminal cysteine hydrolase primarily found in the endosomal-lysosomal compartment of innate and adaptive immune cells. NAAA catalyzes the hydrolytic deactivation of palmitoylethanolamide (PEA), a lipid-derived peroxisome proliferator-activated receptor-alpha (PPAR-alpha) agonist that exerts profound anti-inflammatory effects in animal models. Emerging evidence points to NAAA-regulated PEA signaling at PPAR-alpha as a critical control point for the ...
2 CitationsSource
#1Daniele Piomelli (UCI: University of California, Irvine)H-Index: 93
#1D Dey (UCI: University of California, Irvine)
Last. David Merriott (UCI: University of California, Irvine)
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Radiotherapy, surgery and the chemotherapeutic agent temozolomide (TMZ) are frontline treatments for glioblastoma multiforme (GBM). However beneficial, GBM treatments nevertheless cause anxiety or ...
#1Yannick Fotio (UCI: University of California, Irvine)H-Index: 1
#2Francesca Palese (UCI: University of California, Irvine)H-Index: 1
Last. Daniele Piomelli (UCI: University of California, Irvine)H-Index: 93
view all 5 authors...
BACKGROUND AND PURPOSE: Fatty acid amide hydrolase (FAAH) is an intracellular serine amidase that terminates the signaling activity of various lipid messengers involved in pain regulation, including agonists at cannabinoid receptors (e.g., anandamide) and peroxisome proliferator-activated receptor-alpha (PPAR-alpha) [e.g., palmitoylethanolamide (PEA)]. Here, we investigated whether pharmacological or genetic FAAH removal might prevent and/or reverse tolerance to the antinociceptive effects of mo...
1 CitationsSource
#1Riccardo CastelliH-Index: 11
#2Laura ScalviniH-Index: 6
Last. Daniele PiomelliH-Index: 93
view all 21 authors...
We describe a set of benzisothiazolinone (BTZ) derivatives that are potent inhibitors of monoacylglycerol lipase (MGL), the primary degrading enzyme for the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). Structure-activity relationship studies evaluated various substitutions on the nitrogen atom and the benzene ring of the BTZ nucleus. Optimized derivatives with nanomolar potency allowed to investigate the mechanism of MGL inhibition. Site-directed mutagenesis and mass spectrometry experimen...
#1Rosaria GrecoH-Index: 21
#2Chiara DemartiniH-Index: 9
Last. Cristina Tassorelli (UNIPV: University of Pavia)H-Index: 41
view all 8 authors...
Abstract Background Fatty-acid amide hydrolase (FAAH) is an intracellular serine hydrolase that catalyzes the cleavage of endogenous fatty-acid amides, including the endocannabinoid anandamide (AEA). We previously reported that the peripherally restricted FAAH inhibitor URB937, which selectively increases AEA levels outside the central nervous system, reduces hyperalgesia and c-Fos expression in the trigeminal nucleus caudalis (TNC) and the locus coeruleus in an animal model of migraine based on...
2 CitationsSource