Anxiolytic Effects in Mice of a Dual Blocker of Fatty Acid
Amide Hydrolase and Transient Receptor Potential Vanilloid
Type-1 Channels

J 2009

Anxiolytic Effects in Mice of a Dual Blocker of Fatty Acid Amide Hydrolase and Transient Receptor Potential Vanilloid Type-1 Channels

MICALE, Vincenzo; Luigia CRISTINO; Alessandra TAMBURELLA; Stefania PETROSINO; Gian Marco LEGGIO et al.

Základní údaje

Originální název

Anxiolytic Effects in Mice of a Dual Blocker of Fatty Acid Amide Hydrolase and Transient Receptor Potential Vanilloid Type-1 Channels

Autoři

MICALE, Vincenzo; Luigia CRISTINO; Alessandra TAMBURELLA; Stefania PETROSINO; Gian Marco LEGGIO; Filippo DRAGO a Vincenzo DI MARZO

Vydání

Neuropsychopharmacology, New York, Elsevier Science, 2009, 0893-133X

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

30000 3. Medical and Health Sciences

Stát vydavatele

Spojené státy

Utajení

není předmětem státního či obchodního tajemství

Impakt faktor

Impact factor: 6.993

Označené pro přenos do RIV

DOI

https://doi.org/10.1038/npp.2008.98

UT WoS

000262376200008

Klíčová slova anglicky

endocannabinoid; endovanilloid; FAAH; TRPV1; CB1; anxiety

Příznaky

Mezinárodní význam, Recenzováno

Změněno: 25. 7. 2012 00:06, Olga Křížová

Anotace

V originále

The endocannabinoid-inactivating enzyme, fatty acid amide hydrolase (FAAH), and the transient receptor potential vanilloid type-1 (TRPV1) channel are new targets for the development of anxiolytic drugs. We studied the effect on anxiety-like behavior in the elevated plus maze of a dual FAAH/TRPV1 blocker, N-arachidonoyl-serotonin (AA-5-HT). In male C57BL/6J mice, acute intraperitoneal administration of AA-5-HT (0.1-2.5 mg/kg) increased both the time spent and the number of entries in the open arm, while being inactive at the highest dose tested (5 mg/kg). AA-5-HT was more potent than selective blockers of FAAH or TRPV1 (URB597 and SB366791, respectively). In male Swiss mice, AA-5-HT had to be administered chronically to observe an anxiolytic effect at an intermediate dose (2.5 mg/kg), the highest dose (5 mg/kg) being anxiogenic, and 1 mg/kg being ineffective. In both strains, the anxiolytic effects of AA-5-HT were paralleled by elevation of brain endocannabinoid levels and were reversed by per se inactive doses of the cannabinoid receptors of type-1 (CB(1)) receptor antagonist AM251, or the TRPV1 agonist, olvanil. Immunohistochemical localization of CB(1) and TRPV1 receptors was observed in mouse prefrontal cortex, nucleus accumbens, amygdala, and hippocampus. Simultaneous 'indirect' activation of CB(1) receptors following FAAH inhibition, and antagonism at TRPV1 receptors might represent a new therapeutic strategy against anxiety.

Citovat

MICALE, Vincenzo; Luigia CRISTINO; Alessandra TAMBURELLA; Stefania PETROSINO; Gian Marco LEGGIO; Filippo DRAGO a Vincenzo DI MARZO. Anxiolytic Effects in Mice of a Dual Blocker of Fatty Acid Amide Hydrolase and Transient Receptor Potential Vanilloid Type-1 Channels. Neuropsychopharmacology. New York: Elsevier Science, 2009, roč. 34, č. 3, s. 593-606. ISSN 0893-133X. Dostupné z: https://doi.org/10.1038/npp.2008.98.

@article{987897,
   author = {Micale, Vincenzo and Cristino, Luigia and Tamburella, Alessandra and Petrosino, Stefania and Leggio, Gian Marco and Drago, Filippo and Di Marzo, Vincenzo},
   article_location = {New York},
   article_number = {3},
   doi = {https://doi.org/10.1038/npp.2008.98},
   keywords = {endocannabinoid; endovanilloid; FAAH; TRPV1; CB1; anxiety},
   language = {eng},
   issn = {0893-133X},
   journal = {Neuropsychopharmacology},
   title = {Anxiolytic Effects in Mice of a Dual Blocker of Fatty Acid Amide Hydrolase and Transient Receptor Potential Vanilloid Type-1 Channels},
   volume = {34},
   year = {2009}
}

TY  - JOUR
ID  - 987897
AU  - Micale, Vincenzo - Cristino, Luigia - Tamburella, Alessandra - Petrosino, Stefania - Leggio, Gian Marco - Drago, Filippo - Di Marzo, Vincenzo
PY  - 2009
TI  - Anxiolytic Effects in Mice of a Dual Blocker of Fatty Acid Amide Hydrolase and Transient Receptor Potential Vanilloid Type-1 Channels
JF  - Neuropsychopharmacology
VL  - 34
IS  - 3
SP  - 593-606
EP  - 593-606
PB  - Elsevier Science
SN  - 0893133X
KW  - endocannabinoid
KW  - endovanilloid
KW  - FAAH
KW  - TRPV1
KW  - CB1
KW  - anxiety
N2  - The endocannabinoid-inactivating enzyme, fatty acid amide hydrolase (FAAH), and the transient receptor potential vanilloid type-1 (TRPV1) channel are new targets for the development of anxiolytic drugs. We studied the effect on anxiety-like behavior in the elevated plus maze of a dual FAAH/TRPV1 blocker, N-arachidonoyl-serotonin (AA-5-HT). In male C57BL/6J mice, acute intraperitoneal administration of AA-5-HT (0.1-2.5 mg/kg) increased both the time spent and the number of entries in the open arm, while being inactive at the highest dose tested (5 mg/kg). AA-5-HT was more potent than selective blockers of FAAH or TRPV1 (URB597 and SB366791, respectively). In male Swiss mice, AA-5-HT had to be administered chronically to observe an anxiolytic effect at an intermediate dose (2.5 mg/kg), the highest dose (5 mg/kg) being anxiogenic, and 1 mg/kg being ineffective. In both strains, the anxiolytic effects of AA-5-HT were paralleled by elevation of brain endocannabinoid levels and were reversed by per se inactive doses of the cannabinoid receptors of type-1 (CB(1)) receptor antagonist AM251, or the TRPV1 agonist, olvanil. Immunohistochemical localization of CB(1) and TRPV1 receptors was observed in mouse prefrontal cortex, nucleus accumbens, amygdala, and hippocampus. Simultaneous 'indirect' activation of CB(1) receptors following FAAH inhibition, and antagonism at TRPV1 receptors might represent a new therapeutic strategy against anxiety.
ER  -

MICALE, Vincenzo; Luigia CRISTINO; Alessandra TAMBURELLA; Stefania PETROSINO; Gian Marco LEGGIO; Filippo DRAGO a Vincenzo DI MARZO. Anxiolytic Effects in Mice of a Dual Blocker of Fatty Acid Amide Hydrolase and Transient Receptor Potential Vanilloid Type-1 Channels. \textit{Neuropsychopharmacology}. New York: Elsevier Science, 2009, roč.~34, č.~3, s.~593-606. ISSN~0893-133X. Dostupné z: https://doi.org/10.1038/npp.2008.98.

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