Literature DB >> 18801827

Inhibition of THC-induced effects on the central nervous system and heart rate by a novel CB1 receptor antagonist AVE1625.

L Zuurman1, C Roy, R C Schoemaker, A Amatsaleh, L Guimaeres, J L Pinquier, A F Cohen, J M A van Gerven.   

Abstract

CB1 antagonists such as AVE1625 are potentially useful in the treatment of obesity, smoking cessation and cognitive impairment. Proof of pharmacological action of AVE1625 in the brain can be given by antagonising the effects of delta-9-tetrahydrocannabinol (THC), a CB1/CB2 agonist. Inhibition of THC-induced effects by AVE1625 was observed on Visual Analogue Scales 'alertness', 'feeling high', 'external perception', 'body sway' and 'heart rate'. Even the lowest dose of AVE1625 20 mg inhibited most of THC-induced effects. AVE1625 did not have any effect on psychological and behavioural parameters or heart rate by itself. After THC and AVE1625 administration, changes on electroencephalography were observed. This study shows a useful method for studying the effects of CB1 antagonists. AVE1625 penetrates the brain and antagonises THC-induced effects with doses at or above 20 mg.

Entities:  

Mesh:

Substances:

Year:  2008        PMID: 18801827     DOI: 10.1177/0269881108096509

Source DB:  PubMed          Journal:  J Psychopharmacol        ISSN: 0269-8811            Impact factor:   4.153


  16 in total

Review 1.  Neural substrates underlying the negative impact of cannabinoid exposure during adolescence.

Authors:  Hanna M Molla; Kuei Y Tseng
Journal:  Pharmacol Biochem Behav       Date:  2020-06-09       Impact factor: 3.533

Review 2.  Human Drug Discrimination: Elucidating the Neuropharmacology of Commonly Abused Illicit Drugs.

Authors:  B Levi Bolin; Joseph L Alcorn; Anna R Reynolds; Joshua A Lile; William W Stoops; Craig R Rush
Journal:  Curr Top Behav Neurosci       Date:  2018

3.  Vanishing clinical psychopharmacology.

Authors:  Joop van Gerven; Adam Cohen
Journal:  Br J Clin Pharmacol       Date:  2011-07       Impact factor: 4.335

4.  Surinabant, a selective cannabinoid receptor type 1 antagonist, inhibits Δ9-tetrahydrocannabinol-induced central nervous system and heart rate effects in humans.

Authors:  Linda E Klumpers; Christine Roy; Geraldine Ferron; Sandrine Turpault; Franck Poitiers; Jean-Louis Pinquier; Johan G C van Hasselt; Lineke Zuurman; Frank A S Erwich; Joop M A van Gerven
Journal:  Br J Clin Pharmacol       Date:  2013-07       Impact factor: 4.335

5.  Disturbances of postural sway components in cannabis users.

Authors:  Amanda R Bolbecker; Deborah Apthorp; Ashley Schnakenberg Martin; Behdad Tahayori; Leah Moravec; Karen L Gomez; Brian F O'Donnell; Sharlene D Newman; William P Hetrick
Journal:  Drug Alcohol Depend       Date:  2018-06-21       Impact factor: 4.492

6.  Separate and combined effects of the GABA reuptake inhibitor tiagabine and Δ9-THC in humans discriminating Δ9-THC.

Authors:  Joshua A Lile; Thomas H Kelly; Lon R Hays
Journal:  Drug Alcohol Depend       Date:  2011-10-04       Impact factor: 4.492

Review 7.  Mechanisms contributing to cognitive deficits in cannabis users.

Authors:  Romina Mizrahi; Jeremy J Watts; Kuei Y Tseng
Journal:  Neuropharmacology       Date:  2017-04-14       Impact factor: 5.250

8.  Pharmacokinetic/pharmaco-dynamic modelling and simulation of the effects of different cannabinoid receptor type 1 antagonists on Δ(9)-tetrahydrocannabinol challenge tests.

Authors:  Zheng Guan; Linda E Klumpers; Olubukayo-Opeyemi Oyetayo; Jules Heuberger; Joop M A van Gerven; Jasper Stevens
Journal:  Br J Clin Pharmacol       Date:  2016-01-29       Impact factor: 4.335

9.  Peripheral selectivity of the novel cannabinoid receptor antagonist TM38837 in healthy subjects.

Authors:  Linda E Klumpers; Marianne Fridberg; Marieke L de Kam; Paul B Little; Niels Ole Jensen; Hendrik D Kleinloog; Christian E Elling; Joop M A van Gerven
Journal:  Br J Clin Pharmacol       Date:  2013-12       Impact factor: 4.335

10.  Profiling the subjective effects of Δ⁹-tetrahydrocannabinol using visual analogue scales.

Authors:  Daniël Kleinloog; Frits Roozen; Willem De Winter; Jan Freijer; Joop Van Gerven
Journal:  Int J Methods Psychiatr Res       Date:  2014-02-05       Impact factor: 4.035

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.