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Tetrahydrocanabinol

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https://www.readbyqxmd.com/read/29204742/target-and-tissue-selectivity-prediction-by-integrated-mechanistic-pharmacokinetic-target-binding-and-quantitative-structure-activity-modeling
#1
Anna H C Vlot, Wilhelmus E A de Witte, Meindert Danhof, Piet H van der Graaf, Gerard J P van Westen, Elizabeth C M de Lange
Selectivity is an important attribute of effective and safe drugs, and prediction of in vivo target and tissue selectivity would likely improve drug development success rates. However, a lack of understanding of the underlying (pharmacological) mechanisms and availability of directly applicable predictive methods complicates the prediction of selectivity. We explore the value of combining physiologically based pharmacokinetic (PBPK) modeling with quantitative structure-activity relationship (QSAR) modeling to predict the influence of the target dissociation constant (K D) and the target dissociation rate constant on target and tissue selectivity...
December 4, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28803323/effect-of-footshock-stress-on-place-conditioning-produced-by-%C3%AE-9-tetrahydrocannabinol-and-the-fatty-acid-amide-hydrolase-faah-inhibitor-urb597-in-sprague-dawley-rats
#2
Marieka V DeVuono, Kiri L Wills, Danielle V MacPherson, Kelly M Hrelja, Linda A Parker
RATIONALE: Unlike other drugs of abuse, Δ(9)-tetrahydrocanabinol (THC) is generally aversive in rodent conditioned place preference models, but little is known about how stress may modify THC affective properties. OBJECTIVE: We evaluate the potential of footshock stress to enhance the rewarding effects of THC and the fatty acid amide hydrolase inhibitor, URB597, as it has been shown to enhance their anxiolytic effects. MATERIALS AND METHODS: The effect of footshock stress 24 h prior to each conditioning trial on the rewarding/aversive effects of THC (1, 0...
November 2017: Psychopharmacology
https://www.readbyqxmd.com/read/26733534/adolescent-cannabinoid-exposure-induces-a-persistent-sub-cortical-hyper-dopaminergic-state-and-associated-molecular-adaptations-in-the-prefrontal-cortex
#3
Justine Renard, Laura G Rosen, Michael Loureiro, Cleusa De Oliveira, Susanne Schmid, Walter J Rushlow, Steven R Laviolette
Considerable evidence suggests that adolescent exposure to delta-9-tetrahydrocanabinol (THC), the psychoactive component in marijuana, increases the risk of developing schizophrenia-related symptoms in early adulthood. In the present study, we used a combination of behavioral and molecular analyses with in vivo neuronal electrophysiology to compare the long-term effects of adolescent versus adulthood THC exposure in rats. We report that adolescent, but not adult, THC exposure induces long-term neuropsychiatric-like phenotypes similar to those observed in clinical populations...
February 1, 2017: Cerebral Cortex
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