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Open AccessJournal ArticleDOI

Monohydroxylated metabolites of the K2 synthetic cannabinoid JWH-073 retain intermediate to high cannabinoid 1 receptor (CB1R) affinity and exhibit neutral antagonist to partial agonist activity

Lisa K. Brents, +7 more
- 01 Apr 2012 - 
- Vol. 83, Iss: 7, pp 952-961
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TLDR
The present study indicates that further work examining the physiological effects of synthetic cannabinoid metabolism is warranted, and suggests that a complex mix of metabolically produced CB1R ligands may contribute to the adverse effect profile of JWH-073-containing products.
About: 
This article is published in Biochemical Pharmacology.The article was published on 2012-04-01 and is currently open access. It has received 138 citations till now. The article focuses on the topics: JWH-073 & Cannabinoid.

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Citations
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Journal ArticleDOI

Spice drugs are more than harmless herbal blends: a review of the pharmacology and toxicology of synthetic cannabinoids

Kathryn A. Seely, +3 more
- 03 Dec 2012 - 
TL;DR: A review of the legal status of common synthetic cannabinoids detected in Spice and analytical procedures used to test Spice products and human specimens collected under a variety of clinical circumstances is provided in this paper.
Journal ArticleDOI

Spicing things up: synthetic cannabinoids

Max Spaderna, +2 more
- 09 Jul 2013 - 
TL;DR: There is an urgent need for better research on the effects of synthetic cannabinoids to help clinicians manage adverse events and to better understand cannabinoid pharmacology in humans.
Journal ArticleDOI

Distinct pharmacology and metabolism of K2 synthetic cannabinoids compared to Δ9-THC: Mechanism underlying greater toxicity?

William E. Fantegrossi, +3 more
- 27 Feb 2014 - 
TL;DR: Evidence reported in this mini-review suggests that K2 products are neither safe nor legal alternatives to marijuana, and suggests that distinct pharmacological properties and metabolism of SCBs relative to Δ(9)-THC may contribute to the observed toxicity.
Journal ArticleDOI

Adverse Effects of Synthetic Cannabinoids: Management of Acute Toxicity and Withdrawal

Ziva D. Cooper
- 14 Apr 2016 - 
TL;DR: A background of the pharmacology of SCs, recent findings of adverse effects associated with both acute intoxication and withdrawal as a consequence of daily use, and treatment approaches that have been implemented to address these issues are provided, with an emphasis on pharmacotherapies for managing detoxification.
Journal ArticleDOI

Detection and Activity Profiling of Synthetic Cannabinoids and Their Metabolites with a Newly Developed Bioassay.

Annelies Cannaert, +4 more
- 07 Nov 2016 - 
TL;DR: A new G-protein coupled receptor (GPCR) activation assay based on NanoLuc binary technology is developed and applied, and it is demonstrated that several major metabolites of these SCs retain their activity at cannabinoid receptors.
References
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Journal ArticleDOI

Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.

Yung-Chi Cheng, +1 more
- 01 Dec 1973 - 
TL;DR: The analysis described shows K I does not equal I 50 when competitive inhibition kinetics apply; however, K I is equal to I 50 under conditions of either noncompetitive or uncompetitive kinetics.
Journal ArticleDOI

Human Cannabinoid Pharmacokinetics

Marilyn A. Huestis
- 01 Aug 2007 - 
TL;DR: The cardiovascular and subjective effects of cannabis are blocked by rimonabant, the first CB-1 cannabinoid-receptor antagonist, documenting thatCB-1 receptors mediate these effects of smoked cannabis in humans.
Journal ArticleDOI

Endocannabinoid control of food intake and energy balance

Vincenzo Di Marzo, +1 more
- 01 May 2005 - 
TL;DR: The multifaceted regulation of energy homeostasis by endocannabinoids is discussed, together with its applications to the treatment of eating disorders and metabolic syndromes.
Journal ArticleDOI

'Spice' and other herbal blends: harmless incense or cannabinoid designer drugs?

Volker Auwärter, +5 more
- 01 May 2009 - 
Book ChapterDOI

Pharmacological actions of cannabinoids.

Roger G. Pertwee
- 01 Jan 2005 - 
TL;DR: More information is beginning to emerge about the pharmacological actions of the non-psychoactive plant cannabinoid, cannabidiol, as well as acting on CB1 and CB2 receptors, and there is convincing evidence that anandamide can activate transient receptor potential vanilloid type 1 (TRPV1) receptors.
Related Papers (5)

'Spice' and other herbal blends: harmless incense or cannabinoid designer drugs?

Volker Auwärter, +5 more
- 01 May 2009 - 

Spice drugs are more than harmless herbal blends: a review of the pharmacology and toxicology of synthetic cannabinoids

Kathryn A. Seely, +3 more
- 03 Dec 2012 - 

Spice drugs as a new trend: Mode of action, identification and legislation

Ioanna Vardakou, +2 more
- 01 Sep 2010 - 

Acute toxicity due to the confirmed consumption of synthetic cannabinoids: clinical and laboratory findings

Maren Hermanns-Clausen, +3 more
- 01 Mar 2013 - 

Influence of the N-1 alkyl chain length of cannabimimetic indoles upon CB1 and CB2 receptor binding

Mie Mie Aung, +8 more
- 01 Aug 2000 - 
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Q1. What contributions have the authors mentioned in the paper "Monohydroxylated metabolites of the k2 synthetic cannabinoid jwh-073 retain intermediate to high cannabinoid 1 receptor (cb1r) affinity and exhibit neutral antagonist to partial agonist activity" ?

In conclusion, the present study indicates that further work examining the physiological effects of synthetic cannabinoid metabolism is warranted. This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to their customers the authors are providing this early version of the manuscript. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.