Evidence map›Paper›PMID 23731016›Full record

ArticleACS chemical neuroscience2013

Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors.

Micah J Niphakis, Armand B Cognetta, Jae Won Chang, Matthew W Buczynski, Loren H Parsons, Frederika Byrne, James J Burston, Victoria Chapman, Benjamin F Cravatt

Abstract read
In one paragraph

Article in ACS chemical neuroscience, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 90 papers.

0numbers the graph read from it
0cells of the map it votes in
90citing papers in PubMed
9.3field-weighted citation impact, top 2% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

90 citing papers in PubMed, 147 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Article
  5. Article
  6. The Pharmacological Profile of Plant-Derived Cannabinoids In Vitro.Current topics in behavioral neurosciences · 2026
    Review
  7. Article
  8. Article
  9. Article
  10. Article
  11. Article
  12. Review
  13. Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. Function of Presynaptic Inhibitory Cannabinoid CBInternational journal of molecular sciences · 2024
    Article
  19. Article
  20. Article

30 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 3 institutions in 2 countries.

Micah J NiphakisThe Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92037, United States.
Armand B Cognetta
Jae Won Chang
Matthew W Buczynski
Loren H Parsons
Frederika Byrne
James J Burston
Victoria Chapman
Benjamin F Cravatt
Scripps Research Institute · USQueen's Medical Centre · GBUniversity of Nottingham · GB

Funding

STRUCTURAL STUDIES OF FAAHP01DA017259 · NIDA · SCRIPPS RESEARCH INSTITUTE, THE · PI CRAVATT, BENJAMIN F · 2004 to 2013
$10.6M
CHEMOPROTEOMIC METHODS FOR SERINE HYDROLASE INHIBITOR DEVELOPMENTR01DA033760 · NIDA · SCRIPPS RESEARCH INSTITUTE, THE · PI CRAVATT, BENJAMIN F, SCAMPAVIA, LOUIS DANIEL · 2012 to 2021
$5.1M
Alcohol dependence and brain endocannabinoid functionR01AA020404 · NIAAA · SCRIPPS RESEARCH INSTITUTE, THE · PI MARTIN-FARDON, REMI · 2011 to 2015
$2.2M
Monoacylglycerol Lipase Inhibitors for Treating Opioid Use Disorders (RO)R01DA032933 · NIDA · SCRIPPS RESEARCH INSTITUTE, THE · PI CRAVATT, BENJAMIN F, LICHTMAN, ARON H · 2012 to 2014
$1.5M
Effect of nicotine self-administration on endocannabinoids & related lipidsF32DA029994 · NIDA · SCRIPPS RESEARCH INSTITUTE, THE · PI BUCZYNSKI, MATTHEW WALLACE · 2011 to 2013
$161k
Chemical probes to assess endocannabinoid localization, storage, and transportF32DA032541 · NIDA · SCRIPPS RESEARCH INSTITUTE, THE · PI NIPHAKIS, MICAH JAMES · 2011 to 2013
$155k
Biotechnology and Biological Sciences Research CouncilNIAAA NIH HHS R01 AA020404NIDA NIH HHS DA017259NIDA NIH HHS DA032541NIDA NIH HHS DA032933NIDA NIH HHS DA033760NIDA NIH HHS F32 DA029994NIDA NIH HHS P01 DA017259NIDA NIH HHS R01 DA032933NIDA NIH HHS R01 DA033760
6 · The paper itself

Abstract

Monoacylglycerol lipase (MAGL) is a principal metabolic enzyme responsible for hydrolyzing the endogenous cannabinoid (endocannabinoid) 2-arachidonoylglycerol (2-AG). Selective inhibitors of MAGL offer valuable probes to further understand the enzyme's function in biological systems and may lead to drugs for treating a variety of diseases, including psychiatric disorders, neuroinflammation, and pain. N-Hydroxysuccinimidyl (NHS) carbamates have recently been identified as a promising class of serine hydrolase inhibitors that shows minimal cross-reactivity with other proteins in the proteome. Here, we explore NHS carbamates more broadly and demonstrate their potential as inhibitors of endocannabinoid hydrolases and additional enzymes from the serine hydrolase class. We extensively characterize an NHS carbamate 1a (MJN110) as a potent, selective, and in-vivo-active MAGL inhibitor. Finally, we demonstrate that MJN110 alleviates mechanical allodynia in a rat model of diabetic neuropathy, marking NHS carbamates as a promising class of MAGL inhibitors.

Indexed as

AmidohydrolasesAnimalsBlood GlucoseBrainCarbamatesDiabetes Mellitus, Type 2Diabetic NeuropathiesDrug Evaluation, PreclinicalEndocannabinoidsFatty Acid Amide HydrolasesHEK293 CellsHumansHyperalgesiaInsulinLiverMaleAmidohydrolasesBlood GlucoseCarbamatesEndocannabinoidsFatty Acid Amide HydrolasesInsulinMJN110MJN110yneMonoacylglycerol LipasesN-hydroxysuccinimideSuccinimides

Identifiers

PMID23731016
PMCPMC3778430
OpenAlexW2040580317

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.