Evidence map›Paper›PMID 35056824›Full record

ArticleMolecules (Basel, Switzerland)2022

Identification of an Orally Bioavailable, Brain-Penetrant Compound with Selectivity for the Cannabinoid Type 2 Receptor.

Meirambek Ospanov, Suresh P Sulochana, Jason J Paris, John M Rimoldi, Nicole Ashpole, Larry Walker, Samir A Ross, Abbas G Shilabin, Mohamed A Ibrahim

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
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

1 citing paper in PubMed.

  1. Review
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.

Meirambek OspanovNational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.ORCID 0000-0002-9592-0138
Suresh P SulochanaDepartment of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, MS 38677, USA.ORCID 0000-0003-0665-9757
Jason J ParisDepartment of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, MS 38677, USA.ORCID 0000-0002-5628-1134
John M RimoldiDepartment of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, MS 38677, USA.
Nicole AshpoleDepartment of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, MS 38677, USA.
Larry WalkerNational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.
Samir A RossNational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.ORCID 0000-0002-3807-1299
Abbas G ShilabinDepartment of Chemistry, East Tennessee State University, Johnson City, TN 37614, USA.ORCID 0000-0003-3192-4233
Mohamed A IbrahimNational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, MS 38677, USA.ORCID 0000-0003-0257-860X

Funding

National Institute of Health P30GM122733
6 · The paper itself

Abstract

Modulation of the endocannabinoid system (ECS) is of great interest for its therapeutic relevance in several pathophysiological processes. The CB2 subtype is largely localized to immune effectors, including microglia within the central nervous system, where it promotes anti-inflammation. Recently, a rational drug design toward precise modulation of the CB2 active site revealed the novelty of Pyrrolo[2,1-c][1,4]benzodiazepines tricyclic chemotype with a high conformational similarity in comparison to the existing leads. These compounds are structurally unique, confirming their chemotype novelty. In our continuing search for new chemotypes as selective CB2 regulatory molecules, following SAR approaches, a total of 17 selected (S,E)-11-[2-(arylmethylene)hydrazono]-PBD analogs were synthesized and tested for their ability to bind to the CB1 and CB2 receptor orthosteric sites. A competitive [

Indexed as

Drug DesignAdministration, OralAnimalsBenzodiazepinesBinding SitesBrainEndocannabinoidsKidneyLigandsLiverMaleMiceModels, MolecularPyrrolesReceptors, CannabinoidStructure-Activity RelationshipBenzodiazepinesEndocannabinoidsLigandsPyrrolespyrrolo(2,1-c)(1,4)benzodiazepineReceptors, Cannabinoidcannabinoid receptors CB1/CB2central nervous system (CNS)neurodegenerative diseasesneuroinflammationpharmacokinetics (PK)pyrrolobenzodiazepinesradioligand binding assay

Identifiers

PMID35056824
PMCPMC8778670

What OpenQuestion holds

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Registered trials

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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.