AI Article Synopsis
- This study evaluated the synthetic cannabinoids NPB-22, Adamantyl-THPINACA, and CUMYL-4CN-B7AICA for their activities at cannabinoid receptors (CB1 and CB2) and their effects when inhaled, similar to smoking.
- Using binding assays and inhalation exposure tests on mice, the researchers measured the potency and biological effects of the cannabinoids, identifying the thermal degradation of their components when combusted.
- The results indicated that while NPB-22 and Adamantyl-THPINACA had similar CB activity in lab tests, NPB-22 exhibited weaker biological effects in inhalation tests due to thermal degradation, resulting in byproducts that lacked cannabinoid activity.
Article Abstract
Purpose: NPB-22 (quinolin-8-yl 1-pentyl-1H-indazole-3-carboxylate), Adamantyl-THPINACA (N-(1-adamantantyl)-1-[(tetrahydro-2H-pyran-4-yl)methyl]-1H-indazole-3-carboxamide), and CUMYL-4CN-B7AICA (1-(4-cyanobutyl)-N-(2-phenylpropan-2-yl)-1H- pyrrolo[2,3-b]pyridine-3-carboxamide), synthetic cannabinoids were evaluated in terms of CB (cannabinoid receptor type 1) and CB (cannabinoid receptor type 2) activities, and their biological effects when inhaled similar to cigarettes were examined.
Methods: The half maximal effective concentration values of the aforementioned synthetic cannabinoids at the CB and CB were investigated using [S]guanosine-5'-O-(3-thio)-triphosphate binding assays. In addition, their biological effects were evaluated using the inhalation exposure test with mice. The smoke generated was recovered by organic solvents in the midget impingers, and the thermal degradation compounds of the smoke components were identified and quantified using a liquid chromatography-photo diode array detector.
Results: NPB-22 and Adamantyl-THPINACA had equivalent CB activity in in vitro assays. Meanwhile, NPB-22 had a weaker biological effect on some items on the inhalation exposure test than Adamantyl-THPINACA. When analyzing organic solvents in the midget impingers, it was revealed that NPB-22 was degraded to 8-quinolinol and pentyl indazole 3-carboxylic acid by combustion. In addition, these degradation compounds did not have CB activity.
Conclusion: It was estimated that the biological effects of NPB-22 on the inhalation exposure test weakened because it underwent thermal degradation by combustion, and the resultant degradation compounds did not have any CB activity in vitro.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11269510 | PMC |
| http://dx.doi.org/10.1007/s11419-023-00679-5 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
In vivo assessment of the influence of general anaesthetics on transmembrane water cycling in the brain.
J Cereb Blood Flow Metab
December 2024
Department of Molecular Biotechnology and Health Sciences, University of Torino, Torino, Italy.
This study presents the first in vivo measurement of transcytolemmal water exchange in the brain using a novel Magnetic Resonance technique. We extend previous applications of Chemical Exchange Saturation Transfer (CEST) to examine water exchange across cellular membranes in late-stage chicken embryo brains. The immature blood-brain barrier at this stage allows Gadolinium-Based Contrast Agents (GBCAs) to penetrate the brain's interstitial space, sensitizing the CEST effect to water exchange between intra- and extracellular environments.
View Article and Find Full Text PDFHow I Treat AML relapse after allogeneic HCT.
Blood
December 2024
Dana-Farber Cancer Institute, BOSTON, Massachusetts, United States.
Allogeneic hematopoietic stem-cell transplantation (HCT) is one of the principal curative approaches in the treatment of acute myeloid leukemia (AML); however, relapse post-transplantation remains a catastrophic event with poor prognosis. The incidence of relapse has remained unchanged over the last three decades despite an evolving understanding of the immunobiology of the graft-versus leukemia effect and the immune escape mechanisms that lead to post-HCT relapse. The approach to post-transplant relapse is highly individualized and is dictated both by disease biology and genomics as well as the patient's clinical status at the time of relapse and the interval between relapse and transplantation.
View Article and Find Full Text PDFOptimization of adsorption performance by mesoporous materials developed from local clays and zeolite. Application in the treatment of real pharmaceutical effluents.
J Environ Sci Health B
December 2024
Laboratoire Génie Civil et d'Hydraulique, Université 8 Mai 1945, Guelma, Algeria.
The treatment of effluents from the pharmaceutical industry currently remains a major challenge due to their impact on the environment and public health along with the cost of treatments. Considering these issues, our work focused on the development of materials with effective adsorption properties to treat industrial effluents based on locally available and inexpensive clays and zeolite. Local Algerian kaolin (Djebel Debbagh), palygorskite (Ghoufi) and zeolite (Tinbdar) were treated thermally and chemically prior to synthesis into mesoporous materials of hexagonal structure using pluronic P123 as surfactant.
View Article and Find Full Text PDFA Novel Organophosphate Ester, Tris(2,4-di-butylphenyl) Phosphate, Induced Reproductive Toxicity in Male Zebrafish at Environmentally Relevant Concentrations.
Environ Sci Technol
December 2024
Institute of Hydrobiology, Chinese Academy of Sciences, Wuhan430072, China.
As a novel organophosphate ester (NOPE), tris(2,4-di-butylphenyl) phosphate (TDtBPP) has attracted significant attention due to its unexpectedly high detection in natural environments. However, the ecological toxic effects of environmentally relevant concentrations of TDtBPP in organisms remain entirely unknown. In this study, 1 month old zebrafish were exposed to 0, 50, 500, or 5000 ng/L TDtBPP for 150 days, and the reproductive toxicity in male fish was evaluated.
View Article and Find Full Text PDFEffective Bone Tissue Fabrication Using 3D-Printed Citrate-Based Nanocomposite Scaffolds Laden with BMP9-Stimulated Human Urine Stem Cells.
ACS Appl Mater Interfaces
December 2024
Molecular Oncology Laboratory, Department of Orthopedic Surgery and Rehabilitation Medicine, The University of Chicago Medical Center; Chicago, Illinois 60637, United States.
Effective repair of large bone defects through bone tissue engineering (BTE) remains an unmet clinical challenge. Successful BTE requires optimal and synergistic interactions among biocompatible scaffolds, osteogenic factors, and osteoprogenitors to form a highly vascularized microenvironment for bone regeneration and osseointegration. We sought to develop a highly effective BTE system by using 3D printed citrate-based mPOC/hydroxyapatite (HA) composites laden with BMP9-stimulated human urine stem cells (USCs).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!