Objective: In this study we investigated the effect of CGS 21680 (2-p-(2-Carboxyethyl)phenethylamino-5-N-ethylcarboxamidoadenosine hydrochloride), an adenosine A2A receptor agonist, in a model of dextran sulphate sodium (DSS)-induced colitis.

Methods: NMRI mice were fed 5 % (w/v) DSS, and were treated intraperitoneally with 0.5 mg/kg CGS 21680 or vehicle for 10 days. Changes of bodyweight, colon length, the incidence of rectal bleeding, levels of macrophage inflammatory protein (MIP)-1alpha, MIP-2, interferon gamma, interleukin (IL)-1beta, IL-12 and tumour necrosis factor-alpha from homogenates of colon biopsies, and the release of [3H]acetylcholine (ACh) from longitudinal muscle strip were determined.

Results: DSS significantly decreased bodyweight, colon length, and it increased the incidence of rectal bleeding and levels of MIP-1alpha, MIP-2 and IL-1beta compared to DSS-untreated animals. CGS 21680 had no effect on these changes. No change could be observed in release of ACh in DSS-induced colitis with or without CGS 21680.

Conclusion: In summary, CGS 21680 is ineffective in ameliorating DSS-induced colitis in mice.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2225471PMC
http://dx.doi.org/10.1007/s00011-006-6150-7DOI Listing

Publication Analysis

Top Keywords

cgs 21680
20
adenosine a2a
8
a2a receptor
8
receptor agonist
8
colitis mice
8
bodyweight colon
8
colon length
8
incidence rectal
8
rectal bleeding
8
bleeding levels
8

Similar Publications

CGS-21680 defers cisplatin-induced AKI-CKD transition in C57/BL6 mice.

Chem Biol Interact

November 2024

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt. Electronic address:

Acute kidney injury (AKI), with a high mortality and morbidity, is known as a risk factor for developing progressive chronic kidney disease (CKD). Targeting transition of AKI to CKD displays an excellent therapeutic potential. This study aims at investigating the role of CGS-21680, selective A2AR agonist, in deferring Cis-induced AKI-CKD transition.

View Article and Find Full Text PDF

AR regulate inflammation through PKA/NF-κB signaling pathways in intervertebral disc degeneration.

Eur J Med Res

August 2024

Department of Spine Surgery, Wuhan Fourth Hospital, Hanzheng Street, 473#, QiaoKou District, Wuhan, 430033, China.

Background: Reduction of inflammatory damage and inhibition of nucleus pulposus (NP) apoptosis are considered to be the main effective therapy idea to reverse the intervertebral disc degeneration (IDD) and alleviate the chronic low back pain. The adenosine A2A receptor (A2AR), as a member of G protein-coupled receptor families, plays an important role in the anti-inflammation and relieving pain. So far, the impact of A2AR on IDD therapy is unclear.

View Article and Find Full Text PDF
Article Synopsis
  • Myocardial inflammation and cell death caused by cirrhosis contribute significantly to cirrhotic cardiomyopathy, with CD73 playing a potential role in these processes.
  • In a mouse model of cirrhotic cardiomyopathy, researchers manipulated CD73 levels and observed its effects on heart function, inflammation, and cell death in the myocardium.
  • The findings suggest that the increased expression of CD73 and activation of the A2A receptor help reduce inflammation and apoptosis in heart tissue by inhibiting the NF-κB pathway, providing insights into potential therapeutic targets.
View Article and Find Full Text PDF

Adenosine A2A receptor activation regulates the M1 macrophages activation to initiate innate and adaptive immunity in psoriasis.

Clin Immunol

September 2024

Department of Dermatology, Xiangya Hospital, Central South University, Changsha, China; Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South University, Changsha, China. Electronic address:

Psoriasis is a common inflammatory systemic disease characterized by pro-inflammatory macrophages activation (M1 macrophage) infiltrated in the dermal layer. How M1 macrophage contributes to psoriasis remains unknown. In this study, we found that adenosine A2A receptor (A2AR) agonist CGS 21680 HCl alleviated the imiquimod (IMQ) and mouse IL-23 Protein (rmIL-23)-induced psoriasis inflammation through reducing infiltration of M1.

View Article and Find Full Text PDF
Article Synopsis
  • - CBD is a phytocannabinoid that shows potential for treating various diseases and operates through cannabinoid and other receptors, including the adenosine A receptor.
  • - In lab experiments using CHO cells, CBD could not bind to the A receptor in the same way as a certain fluorescent probe but did influence the receptor’s response to a known agonist.
  • - The findings imply that CBD acts as a negative allosteric modulator of the adenosine A receptor, meaning it can inhibit the receptor’s function without directly competing for the binding site.
View Article and Find Full Text PDF

Want 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!