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In vivo evaluation of 11CTMI, a COX-2 selective PET tracer, in baboons.
The objective of this study is to evaluate [11C]TMI, a selective COX-2 inhibitor (Ki ≤ 1 nM) in nonhuman primates using PET imaging. PET imaging in baboons showed that [11C]TMI penetrates the blood brain barrier (BBB) and accumulates in brain in a somewhat heterogeneous pattern. Metabolite analyses indicated that [11C]TMI undergoes no significant metabolism of parent tracer in the plasma for baseline scans, however a relative faster metabolism was found for blocking scan. All the tested quantification approaches provide comparable tracer total distribution volume (VT) estimates in the range of 3.2-7 (mL/cm3). We ...
Source: Bioorganic and Medicinal Chemistry Letters - October 31, 2018 Category: Chemistry Authors: Kumar JSD, Zanderigo F, Prabhakaran J, Rubin-Falcone H, Parsey RV, Mann JJ Tags: Bioorg Med Chem Lett Source Type: research

Evaluation of 11CTMI as a COX-2 selective PET tracer in baboon
Conclusion: Our PET imaging studies in baboon show that [11C]TMI penetrates the BBB and distributes to COX-2 enriched brain regions. Details of the in vivo evaluation of [11C]TMI in baboon brain will be presented. References 1. Majo VJ et al., Bioorg Med Chem Let., 2005, 15, 4268. 2. Cunningham VJ et al., J Cereb Blood Flow Metab., 2010; 30(1): 46-50. Grant Support: Diane Goldberg Foundation (NYSPI/CUMC) and Pfizer Inc.
Source: Journal of Nuclear Medicine - May 23, 2018 Category: Nuclear Medicine Authors: Kumar, D., Zanderigo, F., Prabhakaran, J., Rubin-Falcone, H., Parsey, R., Mann, J. J. Tags: Neuroscience - Basic Science - Posters Source Type: research

Celecoxib for rheumatoid arthritis.
CONCLUSIONS: Celecoxib may improve clinical symptoms, alleviate pain and contribute to little or no difference in physical function compared with placebo. Celecoxib was associated with fewer numbers of participant withdrawals. Results for incidence of gastroduodenal ulcers (≥ 3 mm) and short-term serious adverse events were uncertain; however, there were few reported events for either.Celecoxib may slightly improve clinical symptoms compared with tNSAIDs. Results for reduced pain and improved physical function were uncertain. Particpants taking celecoxib had lower incidence of gastroduodenal ulcers (≥ 3 mm) and there w...
Source: Cochrane Database of Systematic Reviews - June 9, 2017 Category: General Medicine Authors: Fidahic M, Jelicic Kadic A, Radic M, Puljak L Tags: Cochrane Database Syst Rev Source Type: research