P2X purinergic receptor ligands: recently patented compounds
MetadataShow full item record
Importance of the field: P2X channels are ionotropic purinergic receptors that are currently under scrutiny as attractive targets for novel therapeutics in areas including chronic inflammation, pain and depression. Their wide expression in the CNS, recent advances in the biochemical and pharmacological properties as well as increasing numbers of patents published in this research domain demand a review in this field. Areas covered in this review: The patent literature covering novel drug-like antagonists for each P2X receptor subtype (P2X1R to P2X7R) up to December 2009 is described in this review article together with their recent highlights in pharmacology. What the reader will gain: Readers will gain an up-to-date overview of patents covering drug-like antagonists for seven P2X receptor subtypes within the last 4 years. Take home message: P2X7R antagonists and other P2X inhibitors will probably be on the market for combating rheumatoid arthritis and other diseases. Some P2X7R antagonists are already in Phase I and II clinical trials.
Showing items related by title, author, creator and subject.
The significance of 2-furyl ring substitution with a 2-(para-substituted) aryl group in a new series of pyrazolo-triazolo-pyrimidines as potent and highly selective hA3 adenosine receptors antagonists: new insights into structure-affinity relationship and receptor-antagonist recognitionCheong, S.; Dolzhenko, A.; Kachler, S.; Paoletta, S.; Federico, S.; Cacciari, B.; Dolzhenko, Anton; Klotz, K.; Moro, S.; Spalluto, G.; Pastorin, G. (2010)Among the heterocyclic structures identified as potent human A3 (hA3) adenosine receptor’s antagonists, we have demonstrated that the new pyrazolo-triazolo-pyrimidines, bearing an aryl group in replacement of the C2-furyl ...
Sperm gamma-Aminobutyric acid type A receptor delta subunit (GABRD) and its interaction with purinergic P2X<inf>2</inf>receptors in progesterone-induced acrosome reaction and male fertilityXu, W.; Wang, K.; Chen, Yan; Liang, X.; Yu, M.; Yue, H.; Tierney, M. (2017)© CSIRO 2017. The mechanism underlying the non-genomic action of progesterone in sperm functions and related Ca2+ mobilisation remains elusive. Herein we report the expression of gamma-Aminobutyric acid type A receptor ...
The effects of maternally administered methadone, buprenorphine and naltrexone on offspring: Review of human and animal dataFarid, W.; Dunlop, S.; Tait, Robert; Hulse, G. (2008)Most women using heroin are of reproductive age with major risks for their infants. We review clinical and experimental data on fetal, neonatal and postnatal complications associated with methadone, the current "gold ...