645403-23-2Relevant academic research and scientific papers
ADAMANTANYL-SUBSTITUTED BENZAMIDE COMPOUNDS AND THEIR USE AS P2X7 RECEPTOR ANTAGONISTS
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Page/Page column 20; 23-24, (2020/03/15)
The present invention relates to adamantanyl-substituted benzamide compounds and their use as antagonists of the P2X7 purinoreceptor. The invention further relates to methods for the treatment of disease and conditions associated with the P2X7 purinoreceptor.
The first cns-active carborane: A novel p2x7 receptor antagonist with antidepressant activity
Wilkinson, Shane M.,Gunosewoyo, Hendra,Barron, Melissa L.,Boucher, Aurelie,McDonnell, Michelle,Turner, Peter,Morrison, Daniel E.,Bennett, Maxwell R.,McGregor, Iain S.,Rendina, Louis M.,Kassiou, Michael
, p. 335 - 339 (2014/06/09)
Relative to other polycyclic frameworks (1-3), a carborane cage (4 and Cs·5) exerts a significant biological effect as an inhibitor of the purinergic P2X7 receptor (P2X7R) which allows one to target depression in vivo and thus demonstrate, for the first time, that a carborane has the capacity to modify CNS activity.
POLYCYCLIC MOLECULAR COMPOUNDS
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Page/Page column 61-63, (2008/12/06)
This invention relates to compounds of Formula (I), wherein A is a carboaromatic or heteroaromatic ring having one or more substituents; R6 Formula (A) is optionally substituted with one or more substituents; and n is 0, 1 or an integer greater than 1 and when n is 1 or greater the bond or bonds between the carbon atoms may be saturated or unsaturated, which bind the P2X7 receptor with high affinity. This invention also relates to methods for the diagnosis, treatment or monitoring of disorders in which the P2X7 receptor is implicated, in particular the diagnosis, treatment or monitoring of (the progression of) neuroinflammatory and neurodegenerative disorders in a subject.
Cubyl amides: Novel P2X7 receptor antagonists
Gunosewoyo, Hendra,Guo, Jun Liu,Bennett, Maxwell R.,Coster, Mark J.,Kassiou, Michael
supporting information; experimental part, p. 3720 - 3723 (2009/04/06)
Polycyclic amides 2 and 5-9 were successfully synthesised and their lipophilicity profiles were evaluated using reverse-phase HPLC. All synthesised compounds possessed P2X7R antagonistic properties when tested on rat spinal cord microglia cells. Extensive screening for binding to other neuroreceptor subtypes demonstrated their P2X7 selectivity.
Hit-to-Lead studies: The discovery of potent adamantane amide P2X 7 receptor antagonists
Baxter, Andrew,Bent, Janice,Bowers, Keith,Braddock, Martin,Brough, Steve,Fagura, Malbinder,Lawson, Mandy,McInally, Tom,Mortimore, Mike,Robertson, Mark,Weaver, Richard,Webborn, Peter
, p. 4047 - 4050 (2007/10/03)
A Hit-to-Lead optimisation programme was carried out on the adamantane high throughput screening hit 1 resulting in the discovery of a number of potent P2X7 antagonists.
