253196-37-1Relevant academic research and scientific papers
Synthesis of GluN2A-selective NMDA receptor antagonists with an electron-rich aromatic B-ring
Rajan, Remya,Schepmann, Dirk,Schreiber, Julian A.,Seebohm, Guiscard,Wünsch, Bernhard
, (2020/11/13)
Glutamatergic N-Methyl-D-aspartate (NMDA) receptors are heterotetrameric ion channels that can be comprised of different subunits. GluN2A subunit-containing NMDA receptors are associated with diseases like anxiety, depression, and schizophrenia. However,
PYRAZOLE COMPOUNDS AND USE THEREOF
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Page/Page column 34, (2009/05/29)
The pyrazole compound of the present invention is represented by the following general formula (I). The pyrazole compound of the present invention or a salt thereof or a solvate thereof potently inhibits liver glycogen phosphorylase, and, therefore, is useful as a therapeutic or prophylactic agent for diabetes. wherein each symbol denotes as described in the specifications.
Novel Compounds
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Page/Page column 73; 75, (2008/06/13)
There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.
Synthesis and pharmacological profile of a series of 2,5-substituted-N,N-dimethyltryptamine derivatives as novel antagonists for the vascular 5-HT1B-like receptor
Moloney, Gerard P.,Martin, Graeme R.,Mathews, Neil,Hobbs, Heather,Dodsworth, Susan,Sang, Pang Yih,Knight, Cameron,Maxwell, Miles,Glen, Robert C.
, p. 2713 - 2723 (2007/10/03)
The coronary 5-HT1B-like receptor has been implicated in vasospasm and it is postulated that a 5-HT1B-like antagonist may block the detrimental action of 5-HT whilst not interfering with normal blood vessel function. The synthesis and pharmacological profile of a novel series of 2-(N-heteroaryl)carboxamido-5-substituted-N,N-dimethyltryptamine derivatives as silent (as judged by the inability of angiotensin II to unmask 5-HT1B-like receptor mediated agonist activity in the rabbit femoral artery), competitive and selective 5-HT1B-like receptor antagonists is described. Modifications to the 2-carboxamido sidechain as well as the 5-ethylene linked heterocycle are explored. N-Furfuryl-5-[2-(N-phthalimido)ethyl]-3-[2-(dimethylamino)ethyl]-1H-indole-2- carboxamide (34) was discovered which fulfilled our in vitro selection criteria and which had a favourable pharmacokinetic profile. Compound 34 showed good affinity (pKB = 7.38) for the vascular 5-HT1B-like receptor and greater than 125 fold selectivity over α1-adrenoceptor affinity. The selectivity of 34 and related compounds for the 5-HT1B-like receptor over other receptor subtypes is discussed and a mode of binding for this class of compound to a pharmacophore model is proposed. The Royal Society of Chemistry 1999.
