79322-93-3Relevant articles and documents
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D4 Receptor Agonists with High Subtype Selectivity
Pirzer, Anna S.,Lasch, Roman,Friedrich, Heike,Hübner, Harald,Gmeiner, Peter,Heinrich, Markus R.
, p. 9658 - 9679 (2019)
Many subtype-selective dopamine receptor ligands developed for the D2-D4 family incorporate a 1-arylpiperazine-derived primary recognition motif, which is connected to a lipophilic moiety occupying an extended binding pocket (EBP) of the receptor via an aliphatic linker of variable lengths. The evaluation of a novel group of dopamine receptor ligands now showed that highly subtype-selective ligands [up to Ki(D4.4) = 0.25 nM, D2L/D4.4 = 320, D3/D4.4 = 710 for APH199 (17)] can be obtained by choosing a relatively large and conformationally flexible 1-benzyl-1-phenylsemicarbazide substructure to fill the EBP. The novel chemotype APH199 (17) was found to act as a full agonist at the D4 receptor showing significant bias toward G protein activation over β-arrestin recruitment in comparison to quinpirole.
Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers
Lee, Jie Eun,Koh, Hun Yeong,Seo, Seon Hee,Baek, Yi Yeon,Rhim, Hyewhon,Cho, Yong Seo,Choo, Hyunah,Pae, Ae Nim
scheme or table, p. 4219 - 4222 (2010/09/04)
T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives subs
Synthesis and pharmacology of 1-(4-aryl-1-piperazinyl-alkyl)-4-(4-methoxyphenyl) piperidine-2,6-diones: Tranquilizers
Samant,Kulkarni
, p. 692 - 694 (2007/10/02)
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