102392-05-2Relevant articles and documents
Synthesis, preclinical evaluation and molecular modelling of macrocyclic appended 1-(2-methoxyphenyl)piperazine for 5-HT1A neuroreceptor imaging
Hazari, Puja Panwar,Prakash, Surbhi,Meena, Virendra Kumar,Singh, Niraj,Chuttani, Krishna,Chadha, Nidhi,Singh, Pooja,Kukreti, Shrikant,Mishra, Anil Kumar
, p. 7288 - 7301 (2016)
5-HT1A receptors are known to be implicit in a number of neuropsychiatric fluctuations related to mood and anxiety. Their visualization in the human brain using PET, SPECT or MRI is of great importance in the management and treatment of neurolo
Synthesis and radiolabelling of [123I]-4-iodo-N-(4-(4-(2-methoxyphenyl)-piperazin-1-yl) butyl)-benzamide, a potential dopamine D3 antagonist for SPECT studies
Staelens,Dumont,De Vos,Oltenfreiter,Vandecapelle,Dierckx,Slegers
, p. 297 - 305 (2003)
Schizophrenia is a devastating mental disorder characterized by relapsing psychotic episodes accompanied with emotional, professional and social decline. The classical dopamine hypothesis of schizophrenia postulates that hyperactivity of dopaminergic neur
Photochromic Dopamine Receptor Ligands Based on Dithienylethenes and Fulgides
Lachmann, Daniel,Studte, Carolin,M?nnel, Barbara,Hübner, Harald,Gmeiner, Peter,K?nig, Burkhard
, p. 13423 - 1343 (2017)
We describe the incorporation of the well-investigated class of photochromic dithienylethenes (DTEs) and fulgides into known dopamine receptor ligands such as 1,4-disubstituted aromatic and hydroxybenzoxazinone piperazines as well as aminoindanes. Subtype
Synthesis, in silico, and in vitro studies of novel dopamine D2 and D3 receptor ligands
Elek, Milica,Djokovic, Nemanja,Frank, Annika,Oljacic, Slavica,Zivkovic, Aleksandra,Nikolic, Katarina,Stark, Holger
, (2021/02/26)
Dopamine is an important neurotransmitter in the human brain and its altered concentrations can lead to various neurological diseases. We studied the binding of novel compounds at the dopamine D2 (D2R) and D3 (D3/sub
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 (2019/11/13)
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.