96530-59-5Relevant articles and documents
FLUORESCENT SYSTEMS FOR BIOLOGICAL IMAGING AND USES THEREOF
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Page/Page column 26; 28-29, (2021/02/12)
The invention relates to compounds of formula I, in which Y, Ar1, Ar2, X, R1 and R2 are defined herein, and to their use in a variety of biological imaging techniques and therapeutic methods. In aspects, the invention relates to conjugates comprising the compounds of formula I and their associated uses and therapeutic uses.
Cellular localisation of structurally diverse diphenylacetylene fluorophores
Adams, Candace,Ambler, Carrie A.,Bain, Angus J.,Blacker, Thomas S.,Callaghan, Daniel,Chisholm, David R.,Girkin, John M.,Hughes, Joshua G.,Humann, Rachel,Lembicz, Nicola K.,Pujol, Alba,Whiting, Andrew
, p. 9231 - 9245 (2020/12/03)
Fluorescent probes are increasingly used as reporter molecules in a wide variety of biophysical experiments, but when designing new compounds it can often be difficult to anticipate the effect that changing chemical structure can have on cellular localisa
Structural modifications of neuroprotective anti-parkinsonian (-)-N6-(2-(4-(biphenyl-4-yl)piperazin-1-yl)-ethyl)-N6-propyl-4,5,6, 7-tetrahydrobenzo[d]thiazole-2,6-diamine (D-264): An effort toward the improvement of in vivo efficacy of the parent molecule
Modi, Gyan,Antonio, Tamara,Reith, Maarten,Dutta, Aloke
, p. 1557 - 1572 (2014/03/21)
In our overall goal to develop multifunctional dopamine D 2/D3 agonist drugs for the treatment of Parkinson's disease (PD), we previously synthesized potent D3 preferring agonist D-264 (1a), which exhibited neuroprotective properties in two animal models of PD. To enhance the in vivo efficacy of 1a, a structure-activity relationship study was carried out. Competitive binding and [35S]GTPγS functional assays identified compound (-)-9b as one of the lead molecules with preferential D3 agonist activity (EC50(GTPγS); D3 = 0.10 nM; D2/D3 (EC50): 159). Compounds (-)-9b and (-)-8b exhibited high in vivo activity in two PD animal models, reserpinized and 6-hydroxydopamine (OHDA)-induced unilateral lesioned rats. On the other hand, 1a failed to show any in vivo activity in these models unless the compound was dissolved in 5-10% beta-hydroxy propyl cyclodextrin solution. Lead compounds exhibited appreciable radical scavenging activity. In vitro experiments with dopaminergic MN9D cells indicated neuroprotection by both 1a and (-)-9b from toxicity of MPP+.