Klunk, William E. published the artcileUncharged thioflavin-T derivatives bind to amyloid-beta protein with high affinity and readily enter the brain, Application of 2-(4-Aminophenyl)-6-methylbenzothiazole, the publication is Life Sciences (2001), 69(13), 1471-1484, database is CAplus and MEDLINE.
In vivo assessment of the beta-sheet proteins deposited in amyloid plaques (Aβ peptide) or neurofibrillary tangles (tau protein) presents a target for the development of biol. markers for Alzheimer’s disease (AD). In an effort to develop in vivo beta-sheet imaging probes, derivatives of thioflavin-T (ThT) were synthesized and evaluated. These compounds lack the pos. charged quaternary heterocyclic nitrogen of ThT and are therefore uncharged at physiol. pH. They are 600-fold more lipophilic than ThT. These ThT derivatives bind to Aβ(1-40) fibrils with higher affinity (Ki = 20.2 nM) than ThT (Ki = 890 nM). The uncharged ThT derivatives stained both plaques and neurofibrillary tangles in post-mortem AD brain, showing some preference for plaque staining. A carbon-11 labeled compound, [N-methyl-11C]6-Me-BTA-1, was prepared, and its brain entry and clearance were studied in Swiss-Webster mice. This compound entered the brain at levels comparable to commonly used neuroreceptor imaging agents (0.223% ID-kg/g or 7.61% ID/g at 2 min post-injection) and showed good clearance of free and non-specifically bound radioactivity in normal rodent brain tissue (brain clearance t1/2 = 20 min). The combination of relatively high affinity for amyloid, specificity for staining plaques and neurofibrillary tangles in post-mortem AD brain, and good brain entry and clearance makes [N-methyl-11C]6-Me-BTA-1 a promising candidate as an in vivo positron emission tomog. (PET) beta-sheet imaging agent.
Life Sciences published new progress about 92-36-4. 92-36-4 belongs to thiazole, auxiliary class Organic Pigment, name is 2-(4-Aminophenyl)-6-methylbenzothiazole, and the molecular formula is C14H12N2S, Application of 2-(4-Aminophenyl)-6-methylbenzothiazole.
Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica