Synthesis and biological evaluation of 99mTc, Re-monoamine-monoamide conjugated to 2-(4-aminophenyl)benzothiazole as potential probes for beta-amyloid plaques in the brain

Bioorganic & Medicinal Chemistry Letters
Xiangji ChenBoli Liu

Abstract

The benzothiazole aniline (BTA) conjugated with monoamine-monoamide (MAMA) was synthesized and then labeled with (99m)Tc. Its corresponding rhenium analogue was synthesized, and the fluorescent staining was performed in brain sections of both Tg mouse and Alzheimer's disease (AD) patient. The fluorescent rhenium complex Re-MAMA-BTA selectively bound to the amyloid aggregates in the brain sections of both APP Tg mouse and AD patient. The analogous (99m)Tc-MAMA-BTA complex could enter the normal mouse brain with high initial uptake. These results are encouraging for further exploration of their derivatives as imaging agents for Abeta plaques in the brain.

References

Jan 16, 2002·The American Journal of Geriatric Psychiatry : Official Journal of the American Association for Geriatric Psychiatry·Kooresh Shoghi-JadidJorge R Barrio
Nov 17, 2004·The American Journal of Geriatric Psychiatry : Official Journal of the American Association for Geriatric Psychiatry·Nicolaas P L G VerhoeffSylvain Houle
Jul 21, 2006·Brain : a Journal of Neurology·Henry EnglerAgneta Nordberg
Nov 30, 2006·Drug Discovery Today·Andrew Lockhart

❮ Previous
Next ❯

Citations

Sep 26, 2013·Journal of Medicinal Chemistry·Hee-Kyung KimTae-Jeong Kim
Mar 3, 2009·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Masahiro Ono
Jun 15, 2013·Beilstein Journal of Organic Chemistry·Todd J EckroatSylvie Garneau-Tsodikova
Jul 26, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Oxana V KharissovaPerla Elizondo Martínez
May 24, 2011·International Journal of Molecular Imaging·Masahiro Ono, Hideo Saji
Oct 13, 2014·European Journal of Medicinal Chemistry·Yanping Yang, Mengchao Cui
Dec 18, 2014·Dalton Transactions : an International Journal of Inorganic Chemistry·David J HaynePaul S Donnelly
Mar 10, 2015·Dalton Transactions : an International Journal of Inorganic Chemistry·Jianhua JiaBoli Liu
Apr 12, 2018·Current Medicinal Chemistry·Sajjad MolavipordanjaniSeyed Jalal Hosseinimehr
Sep 24, 2020·Photochemical & Photobiological Sciences : Official Journal of the European Photochemistry Association and the European Society for Photobiology·Alexandre C OliveiraHugh D Burrows
Nov 11, 2010·ACS Medicinal Chemistry Letters·Masahiro OnoMorio Nakayama
Jan 31, 2018·Molecular Pharmaceutics·Ji-Ae ParkYong Jin Lee

❮ Previous
Next ❯

Related Concepts

Related Feeds

Alzheimer's Disease: APP

Amyloid precursor protein (APP) proteolysis is critical for the development of Alzheimer's disease, a neurodegenerative disease associated with accumulation of amyloid plaques in the brain. Here is the latest research on APP and Alzheimer's disease.

Alzheimer's Disease: Amyloid Beta

Alzheimer's disease is a neurodegenerative disease associated with the accumulation of amyloid plaques in the brain; these plaques are comprised of amyloid beta deposits. Here is the latest research in this field.

Blood Brain Barrier

The blood brain barrier is a border that separates blood from cerebrospinal fluid. Discover the latest search on this highly selective semipermeable membrane here.

Blood Brain Barrier Chips

The blood brain barrier (BBB) is comprised of endothelial cells that regulate the influx and outflux of plasma concentrations. Lab-on-a-chip devices allow scientists to model diseases and mechanisms such as the passage of therapeutic antibodies across the BBB. Discover the latest research on BBB chips here.