Novel 99mTc-2-arylimidazo[2,1-b]benzothiazole derivatives as SPECT imaging agents for amyloid-β plaques
Copyright © 2019 Elsevier Masson SAS. All rights reserved..
Six novel 2-arylimidazo[2,1-b]benzothiazole (IBT) derivatives were synthesized as potential tridentate radiotracers for AD imaging purposes. Two of these ligands (6a,b) were successfully labeled with 99mTc radionuclide at high radiochemical purity using fac-[99mTc(CO)3(H2O)3]+ synthon. [99mTc]7a and [99mTc]7b were evaluated as single photon emission computed tomography (SPECT) imaging agents for Aβ plaque in AD. [99mTc]7a and [99mTc]7b exhibited suitable affinity toward Aβ aggregates with IC50 values of 33.2 and 102.5 nM, respectively. The IC50 value of these radiotracers depends on the length of the spacer (alkyl chain). In biodistribution study, these complexes showed good initial brain uptakes (0.78 and 0.86% ID/g at 2 min post-injection) and fast blood clearance. Autoradiography results confirmed that these small 99mTc complexes (Mw about 600 Da) can bind to Aβ plaques in the brain sections of the rat AD model. Histopathological staining with Congo red approved the presence of Aβ plaques in these brain sections.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2019 |
|---|---|
| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:175 |
|---|---|
| Enthalten in: |
European journal of medicinal chemistry - 175(2019) vom: 01. Aug., Seite 149-161 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Molavipordanjani, Sajjad [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Completed 15.07.2019 Date Revised 15.07.2019 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1016/j.ejmech.2019.04.069 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM296979791 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM296979791 | ||
| 003 | DE-627 | ||
| 005 | 20231225091014.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2019 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1016/j.ejmech.2019.04.069 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n0989.xml |
| 035 | |a (DE-627)NLM296979791 | ||
| 035 | |a (NLM)31078865 | ||
| 035 | |a (PII)S0223-5234(19)30397-6 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Molavipordanjani, Sajjad |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Novel 99mTc-2-arylimidazo[2,1-b]benzothiazole derivatives as SPECT imaging agents for amyloid-β plaques |
| 264 | 1 | |c 2019 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 15.07.2019 | ||
| 500 | |a Date Revised 15.07.2019 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2019 Elsevier Masson SAS. All rights reserved. | ||
| 520 | |a Six novel 2-arylimidazo[2,1-b]benzothiazole (IBT) derivatives were synthesized as potential tridentate radiotracers for AD imaging purposes. Two of these ligands (6a,b) were successfully labeled with 99mTc radionuclide at high radiochemical purity using fac-[99mTc(CO)3(H2O)3]+ synthon. [99mTc]7a and [99mTc]7b were evaluated as single photon emission computed tomography (SPECT) imaging agents for Aβ plaque in AD. [99mTc]7a and [99mTc]7b exhibited suitable affinity toward Aβ aggregates with IC50 values of 33.2 and 102.5 nM, respectively. The IC50 value of these radiotracers depends on the length of the spacer (alkyl chain). In biodistribution study, these complexes showed good initial brain uptakes (0.78 and 0.86% ID/g at 2 min post-injection) and fast blood clearance. Autoradiography results confirmed that these small 99mTc complexes (Mw about 600 Da) can bind to Aβ plaques in the brain sections of the rat AD model. Histopathological staining with Congo red approved the presence of Aβ plaques in these brain sections | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a (99m)Tc | |
| 650 | 4 | |a 2-arylimidazo[2,1-b]benzothiazole | |
| 650 | 4 | |a Alzheimer's disease | |
| 650 | 4 | |a Autoradiography | |
| 650 | 4 | |a Binding assay | |
| 650 | 4 | |a Single photon emission computed tomography (SPECT) imaging | |
| 650 | 4 | |a β-Amyloid plaque | |
| 650 | 7 | |a Benzothiazoles |2 NLM | |
| 650 | 7 | |a Imidazoles |2 NLM | |
| 650 | 7 | |a Organotechnetium Compounds |2 NLM | |
| 650 | 7 | |a Radiopharmaceuticals |2 NLM | |
| 650 | 7 | |a benzothiazole |2 NLM | |
| 650 | 7 | |a G5BW2593EP |2 NLM | |
| 700 | 1 | |a Emami, Saeed |e verfasserin |4 aut | |
| 700 | 1 | |a Mardanshahi, Alireza |e verfasserin |4 aut | |
| 700 | 1 | |a Talebpour Amiri, Fereshteh |e verfasserin |4 aut | |
| 700 | 1 | |a Noaparast, Zohreh |e verfasserin |4 aut | |
| 700 | 1 | |a Hosseinimehr, Seyed Jalal |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t European journal of medicinal chemistry |d 1994 |g 175(2019) vom: 01. Aug., Seite 149-161 |w (DE-627)NLM106608835 |x 1768-3254 |7 nnns |
| 773 | 1 | 8 | |g volume:175 |g year:2019 |g day:01 |g month:08 |g pages:149-161 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1016/j.ejmech.2019.04.069 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 175 |j 2019 |b 01 |c 08 |h 149-161 | ||