Journal of labelled compounds and radiopharmaceuticals p. 185 - 190 (2011)
Update date:2022-08-03
Topics:
Madsen, Jacob
Elfving, Betina
Frokjaer, Vibe G.
Kornum, Birgitte R.
Thomsen, Gerda
Martiny, Lars
Knudsen, Gitte M.
Two novel radioligands for the serotonin transporter (SERT), [ 125I]{3-[5-iodo-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-1-yl] -propyl}-dimethylamine ([125I]-2) and S-[125I]{3-[5-iodo- 1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-1-yl]-propyl}-dimethylamine ([ 125I]-(S)-2) were synthesized in a Br/125I exchange reaction. Binding experiments in rats yielded Kd values of 0.7 ± 0.06 and 0.52± 0.02 nM for [125I]-2 and [ 125I]-(S)-2, respectively. One hour after intravenous injection of [125I]-2, 0.34% of the injected dose had accumulated in the brain. The highest hypothalamus-to-cerebellum ratio was reached 2 h after injection of [125I]-(S)-2 and amounted to 2.4. Pre-treatment experiments with paroxetine resulted in effective reduction of the target-to-cerebellum ratios. The corresponding iodine-123 labelled compound S-[123I]{3-[5-Iodo-1- (4-fluorophenyl)-1,3-dihydroisobenzofuran-1-yl]-propyl}-dimethylamine [ 123I]-S-2 was investigated in a pig single photon emission computed tomography (SPECT) study. Between 60 and 110 min after IV injection, the midbrain-to-cerebellum ratio was 1.2. However, the uptake did not differ between high-density and medium-density regions questioning the feasibility of the radioligand in imaging cortical SERT distribution in vivo. These data suggest that the iodine-labelled derivatives of citalopram and escitalopram are not superior to another SPECT tracer for the SERT, namely [123I]ADAM. Copyright
View Morewebsite:http://www.acrospharmatech.com
Contact:+1-3234804688
Address:Flat/RM 1502,Easey Commercial building 253-261 Hennessy Road,Wanchai,HongKong
Contact:+86-021-58123769
Address:No.780 of Cailun Road,Zhangjiang Hi-tech Park,Pudong,Shanghai
shanghai Tauto Biotech Co., Ltd
website:http://www.tautobiotech.com/en/index.htm
Contact:+86-21-51320588 ext. 8025
Address:No. 326, Aidisheng Rd , Zhangjiang Hi-tech Park, Shanghai , P.R.CHINA
Chengdu NoVi Biotechnology Co., Ltd.(expird)
Contact:13551243286/028-81458053
Address:NO.168-1-224 JULONG ROAD WUHOU DISTRICT, CHENGDU CITY,SICHUAN PROVINCE
Huludao Tianqi Shengye Chemical Co.,Ltd.
Contact:0086 429 2075777
Address:Area B,Shipbuilding Industry Park,Beigang District,Huludao City,Liaoning prov.,China
Doi:10.1016/0223-5234(90)90002-K
(1990)Doi:10.1016/S0040-4039(01)82824-0
(1966)Doi:10.1016/S0040-4039(00)97730-X
(1990)Doi:10.1021/acs.orglett.6b01408
(2016)Doi:10.1016/0223-5234(90)90205-H
(1990)Doi:10.1016/j.ejmech.2007.06.017
(2008)