TY - JOUR
T1 - Structure-localization relationships of 11C-labeled phentermine derivatives
T2 - Effect of aromatic substitution
AU - Elmaleh, David R.
AU - Kizuka, Hiro
AU - Hanson, Robert N.
AU - Jones, Gerald S.
AU - Herman, Lee W.
AU - Strauss, H. William
N1 - Funding Information:
Acknon,led~ernenrs~Thls work was supported in part by Public Health Service Grant 1 ROI HL24666 and Department of Energy Contract DE-FG02-86-ER60460.
PY - 1993/5
Y1 - 1993/5
N2 - A series of phentermine analogs, including the unsubstituted, the para-F, -Cl, -Br and -I, and the meta-CF3 derivatives, were labeled by [11C]methylation and evaluated in rats to determine the structure-localization relationships for this class of regional cerebral blood flow imaging agents. All the phentermines were well-localized in the brain; however, only the para-substituted agents were well-retained. Localization in the nontarget tissue was affected by the lipophilicity of the substituent. Comparison with the radioiodinated analogs showed virtually identical results, which suggests that the compounds were not significantly metabolized. The agent with the best biodistribution characteristics was the N-[11C]methyl-p-iodophentermine, with the p-bromo analog almost equivalent.
AB - A series of phentermine analogs, including the unsubstituted, the para-F, -Cl, -Br and -I, and the meta-CF3 derivatives, were labeled by [11C]methylation and evaluated in rats to determine the structure-localization relationships for this class of regional cerebral blood flow imaging agents. All the phentermines were well-localized in the brain; however, only the para-substituted agents were well-retained. Localization in the nontarget tissue was affected by the lipophilicity of the substituent. Comparison with the radioiodinated analogs showed virtually identical results, which suggests that the compounds were not significantly metabolized. The agent with the best biodistribution characteristics was the N-[11C]methyl-p-iodophentermine, with the p-bromo analog almost equivalent.
UR - http://www.scopus.com/inward/record.url?scp=0027604282&partnerID=8YFLogxK
U2 - 10.1016/0969-8043(93)90023-4
DO - 10.1016/0969-8043(93)90023-4
M3 - Article
C2 - 8485509
AN - SCOPUS:0027604282
SN - 0969-8043
VL - 44
SP - 821
EP - 829
JO - Applied Radiation and Isotopes
JF - Applied Radiation and Isotopes
IS - 5
ER -