In vitro evaluation of N-(fluoro)isopropyl norephedrine as potential cardiac imaging agents for PET.
N-Isopropylnorephedrine (INE) and N-fluoroisopropylnorephedrine (FINE) were found to have a poor affinity for either beta-adrenoceptors and the norepinephrine carrier protein. The low affinity of both compounds for Uptake-1 is probably due to the introduction of a bulky substituent on the nitrogen atom. It is concluded that INE and FINE cannot be used for cardiac imaging with PET.
de Groot
T J
TJ
Pet-Center, University of Groningen, Netherlands.
Buitenhuis
C K
CK
Rutgers
M
M
van Waarde
A
A
Visser
G M
GM
Smets
L A
LA
Brodde
O E
OE
Vaalburg
W
W
D019797:3-Iodobenzylguanidine; D000818:Animals; D002352:Carrier Proteins / Q000378:metabolism; D006321:Heart / Q000000981:diagnostic imaging*; D006801:Humans; D007462:Iodobenzenes / Q000378:metabolism; D008024:Ligands; D009206:Myocardium / Q000378:metabolism*; D016716:PC12 Cells; D010665:Phenylpropanolamine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism; D011943:Receptors, Adrenergic, beta / Q000378:metabolism; D014055:Tomography, Emission-Computed; D014407:Tumor Cells, Cultured
D002352:Carrier Proteins; D007462:Iodobenzenes; D008024:Ligands; D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta; C103217:N-fluoroisopropylnorephedrine; D010665:Phenylpropanolamine; D019797:3-Iodobenzylguanidine