Pharmacology and pharmacokinetics of stereoisomers in radiopharmacy.
Nowadays stereochemistry and biologic stereospecificity are involved in the search for new radiopharmaceuticals. This article reviews: 1) The factors involved in selective distribution of stereoisomers: first-pass effect, binding to plasma proteins, enzyme effect and membrane transport; 2) the distinction between pharmacologic specific receptors and acceptor sites; recognition of stereoisomer ligands by specific receptors of opioids, neuroamines, steroids; 3) the ligands labeled with positron emitter radionuclides useful for tomography: dopaminergic, opiate, serotonergic, benzodiazepine ligands and muscarinic ligands; these ligands are labeled with 11C, 18F or 75Br. The balance between the benefit of using a stereoisomer and the burden of sophistication in its chemical preparation is discussed. In conclusion, there is not a clearcut position in favor of a systematic choice of an enantiomer radiopharmaceutical.
Cohen
Y
Y
Department of Pharmacology, University of Paris, School of Pharmacy, Chatenay-Malabry, France.
Besnard
M
M
Merlin
L
L
D002250:Carbon Radioisotopes; D003847:Deoxyglucose / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D005283:Fentanyl / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D005442:Flumazenil / Q000493:pharmacokinetics / Q000494:pharmacology*; D005462:Fluorine Radioisotopes; D019788:Fluorodeoxyglucose F18; D007650:Ketanserin / Q000493:pharmacokinetics / Q000494:pharmacology*; D008715:Methionine / Q000493:pharmacokinetics / Q000494:pharmacology*; D013237:Stereoisomerism; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D005462:Fluorine Radioisotopes; D019788:Fluorodeoxyglucose F18; D005442:Flumazenil; D007650:Ketanserin; D003847:Deoxyglucose; D008715:Methionine; C017114:carfentanil; D005283:Fentanyl