LGD1069,4-[ 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethenyi] benzoic acid, is the first retinoid X receptor (RXR) selective retinoid to enter clinical trials for treatment of dermatological diseases and cancer. In order to examine biological properties such as receptor binding, metabolism and bioavailability, [ I 'C]-. I14C]-, and [3H]-labeled LGD1069 is required. Herein, we describe synthetic methods for preparing isotopically labeled homologs of LGD1069 as well as comparative competition binding data for [6,7-3H]-LGD1069 and [3H]-9-cis retinoic acid with RXR active retinoids. The final radiolabeled products, [6,7-3H]-LGD 1069 and 3-[14C]-LGD1069 have specific activities of 56 Ci/mmol and 49 mCi/mmol, respectively. Radiochemical purities are 99.5% for [6,7-3H]-LGDlO69 and 99.0% for 3-[14C]-LGD1069. The chemical purity is 99.0% for 3-['3CD3]-LGD1069. Competition binding studies with known retinoids show similar Q values when either [6,7-3H]-LGD1069 or [3H]-9-cis retinoic acid is used as the radioligand.
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