A simple method of preparation for [123I]-(S)-(-)-IBZM.
Sterile, apyrogenic [123I]IBZM was prepared in a sealed, capped 'V' vial, followed by SEP-PAK C-18 cartridge purification, and then was placed under sealed vial condensation. The quantity of BZM present in the final product ranged from 3.3-5.9 micrograms, as measured by a UV spectrophotometer at 254 and 308 nm. Animal biodistribution studies revealed that the [123I]IBZM prepared by this method which contained 5.9 micrograms of BZM, compared to the standard preparation method containing 0 microgram of BZM, resulted in identical brain uptakes at 15, 30, 60, and 120 min post-injection. The in vitro and in vivo studies demonstrated that a small amount of BZM presence in the final product did not affect the radiochemical purity, nor the D2 receptor binding capacity in the rat brain of [123I]IBZM. The preparation time can be shortened to 1.5 h compared with at least 2-4 h needed for the standard method of preparation. This factor may be important in routine clinical application.
Wang
T S
TS
Department of Radiology, College of Physicians and Surgeons, Columbia University, New York, NY 10032, USA.
Malaspina
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D
Van Heertum
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RL
D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D003287:Contrast Media / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D018492:Dopamine Antagonists / Q000138:chemical synthesis*; D007457:Iodine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D008297:Male; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley
D001549:Benzamides; D003287:Contrast Media; D018492:Dopamine Antagonists; D007457:Iodine Radioisotopes; D011759:Pyrrolidines; C055743:3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide