(S)-N-[(1-Ethyl-2-pyrrolidinyl)methyl]-2-hydroxy-3-iodo-6- methoxybenzamide ([123I]IBZM) is a central nervous system (CNS) D-2 dopamine receptor imaging agent. In order to investigate the versatility of this parent structure in specific dopamine receptor localization and the potential for developing new dopamine receptor imaging agents, a series of new iodinated benzamides with fused ring systems, naphthalene (INAP) and benzofuran (IBF), was synthesized and radiolabeled, and the in vivo and in vitro biological properties were characterized. The best analogue of IBZM is IBF (21). The specific binding of [125I]IBF (21) with rat striatal tissue preparation was found to be saturable and displayed a Kd of 0.106 +/- 0.015 nM. Competition data of various receptor ligands for [125I]IBF (21) binding show the following rank order of potency: spiperone greater than IBF (21) greater than IBZM greater than (+)-butaclamol greater than (+/-)-ADTN,6,7 greater than ketanserin greater than SCH-23390 much greater than propranolol. The in vivo biodistribution results confirm that [125I]IBF (21) concentrated in the striatal area after iv injection into rats. The study demonstrates that [123I]IBF (21) is a potential agent for imaging CNS D-2 dopamine receptors.
Reaction of the bromonaphthalenecarboxylic acid chloride (I) with the (S)‐(‐)‐(aminomethyl)pyrrolidine (II) yields the amide (III) which is converted to the desired iodonaphthalene (VI) via the stannyl derivative (V).
Mucormycosis is an opportunistic, angioinvasive fungal infection characteristically affecting individuals with diabetes mellitus, chronic renal failure, and hematologic malignancies. In most cases it is a rapidly progressive infection with an 80% overall mortality. Radiographic manifestations are usually nonspecific focal consolidation or masses. The air crescent sign is a rare manifestation of angioinvasive fungi and indicates either aspergillosis or mucormycosis.
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