Radiosynthesis of. sigma. receptor ligands for positron emission tomography: carbon-11 and fluorine-18 labeled guanidines

…, MS Sonders, E Weber, HN Wagner Jr

Index: Wilson; Dannals; Ravert; Sonders; Weber; Wagner Jr. Journal of Medicinal Chemistry, 1991 , vol. 34, # 6 p. 1867 - 1870

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Citation Number: 43

Abstract

A series of analogues of the potent and selective n receptor ligand 1, 3-ditolylguanidine (DTG) were synthesized and demonstrated to have high affinity for the u receptor as measured by in-vitro [3H] DTG displacement studies using guinea pig brain tissue. Three of these l-aryl-3-(l-adamantyl) guanid~ es were radiolabeled-two with carbon-11 and one with fluorine-18. Radiochemical yields and specific activities were sufficient for these ...