133985-85-0Relevant articles and documents
Radiosynthesis, Cerebral Distribution, and Binding of -1-(p-Iodophenyl)-3-(1-adamantyl)guanidine, a Ligand for ? Binding Sites
Kimes, Alane S.,Wilson, Alan A.,Scheffel, Ursula,Campbell, Bruce G.,London, Edythe D.
, p. 4683 - 4689 (1992)
An analog of 1,3-di-o-tolylguanidine (DTG), -labeled 1-(p-iodophenyl)-3-(1-adamantyl)guanidine (PIPAG), was synthesized as a potential ligand for cerebral ? binding sites.Data from in vitro binding experiments and in vivo experiments on brain distribution suggested that PIPAG binds to ? binding sites with high affinity (Kd in low nanomolar range) as determined by Scatchard analysis and relative potencies of ?-specific drugs.Haloperidol had the highest potency to inhibit PIPAG binding.It was followed by DTG, BMY 14802, and (+)-N-allylnormetazocine.Compounds with high affinities for dopamine receptors (but low affinity for ? binding sites), for opioid receptors, for nicotinic acetylcholine receptors, and for phencyclidine receptors were ineffective inhibitors of PIPAG binding.
Radiosynthesis of σ receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines
Wilson,Dannals,Ravert,Sonders,Weber,Wagner Jr.
, p. 1867 - 1870 (2007/10/02)
A series of analogues of the potent and selective σ receptor ligand 1,3-ditolylguanidine (DTG) were synthesized and demonstrated to have high affinity for the σ receptor as measured by in vitro [3H]DTG displacement studies using guinea pig brai
