title: Synthesis of carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as new potential PET AMPA receptor ligands.
abstract: New carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives were designed and synthesized as potential positron emission tomography AMPA (2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid) receptor ligands to image brain diseases. The single crystal structure of the most potent compound N-acetyl-1-(4'-chlorophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (5a) is first reported.
authors.affiliation: Department of Radiology, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
authors.forename: Mingzhang
authors.initials: M
authors.lastname: Gao
authors.forename: Deyuan
authors.initials: D
authors.lastname: Kong
authors.forename: Abraham
authors.initials: A
authors.lastname: Clearfield
authors.forename: Qi-Huang
authors.initials: QH
authors.lastname: Zheng
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D002244:Carbon / Q000737:chemistry; D005461:Fluorine / Q000737:chemistry; D007546:Isoquinolines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D007553:Isotope Labeling; D008024:Ligands; D051379:Mice; D015394:Molecular Structure; D049268:Positron-Emission Tomography; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000188:drug therapy
chemical_list: D000577:Amides; D000927:Anticonvulsants; D007546:Isoquinolines; D008024:Ligands; C510615:R-4-(3-hydroxyphenyl)-N,N-7,8-tetramethyl-3,4-dihydroisoquinoline-2(1H)-carboxamide; D018091:Receptors, AMPA; D005461:Fluorine; D002244:Carbon