title: A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone.
abstract: A selective metabotropic glutamate 1 receptor (mGlu1) antagonist was labeled with the positron-emitting radioisotope carbon-11 and evaluated in ex vivo biodistribution studies and micro-positron emission tomography (micro-PET) imaging experiments in rats. Results from animal experiments demonstrate that the radioligand [11C]2 is the first PET tracer capable of labeling the rat mGlu1 receptor in vivo.
authors.affiliation: Departments of Psychiatry and Radiology, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, New York, NY 10032, USA. hh285@columbia.edu
authors.forename: Yiyun
authors.initials: Y
authors.lastname: Huang
authors.forename: Raj
authors.initials: R
authors.lastname: Narendran
authors.forename: François
authors.initials: F
authors.lastname: Bischoff
authors.forename: Ningning
authors.initials: N
authors.lastname: Guo
authors.forename: Zhihong
authors.initials: Z
authors.lastname: Zhu
authors.forename: Sung-A
authors.initials: SA
authors.lastname: Bae
authors.forename: Anne S
authors.initials: AS
authors.lastname: Lesage
authors.forename: Marc
authors.initials: M
authors.lastname: Laruelle
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D002250:Carbon Radioisotopes; D008024:Ligands; D049268:Positron-Emission Tomography; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
chemical_list: C502015:(3-ethyl-2-methyl-quinolin-6-yl)-(4-methoxycyclohexyl)methanone methanesulfonate; D002250:Carbon Radioisotopes; D008024:Ligands; D011804:Quinolines; D019275:Radiopharmaceuticals; D018094:Receptors, Metabotropic Glutamate; C104077:metabotropic glutamate receptor type 1