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.
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.
Huang
Yiyun
Y
Departments of Psychiatry and Radiology, Columbia University College of Physicians and Surgeons, 1051 Riverside Drive, New York, NY 10032, USA. hh285@columbia.edu
Narendran
Raj
R
Bischoff
François
F
Guo
Ningning
N
Zhu
Zhihong
Z
Bae
Sung-A
SA
Lesage
Anne S
AS
Laruelle
Marc
M
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
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