A novel radioligand for imaging the AT1 angiotensin receptor with PET
2-Butyl-5-methoxymethyl-6-(1-oxopyridin-2-yl)-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine (KR31173) was radiolabeled by coupling a tetrazole-protected hydroxy precursor with [(11)C] methyl iodide and removing the protecting group by acid hydrolysis. In mice, the hig...
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| Veröffentlicht in: | Nuclear medicine and biology 2004-07, Vol.31 (5), p.571-574 |
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| creator | Mathews, William B Yoo, Sung-Eun Lee, Sung-Hou Scheffel, Ursula Rauseo, Paige A Zober, Tamas G Gocco, Gerard Sandberg, Kathryn Ravert, Hayden T Dannals, Robert F Szabo, Zsolt |
| description | 2-Butyl-5-methoxymethyl-6-(1-oxopyridin-2-yl)-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine (KR31173) was radiolabeled by coupling a tetrazole-protected hydroxy precursor with [(11)C] methyl iodide and removing the protecting group by acid hydrolysis. In mice, the highest uptake of [(11)C] KR31173 was in the adrenal glands, kidneys, and liver. Tissue to blood ratios were generally greater than 10:1. Uptake of the tracer in the adrenal glands, kidneys, lungs, and heart was blocked with a 1 mg/kg dose of KR31173 or MK-996. |
| doi_str_mv | 10.1016/j.nucmedbio.2003.10.014 |
| format | Article |
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In mice, the highest uptake of [(11)C] KR31173 was in the adrenal glands, kidneys, and liver. Tissue to blood ratios were generally greater than 10:1. 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In mice, the highest uptake of [(11)C] KR31173 was in the adrenal glands, kidneys, and liver. Tissue to blood ratios were generally greater than 10:1. Uptake of the tracer in the adrenal glands, kidneys, lungs, and heart was blocked with a 1 mg/kg dose of KR31173 or MK-996.</description><subject>Adrenal Glands - diagnostic imaging</subject><subject>Adrenal Glands - metabolism</subject><subject>Animals</subject><subject>Carbon Radioisotopes - pharmacokinetics</subject><subject>Imidazoles - pharmacokinetics</subject><subject>Kidney - diagnostic imaging</subject><subject>Kidney - metabolism</subject><subject>Ligands</subject><subject>Liver - diagnostic imaging</subject><subject>Liver - metabolism</subject><subject>Male</subject><subject>Mice</subject><subject>Organ Specificity</subject><subject>Positron-Emission Tomography - methods</subject><subject>Radiopharmaceuticals - pharmacokinetics</subject><subject>Receptor, Angiotensin, Type 1 - metabolism</subject><subject>Reproducibility of Results</subject><subject>Sensitivity and Specificity</subject><subject>Tetrazoles - pharmacokinetics</subject><subject>Tissue Distribution</subject><issn>0969-8051</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkM1OwzAQhH0A0VJ4BfCJW8I6cVznWFXlR6oEh3K2HNtJXaV2sRMQb4-rVrCXlXZmdrUfQvcEcgKEPe5yN6q90Y31eQFQpmkOhF6gKdSszjhUZIKuY9xBclMCV2hCqoLUxZxO0WqBnf8yPQ5SW9_bTjqNWx-w3cvOug4PW4MXG4Kl66wfjIvW4WCUOQzJ9G2HLX5fbW7QZSv7aG7PfYY-nlab5Uu2fnt-XS7WmSoKOmSSMKB1C0qWbUU4pdAYqklRakUqVRVcNoxzBrqsGFNzUExzUivNaMNbU9Nyhh5Oew_Bf44mDmJvozJ9L53xYxQsFWW0Ssb5yaiCjzGYVhxC-ij8CALiSE3sxB81caR2FBK1lLw7nxibJP_nzsjKX_yQbLM</recordid><startdate>200407</startdate><enddate>200407</enddate><creator>Mathews, William B</creator><creator>Yoo, Sung-Eun</creator><creator>Lee, Sung-Hou</creator><creator>Scheffel, Ursula</creator><creator>Rauseo, Paige A</creator><creator>Zober, Tamas G</creator><creator>Gocco, Gerard</creator><creator>Sandberg, Kathryn</creator><creator>Ravert, Hayden T</creator><creator>Dannals, Robert F</creator><creator>Szabo, Zsolt</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>200407</creationdate><title>A novel radioligand for imaging the AT1 angiotensin receptor with PET</title><author>Mathews, William B ; 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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Adrenal Glands - diagnostic imaging Adrenal Glands - metabolism Animals Carbon Radioisotopes - pharmacokinetics Imidazoles - pharmacokinetics Kidney - diagnostic imaging Kidney - metabolism Ligands Liver - diagnostic imaging Liver - metabolism Male Mice Organ Specificity Positron-Emission Tomography - methods Radiopharmaceuticals - pharmacokinetics Receptor, Angiotensin, Type 1 - metabolism Reproducibility of Results Sensitivity and Specificity Tetrazoles - pharmacokinetics Tissue Distribution |
| title | A novel radioligand for imaging the AT1 angiotensin receptor with PET |
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