Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines
Journal Article
·
· J. Med. Chem.; (United States)
Fourteen /sup 125/I-labeled aralkylguanidines were synthesized and evaluated as potential imaging agents for the adrenal medullae and tumors of adrenomedullary origin. These guanidines are radiotracer analogues of guanethidine, an antihypertensive agent thought to mediate neuron blockade by uptake into adrenergic nerves. Dog adrenal medullae were used as a model to test radiotracer affinity for catecholamine storage tissue. Tissue distribution studies revealed that a number of radioiodinated guanidines showed pronounced localization in the adrenal medullae following intravenous injection, in certain cases exceeding that of either (-)-(/sup 3/H)norepinephrine or (/sup 14/C)guanethidine. (m-(/sup 125/I)Iodobenzyl)guanidine (m-IBG, 2b) gave the best combination of high concentration and selectivity. The low adrenomedullary affinity observed with (/sup 14/C)guanidine and m-(/sup 125/I)iodobenzylamine demonstrates the uniqueness of the aralkylguanidine structure. Preliminary evidence suggests that 2b is a storage analogue of norepinephrine. (/sup 125/I)2a is now being used clinically in imaging and radiotherapy of catecholamine tumors, such as pheochromocytoma.
- Research Organization:
- Univ. of Michigan Medical Center, Ann Arbor
- OSTI ID:
- 6746983
- Journal Information:
- J. Med. Chem.; (United States), Journal Name: J. Med. Chem.; (United States) Vol. 27:2; ISSN JMCMA
- Country of Publication:
- United States
- Language:
- English
Similar Records
Imaging the primate adrenal medulla with (/sup 123/I) and (/sup 131/I) metaiodobenzylguanidine: concise communication
Human absorbed dose calculations for iodine-131 and iodine-123 labeled meta-iodobenzyl-guanidine (mIBG): a potential myocardial and adrenal medulla imaging agent
Radiopharmaceuticals for diagnosis and treatment: Progress report for the period November 1, 1968 through July 1, 1987
Journal Article
·
Tue Mar 31 23:00:00 EST 1981
· J. Nucl. Med.; (United States)
·
OSTI ID:6582513
Human absorbed dose calculations for iodine-131 and iodine-123 labeled meta-iodobenzyl-guanidine (mIBG): a potential myocardial and adrenal medulla imaging agent
Conference
·
Mon Jun 01 00:00:00 EDT 1981
· HHS Publ. (FDA) (U.S.); (United States)
·
OSTI ID:5870145
Radiopharmaceuticals for diagnosis and treatment: Progress report for the period November 1, 1968 through July 1, 1987
Technical Report
·
Wed Jul 01 00:00:00 EDT 1987
·
OSTI ID:6155423
Related Subjects
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ADRENAL GLANDS
ANIMALS
BETA DECAY RADIOISOTOPES
BODY
CARBON 14 COMPOUNDS
COMPARATIVE EVALUATIONS
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DISEASES
DOGS
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
GLANDS
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NEOPLASMS
NUCLEI
ODD-EVEN NUCLEI
ORGANS
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIOPHARMACEUTICALS
TESTING
TRITIUM COMPOUNDS
UPTAKE
VERTEBRATES
62 RADIOLOGY AND NUCLEAR MEDICINE
ADRENAL GLANDS
ANIMALS
BETA DECAY RADIOISOTOPES
BODY
CARBON 14 COMPOUNDS
COMPARATIVE EVALUATIONS
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DISEASES
DOGS
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ENDOCRINE GLANDS
GLANDS
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NEOPLASMS
NUCLEI
ODD-EVEN NUCLEI
ORGANS
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIOPHARMACEUTICALS
TESTING
TRITIUM COMPOUNDS
UPTAKE
VERTEBRATES