2-Hydroxy-N,N-dimethyl-N-(methyl-11C)ethanaminium
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2-Hydroxy-N,N-dimethyl-N-(methyl-11C)ethanaminium
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CAS No:
94793-58-5
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Formula:
C5H14NO
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Chemical Name:
2-Hydroxy-N,N-dimethyl-N-(methyl-11C)ethanaminium
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Synonyms:
Ethanaminium,2-hydroxy-N,N-dimethyl-N-(methyl-11C)-;2-Hydroxy-N,N-dimethyl-N-(methyl-11C)ethanaminium
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CAS No:
Description
(11)C-choline is a choline in which one of the methyl carbons is replaced by an (11)C isotope. An intravenous radioactive diagnostic agent used (in the form of its chloride salt) as a tracer during positron emission tomography scans to help detect sites of recurrent prostate cancer. It has a role as a radioactive imaging agent and a radioactive tracer. It is a member of cholines and an (11)C-modified compound.|Choline C 11 Injection is a radioactive diagnostic agent for positron emission tomography (PET) imaging of pat ients with suspected prostate cancer recurrence and non-informative bone scintigraphy, computerized tomography (CT) or magnetic resonance imaging.|Choline c-11 is a Radioactive Diagnostic Agent. The mechanism of action of choline c-11 is as a Radiopharmaceutical Activity.|Carbon C 11 Choline is a radiotracer consisting of choline labeled with the positron-emitting isotope carbon C 11 with potential imaging use. Upon administration, C-11 choline incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, an enzyme frequently upregulated in human tumors, yielding phosphoryl C-11 choline. In turn, phosphoryl C-11 choline is integrated into phospholipids in the cell membrane as part of phosphatidylcholine. As the proliferation of cancer cells is much higher than normal cells, tumor cells exhibit an increased rate of C-11 choline uptake and incorporation, allowing tumor imaging with positron emission tomography (PET).
2-Hydroxy-N,N-dimethyl-N-(methyl-11C)ethanaminium Basic Attributes
103.17 g/mol
103.1189717 g/mol
M4AS4XGD4Q
DTXSID10241624
C78485
Drug Information
Choline C 11 Injection is indicated for positron emission tomography (PET) imaging of patients with suspected prostate cancer recurrence and non-informative bone scintigraphy, computerized tomography (CT) or magnetic resonance imaging (MRI). In these patients, 11 C-choline PET imaging may help identify potential sites of prostate cancer recurrence for subsequent histologic confirmation. Suspected prostate recurrence is based upon elevated blood prostate specific antigen (PSA) levels following initial therapy. In clinical studies, imag es w ere produced with PET/CT coregistration.
In a study of men with prostatic hyperplasia or primary prostate cancer, PET imaging showed 11C-choline radioactivity accumulated rapidly within the prostate; uptake appeared to peak by five minutes following injection of the drug and activity was retained over the subsequent 30 minute scanning period. Little uptake was observed in the bladder and rectum.
Urinary excretion of 11C-choline was < 2% of the injected radioactivity at 1.5 hours after injection of the drug.|11C-choline distributes mainly to the pancreas, kidneys, liver, spleen and colon|The rate of 11C- choline excretion in urine was 0.014 mL/min.
Following intravenous administration, 11C-choline undergoes metabolism resulting in the detection of 11C- betaine as the major metabolite in blood. In a study of patients with prostate cancer or brain disorders, the fractional activities of 11C-choline and 11C- betaine in human arterial plasma appeared to reach a plateau within 25 minutes, with 11C- betaine representing 82% ± 9% of the total 11C detected at that time point. A small amount of unmetabolized 11C-choline was detected within the blood at the final sampling time point (40 minutes).
Choline C 11 Injection is a radiolabeled analog of choline, a precursor molecule essential for the biosynthesis of cell membrane phospholipids. Choline is involved in synthesis of the structural components of cell membranes, as well as modulation of trans-membrane signaling. Increased phospholipid synthesis (i.e., increased uptake of choline) has been associated with cell proliferation and the transformation process that occurs in tumor cells.
2-Hydroxy-N,N-dimethyl-N-(methyl-11C)ethanaminium Use and Manufacturing
Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients
Computed Properties
Molecular Weight:103.17
XLogP3:-0.4
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:1
Rotatable Bond Count:2
Exact Mass:103.1189717
Monoisotopic Mass:103.1189717
Topological Polar Surface Area:20.2
Heavy Atom Count:7
Formal Charge:1
Complexity:46.5
Isotope Atom Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
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