DT-Web

DB00789 - Gadopentetate dimeglumine


Identification
Name Gadopentetate dimeglumine
Accession Number DB00789 (APRD00991)
Type small molecule
Description A complex of gadolinium with a chelating agent, diethylenetriamine penta-acetic acid (DTPA see pentetic acid), that is given to enhance the image in cranial and spinal MRIs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p706)
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 938
Groups approved
Monoisotopic Weight 938.260314726
Pharmacology
Indication For use with magnetic resonance imaging (MRI) in adults, and pediatric patients (2 years of age and older) to visualize lesions with abnormal vascularity in the brain (intracranial lesions), spine and associated tissues as well as lesions with abnormal vascularity in the head and neck. Also used to facilitate the visualization of lesions with abnormal vascularity in the body (excluding the heart).
Mechanism of action Based on the behavior of protons when placed in a strong magnetic field, which is interpreted and transformed into images by magnetic resonance (MR) instruments. MR images are based primarily on proton density and proton relaxation dynamics. MR instruments are sensitive to two different relaxation processes, the T1 (spin-lattice or longitudinal relaxation time) and T2 (spin-spin or transverse relaxation time). Paramagnetic agents contain one or more unpaired electrons that enhance the T1 and T2 relaxation rates of protons in their molecular environment. The proton relaxation effect (PRE) of an unpaired electron is 700 times stronger than that of a proton itself. In MRI, visualization of normal and pathological brain tissue depends in part on variations in the radio frequency signal intensity that occur with changes in proton density, alteration of the T1, and variation in T2. When placed in a magnetic field, gadopentetate dimeglumine shortens the T1 and T2 relaxation times in tissues where it accumulates. In the central nervous system (CNS), gadopentetate dimeglumine enhances visualization of normal tissues that lack a blood-brain barrier, such as the pituitary gland and the meninges. Gadopentetate dimeglumine does not cross the intact blood-brain barrier; therefore, it does not accumulate in normal brain tissue or in CNS lesions that have not caused an abnormal blood-brain barrier (e.g., cysts, mature post-operative scars). Abnormal vascularity or disruption of the blood-brain barrier allows accumulation of gadopentetate dimeglumine in lesions such as neoplasms, abscesses, and subacute infarcts. Outside the CNS, gadopentetate dimeglumine rapidly reaches equilibrium in the interstitial compartment and enhances signal in all tissues as a function of delivery and size of the interstitial compartment. This compound has also been found to inhibit human erythrocyte 6-phosphogluconate dehydrogenase.
Absorption Not Available
Protein binding Not Available
Biotransformation No detectable biotransformation or decomposition.
Route of elimination Gadopentetate is exclusively eliminated in the urine with 83 ? 14% (mean ? SD) of the dose excreted within 6 hours and 91 ? 13% (mean ? SD) by 24 hours, post-injection.
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


6-phosphogluconate dehydrogenase, decarboxylating
Name 6-phosphogluconate dehydrogenase, decarboxylating
Gene Name PGD
Pharmacological action unknown
Actions inhibitor
References
  • Akkemik E, Budak H, Ciftci M: Effects of some drugs on human erythrocyte 6-phosphogluconate dehydrogenase: an in vitro study. J Enzyme Inhib Med Chem. 2010 Mar 17. - Pubmed
  • Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. - Pubmed
DTHybrid score 0.5

Predictions


Id Partner name Gene Name Score
2621 Thermoresistant gluconokinase gntK 0.0571
2206 Glucose-6-phosphate isomerase GPI 0.0429
766 Beta-2 adrenergic receptor ADRB2 0.0409
790 DNA polymerase subunit alpha B POLA2 0.0348
6217 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B PDE8B 0.0175
6216 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A PDE8A 0.0163
691 cAMP-specific 3',5'-cyclic phosphodiesterase 7B PDE7B 0.015
2164 Multidrug resistance-associated protein 4 ABCC4 0.0145
779 High-affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A PDE7A 0.0141
6024 Cytochrome P450 1A1 CYP1A1 0.0139
6013 Cytochrome P450 2E1 CYP2E1 0.0132
4109 cAMP-specific 3',5'-cyclic phosphodiesterase 4C PDE4C 0.0126
4200 Cytochrome P450 1A2 CYP1A2 0.0116
1024 Solute carrier family 22 member 11 SLC22A11 0.0112
290 Prostaglandin G/H synthase 2 PTGS2 0.0109
6152 Solute carrier organic anion transporter family member 2A1 SLCO2A1 0.0107
2757 Inorganic pyrophosphatase ppa 0.0107
6238 Inorganic pyrophosphatase ppa 0.0107
6968 Inorganic pyrophosphatase PPA1 0.0107
2383 2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase ispF 0.0107
2937 2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase ispF 0.0107
4620 2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase ispF 0.0107
6594 2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase ispF 0.0107
6609 2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase ispF 0.0107
6646 2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase ispF 0.0107
1971 cAMP-specific 3',5'-cyclic phosphodiesterase 4A PDE4A 0.0106
2358 cAMP-specific 3',5'-cyclic phosphodiesterase 4D PDE4D 0.0105
558 Solute carrier family 12 member 1 SLC12A1 0.0105
20 Prostaglandin G/H synthase 1 PTGS1 0.0102
6142 Solute carrier family 22 member 8 SLC22A8 0.0097
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0096
541 cAMP-specific 3',5'-cyclic phosphodiesterase 4B PDE4B 0.0096
2755 Hypoxanthine-guanine-xanthine phosphoribosyltransferase LACZ 0.0095
4553 Bifunctional adenosylcobalamin biosynthesis protein cobU cobU 0.0094
2647 RNA-directed RNA polymerase P2 0.0094
355 GMP synthase [glutamine-hydrolyzing] GMPS 0.0093
4353 GMP synthase [glutamine-hydrolyzing] guaA 0.0093
2434 NH(3)-dependent NAD(+) synthetase nadE 0.009
2910 NH(3)-dependent NAD(+) synthetase nadE 0.009
3217 NH(3)-dependent NAD(+) synthetase nadE 0.009
1729 Solute carrier family 22 member 6 SLC22A6 0.0089
587 Serum albumin ALB 0.0089
3010 Regulatory protein blaR1 blaR1 0.0087
4924 Cytochrome P450 2C8 CYP2C8 0.0087
2149 Angiogenin ANG 0.0087
2727 S-adenosylmethionine synthetase metK 0.0084
2885 Carboxyethyl-arginine beta-lactam-synthase bls 0.0082
4600 Malonamidase E2 Not Available 0.0082
4757 Cytochrome P450 2C9 CYP2C9 0.008
2717 Folylpolyglutamate synthase fgs 0.0079
357 Carbonic anhydrase 2 CA2 0.0078
118 Organic cation/carnitine transporter 2 SLC22A5 0.0077
6395 Myosin-14 MYH14 0.0074
2428 Thiamine-phosphate pyrophosphorylase thiE 0.0074
492 Histamine H1 receptor HRH1 0.0073
4512 Cytochrome P450 3A4 CYP3A4 0.0071
87 Hypoxanthine-guanine phosphoribosyltransferase HPRT1 0.0067
5294 Nucleoside diphosphate kinase A NME1 0.0062
5818 Folate receptor alpha FOLR1 0.0059
293 Gamma-glutamyl hydrolase GGH 0.0052
1650 Heme carrier protein 1 SLC46A1 0.0046
773 Folylpolyglutamate synthase, mitochondrial FPGS 0.0045
2287 Bifunctional purine biosynthesis protein PURH [Includes: Phosphoribosylaminoimidazolecarboxamide formyltransferase ATIC 0.0042
6155 ATP-binding cassette transporter sub-family C member 11 ABCC11 0.0041
6160 Solute carrier organic anion transporter family member 3A1 SLCO3A1 0.0037
3917 Methylenetetrahydrofolate reductase MTHFR 0.0037
6150 Solute carrier organic anion transporter family member 4C1 SLCO4C1 0.0036
6020 Aldehyde oxidase AOX1 0.0034
24 Thymidylate synthase TMP1 0.0034
359 Thymidylate synthase TYMS 0.0034
2626 Thymidylate synthase thyA 0.0034
2729 Thymidylate synthase thyA 0.0034
5352 Thymidylate synthase THYA 0.0034
365 Dihydrofolate reductase DHFR 0.0033
2381 Dihydrofolate reductase DFR1 0.0033
2833 Dihydrofolate reductase Not Available 0.0033
2931 Dihydrofolate reductase folA 0.0033
3544 Dihydrofolate reductase folA 0.0033
3682 Dihydrofolate reductase folA 0.0033
6642 Dihydrofolate reductase folA 0.0033
6756 Dihydrofolate reductase dfrA 0.0033
6158 Solute carrier organic anion transporter family member 1C1 SLCO1C1 0.0033
6148 Multidrug resistance-associated protein 7 ABCC10 0.0033
738 Monocarboxylate transporter 1 SLC16A1 0.0032
6157 Solute carrier organic anion transporter family member 1B3 SLCO1B3 0.003
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.0029
6143 Solute carrier family 22 member 7 SLC22A7 0.0027
862 Multidrug resistance-associated protein 1 ABCC1 0.0026
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0026
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0025
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0024
1588 Multidrug resistance protein 1 ABCB1 0.0019
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