Gadopentetate (Gd-DTPA) (tail intravenously; 2 and 5 mmol/kg; single dose) exhibits a pyramidal cycle, TCA cycle, activation, and disruption as part of a systemic activating response. An animal model of how group dynamics are disrupted: rat [1]

Animal/Disease Models: Rats[1]
Doses: 2 and 5mmol/kg
Route of Administration: tail vein injection, single
Experimental Results:Observed urinary and serum metabonomic recovery but the metabolic effects of high-dosed (5mmol/kg) lasted long. Observed hyperlipidemia after Gd-DTPA injection.

Absorption, Distribution and Excretion
Following injection, gadopentetate dimeglumine is primarily excreted in the urine, with 83 ± 14% (mean ± standard deviation) of the dose excreted within 6 hours and 91 ± 13% (mean ± standard deviation) within 24 hours. 266 ± 43 mL/kg 1.94 ± 0.28 mL/min/kg [Normal Subjects] Metabolism/Metabolites No biotransformation or degradation was detected. Biological Half-Life Distribution half-life: 12 minutes; elimination half-life: 100 minutes.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
After a mother uses gadopentetate calcium, the gadolinium content in her breast milk is less than 1% of the infant's allowable intake. Furthermore, because gadopentetate calcium is poorly absorbed orally, it is unlikely to enter the infant's bloodstream and will not have any adverse effects on breastfed infants. Gadopentetate calcium releases more free gadolinium than some other gadolinium-containing contrast agents. Some European guidelines recommend suspending breastfeeding for 24 hours after contrast agent injection, but guidelines developed by North American professional organizations state that breastfeeding mothers do not need to interrupt breastfeeding after receiving gadolinium-containing contrast agents. ◉ Effects on Breastfed Infants
No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk
No published information found as of the revision date.

[1]. Gd-DTPA-induced dynamic metabonomic changes in rat biofluids. Magn Reson Imaging. 2017 Dec;44:15-25.

[2]. Analysis of pharmacokinetics of Gd-DTPA for dynamic contrast-enhanced magnetic resonance imaging. Magn Reson Imaging. 2016 Sep;34(7):1034-40.

complex of gadolinium and the chelating agent diethylenetriaminepentaacetic acid (DTPA, see pentaacetic acid) is used to enhance images on magnetic resonance imaging (MRI) of the brain and spine. (From Martindale Pharmacopoeia, 30th edition, p. 706)
A complex of gadolinium and the chelating agent diethylenetriaminepentaacetic acid (DTPA, see pentaacetic acid) is used to enhance images on magnetic resonance imaging (MRI) of the brain and spine. (From Martindale Pharmacopoeia, 30th edition, p. 706)
Indications

For use in adults and children (2 years and older) on magnetic resonance imaging (MRI) to visualize vascular abnormalities in the brain (intracranial lesions), spine and related tissues, and head and neck vascular abnormalities. It may also be used to assist in visualizing vascular abnormalities in vivo (excluding the heart).
FDA Label
Mechanism of Action

Based on the behavior of protons in a strong magnetic field, which is interpreted and converted into images by a magnetic resonance (MR) instrument. MR imaging is primarily based on proton density and proton relaxation dynamics. MR instruments are sensitive to two distinct relaxation processes: T1 (spin-lattice or longitudinal relaxation time) and T2 (spin-spin or transverse relaxation time). Paramagnetic contrast agents contain one or more unpaired electrons, which enhance the T1 and T2 relaxation rates of protons in their molecular environment. The proton relaxation effect (PRE) of unpaired electrons is 700 times stronger than that of the proton itself. In MRI, the imaging of normal and diseased brain tissue depends on variations in radiofrequency signal intensity, which are caused by changes in proton density, alterations in T1, and changes in T2. When placed in a magnetic field, gadopentetate dimeglumine can shorten the T1 and T2 relaxation times in tissues where it accumulates. In the central nervous system (CNS), gadopentetate dimeglumine enhances the visualization of normal tissues lacking the blood-brain barrier, such as the pituitary gland and meninges. Gadopentetate dimeglumine cannot cross the intact blood-brain barrier; therefore, it does not accumulate in normal brain tissue or in central nervous system lesions that do not cause blood-brain barrier abnormalities (e.g., cysts, mature postoperative scars). Abnormal vascular distribution or disruption of the blood-brain barrier can cause gadopentetate dimeglumine to accumulate in lesions such as tumors, abscesses, and subacute infarctions. Outside the central nervous system, gadopentetate dimeglumine rapidly reaches equilibrium in the interstitial spaces and enhances signaling in all tissues depending on the dose and size of the interstitial spaces. Studies have also found that this compound can inhibit human erythrocyte 6-phosphate gluconate dehydrogenase.

C14H18GDN3O10.2H

547.57

548.039

80529-93-7

16212436

White to off-white solid powder

721.1ºC at 760 mmHg

129ºC (dec.)(lit.)

389.9ºC

3

14

13

29

497

0

JBUMALASVLVYKI-UHFFFAOYSA-K

InChI=1S/C14H23N3O10.Gd.H2O/c18-10(19)5-15(1-3-16(6-11(20)21)7-12(22)23)2-4-17(8-13(24)25)9-14(26)27;;/h1-9H2,(H,18,19)(H,20,21)(H,22,23)(H,24,25)(H,26,27);;1H2/q;+3;/p-3

2-[bis[2-[carboxylatomethyl(carboxymethyl)amino]ethyl]amino]acetate;gadolinium(3+);hydrate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~182.63 mM)
DMSO : ~1 mg/mL (~1.83 mM)

Solubility in Formulation 1: 100 mg/mL (182.63 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)