Methyl N-methylanthranilate

Basic toxicokinetics

Administrative data

Endpoint:

basic toxicokinetics in vitro / ex vivo

Type of information:

experimental study

Adequacy of study:

key study

Reliability:

4 (not assignable)

Rationale for reliability incl. deficiencies:

other: Data is available online

Data source

Reference

Reference Type:

study report

Title:

Unnamed

Year:

2005

Materials and methods

Test guideline

Qualifier:

according to guideline

Guideline:

other:

Principles of method if other than guideline:

Details of guidelines not mentioned in the publication

GLP compliance:

not specified

Test material

Test material information

Constituent 1

Reference substance name:

Methyl N-methylanthranilate

EC Number:

201-642-6

EC Name:

Methyl N-methylanthranilate

Cas Number:

85-91-6

Molecular formula:

C9H11NO2

IUPAC Name:

methyl 2-(methylamino)benzoate

Test material form:

other: liquid

Details on test material:

Methyl N Methylanthranilate (MNMA)

Radiolabelling:

no

Test animals

Species:

other: Guinea pigs (Liver microsomes & cytosol)

Strain:

Hartley

Sex:

male

Administration / exposure

Route of administration:

other: in-vitro hence not applicable

Vehicle:

other: in-vitro hence not applicable

Details on exposure:

MNMA was incubated with guinea pigs liver microsomes (5 µg protein) or cytosol (50 µg protein) in sodium-potassium phosphate buffer 38 mM (pH 7.4) in a final volume of 260 µl. The mixture was incubated at 37oC for 10 mins, and the reaction was terminated by the addition of acetonitrile 200 µl containing methyl p-methoxybenzoate (0.20 µg) as an internal standard. After the removal of protein by centrifugation, 50 µl of the supertanant was injected onto a High Performance Liquid Chromatography (HPLC) system.

Duration and frequency of treatment / exposure:

10 mins

Doses / concentrations

Remarks:

Doses / Concentrations:
1000 µM

No. of animals per sex per dose / concentration:

Not applicable

Control animals:

no

Results and discussion

Main ADME results

Type:

metabolism

Results:

MNMA was hydrolyzed by guinea pigs liver microsomes to produce N-Methyl Anthranilic acid. MNMA was also N-Demthylated by Guinea pigs liver microsomes & cytosol to form anthranilic acid (AA).

Toxicokinetic / pharmacokinetic studies

Details on absorption:

Not Applicable

Details on distribution in tissues:

Not Applicable

Details on excretion:

Not Applicable

Metabolite characterisation studies

Metabolites identified:

yes

Details on metabolites:

N-Methyl Anthranilic acid &
Anthranilic acid (AA)

Any other information on results incl. tables

MNMA was hydrolyzed byguinea pigs liver microsomes to produceN-Methyl Anthranilic acid.MNMA was also N-Demthylated byGuinea pigs liver microsomes & cytosol to form anthranilic acid (AA).

Kinetic analysis indicated that Vmax/Km values were 7.4 fold higher in microsomes than in cytosol

Applicant's summary and conclusion

Conclusions:

Interpretation of results (migrated information): low bioaccumulation potential based on study results
In vitro study of hepatic metabolism of Methyl N Methylanthranilate in guinea pigs liver microsomes was conducted wherein the kinetic analysis indicated that Vmax/Km values were 7.4 fold higher in microsomes than in cytosol. Vmax/Km values reflect the intrinsic clearance potential after hydrolysis and thus the bio-accumulation potential of Methyl N Methylanthranilate (MNMA) is expected to be low.

Executive summary:

In vitro study of hepatic metabolism of Methyl N Methylanthranilate in guinea pigs liver microsomes was conducted wherein the kinetic analysis indicated that Vmax/Km values were 7.4 fold higher in microsomes than in cytosol. Vmax/Km values reflect the intrinsic clearance potential after hydrolysis and thus the bio-accumulation potential ofMethyl N Methylanthranilate (MNMA)is expected to be low.