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Additional toxicological data

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Endpoint:
additional toxicological information
Type of information:
experimental study
Adequacy of study:
other information
Reliability:
2 (reliable with restrictions)
Rationale for reliability incl. deficiencies:
other: The study meets generally accepted scientific standards, is well documented and is acceptable for assessment.

Data source

Referenceopen allclose all

Reference Type:
publication
Title:
Inhibition of choline acetyltransferase by tertiary alkylaminoethyl esters
Author:
Rowell PP & Chiou CY
Year:
1976
Bibliographic source:
Biochemical Pharmacology, Vol. 25, pp. 1093-1099
Reference Type:
secondary source
Title:
No information
Author:
OECD SIDS
Year:
2005
Bibliographic source:
OECD SIDS, 2-Dimethylaminoethyl acrylate, CAS No: 2439-35-2, 05/2005

Materials and methods

Principles of method if other than guideline:
Inhibition studies with the test substance on cell-free choline acetyltransferase extracted from rat brain in vitro, cellular choline acetyltransferase in minced rat brain tissue in vitro, frog sciatic nerve gastrocnemius muscle preparation in vitro, and rat sciatic nerve gastrocnemius muscle preparation in situ.
GLP compliance:
no

Test material

Constituent 1
Chemical structure
Reference substance name:
2-(dimethylamino)ethyl acrylate
EC Number:
219-460-0
EC Name:
2-(dimethylamino)ethyl acrylate
Cas Number:
2439-35-2
Molecular formula:
C7H13NO2
IUPAC Name:
2-(dimethylamino)ethyl acrylate
Details on test material:
- Name of test material (as cited in study report): N,N-dimethylaminoethyl acrylate (Acryl-DMA)
- Purity unknown

Results and discussion

Any other information on results incl. tables

The IC50's of the test substance to inhibit ChAc were 5.02 ± 0.95 x 104 M and 5.75 ± 0.91 x 104 M in the extracted cell-free ChAc system and cellular minced brain ChAc system, respectively. The test substance showed reversible inhibition and was uncompetitive in nature with respect to both substrates, choline and acetyl CoA. The interaction of the test substance with acetylcholinesterase and butyrylcholinesterase was also investigated. The test substance was 3-5-fold less potent to inhibit cholinesterases than to inhibit ChAc,

demonstrating fair specificity toward ChAc inhibition. The hydrolysis of the ester linkage in the test substance was not affected by these cholinesterases. The test substance produced blockade of indirectly stimulated nerve-muscle preparations both in vitro and in situ, and the blockade in the isolated preparation was reversible with washing.

Applicant's summary and conclusion

Conclusions:
The test substance is a reversible, uncompetitive inhibitor of choline acetyltransferase (ChAc) in vitro and blocks indirectly stimulated nerve-muscle preparations both in vitro and in situ.

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