2-dibutylaminoethanol

Specific investigations: other studies

Administrative data

Endpoint:

mechanistic studies

Type of information:

experimental study

Adequacy of study:

other information

Reliability:

2 (reliable with restrictions)

Rationale for reliability incl. deficiencies:

other: Acceptable, well-documented publication which meets basic scientific principles.

Data source

Reference

Reference Type:

publication

Title:

Cholinesterase inhibition in the acute toxicity of alkyl-substituted 2-Aminoethanols

Author:

Hartung R, Cornish HH

Year:

1968

Bibliographic source:

Toxicology and applied pharmacology, 12: 486-494

Materials and methods

Test guideline

Qualifier:

no guideline followed

Principles of method if other than guideline:

The acute oral and intraperitoneal toxicity of a series of alkyl-substituted 2-aminoethanols was studied in relation to cholinesterase inhibition. The oral and intraperitoneal toxicities of these compounds were studied in male Sprague-Dawley rats. Cholinesterase inhibition was conducted in vitro, using a purified enzyme preparation derived from bovine erythrocytes. In vivo cholinesterase inhibition was also investigated in brain and red cells of treated animals.

GLP compliance:

no

Type of method:

other: in vitro and in vivo

Endpoint addressed:

neurotoxicity

Test material

Test material information

Constituent 1

Reference substance name:

2-dibutylaminoethanol

EC Number:

203-057-1

EC Name:

2-dibutylaminoethanol

Cas Number:

102-81-8

Molecular formula:

C10H23NO

IUPAC Name:

2-(dibutylamino)ethan-1-ol

Details on test material:

- Name of test material (as cited in study report): Dibutylaminoethanol
No further data available.

Test animals

Species:

rat

Strain:

Sprague-Dawley

Sex:

male

Administration / exposure

Route of administration:

other: intraperitoneal and oral

Vehicle:

not specified

Analytical verification of doses or concentrations:

not specified

Duration of treatment / exposure:

no data

Frequency of treatment:

no data

Post exposure period:

no data

Doses / concentrations

Remarks:

Doses / Concentrations:
no data
Basis:

No. of animals per sex per dose:

no data

Control animals:

not specified

Results and discussion

Details on results:

The data of this publication indicate that neutralized N-alkyl substituted 2-aminoethanols inhibit cholinesterase in vitro. Inhibition increases as the degree of substitiution and the molecular size of the nitrogenous head of the aminoethanol molecule increase.
The oral LD50 values are uniformly higher than the intraperitoneal LD50 values (Dibutylaminoethanol: oral LD50: 1.78 g/kg bw (1.33 - 2.39); intraperitoneal LD50: 0.144 g/kg bw (0.091 - 0.219).
When the toxicity data and the inhibitory concentrations (50% inhibition) are compared on the basis of molar concentrations, some interesting trends become evident. As the inhibitory capacity of the substituted 2-aminoethanol increases, there appears to be a concurrent increase in the intraperitoneal toxicity, resulting in a very significant correlation coefficient of r = 0.676. When the oral LD50 values are compared on the same basis, they generate a correlation coefficient of r = 0.378, which has only marginal significance. For Dibutylaminoethanol an inhibitor concentration producing 50% inhibition of 1.1 mmol/Liter was found and correlated to an oral LD50 of 10.3 and and i.p. LD50 of 0.831 mmol/kg.
When four of the aminoethanols (Ethylaminoethanol, Dimethylaminoethanol, Dibutylaminoethanol, Dibutylcholine) were given intraperitoneally, they produced moderate but significant depressions in brain cholinesterase activities. A significant depression in red cell cholinesterase activity was only noted for Dimethylaminoethanol.