Ethyl 2-(dimethylamino)-1-phenylcyclohex-3-ene-1-carboxylate

Acute Toxicity: other routes

Administrative data

Endpoint:

acute toxicity: other routes

Type of information:

migrated information: read-across from supporting substance (structural analogue or surrogate)

Adequacy of study:

supporting study

Reliability:

2 (reliable with restrictions)

Rationale for reliability incl. deficiencies:

other: Non-GLP non-guideline, published in peer reviewed literature, limitation in design and/or reporting but otherwise adequate for assessment

Data source

Reference

Reference Type:

publication

Title:

Zur Pharmakologie eines neuen stark wirksamen Analgeticums

Author:

Herrmann M.

Year:

1970

Bibliographic source:

Arzneimittelforschung. 1970 Aug;20(8):977-83.

Materials and methods

Principles of method if other than guideline:

Ten SIV 50 male rats per dose were exposed intravenously to the test substance. Animals were observed for 7 days, clinical signs and mortality were recorded.

GLP compliance:

no

Limit test:

no

Test material

Test material information

Constituent 1

Reference substance name:

Ethyl trans-(±)-2-(dimethylamino)-1-phenylcyclohex-3-ene-1-carboxylate hydrochloride

EC Number:

248-226-0

EC Name:

Ethyl trans-(±)-2-(dimethylamino)-1-phenylcyclohex-3-ene-1-carboxylate hydrochloride

Cas Number:

27107-79-5

IUPAC Name:

27107-79-5

Constituent 2

Reference substance name:

3-Cyclohexene-1-carboxylic acid, 2-(dimethylamino)-1-phenyl-, ethyl ester, hydrochloride, (1R,2S)-rel-

IUPAC Name:

3-Cyclohexene-1-carboxylic acid, 2-(dimethylamino)-1-phenyl-, ethyl ester, hydrochloride, (1R,2S)-rel-

Details on test material:

- Name of test material (as cited in study report): Go 1261 C; Tilidine HCl

Test animals

Species:

rat

Strain:

other: SIV 50

Sex:

male

Details on test animals or test system and environmental conditions:

TEST ANIMALS
- Weight at study initiation: 100 - 130 g
- Fasting period before study: 24 hours
- Water: ad libitum

Administration / exposure

Route of administration:

intravenous

Vehicle:

not specified

Details on exposure:

Injection volume: 1 mL/100 g

No. of animals per sex per dose:

10

Details on study design:

- Duration of observation period following administration: 7 days
- Other examinations performed: clinical signs

Statistics:

The experimental results were statistically analyzed according to the method of Litchfield J.T. and Wilcoxon (1949).

Results and discussion

Effect levels

Sex:

male

Dose descriptor:

LD50

Effect level:

74.1 mg/kg bw

Based on:

test mat.

95% CL:

61 - 90.2

Mortality:

Animals that died, died within 12 hours after administration.

Clinical signs:

- At doses corresponding to about ten times the analgesic dose, the typical Straub-like tail phenomenon (S-shaped tail completely bent over the back of the animal) was observed. Tonic-clonic convulsions were observed at higher doses.
- All clinical signs were disappeared within 24 h in animals that survived.

Applicant's summary and conclusion

Conclusions:

Under the conditions of this test, the LD50 was determined to be 74.1 mg/kg bw.

Executive summary:

Ten SIV 50 male rats per dose were exposed intravenously to the test substance. Animals were observed for 7 days, clinical signs and mortality were recorded. The typical Straub-like tail phenomenon was observed at doses ten times the analgesic dose. Tonic-clonic convulsions were observed at higher doses. The LD50 was determined to be 74.1 mg/kg bw.