(3-fluoro-4'-propyl[biphenyl]-4-yl)boronic acid

Eye irritation

Administrative data

Endpoint:

eye irritation: in vivo

Type of information:

experimental study

Adequacy of study:

key study

Study period:

2006-11-15 to 2006-11-29

Reliability:

1 (reliable without restriction)

Rationale for reliability incl. deficiencies:

guideline study

Data source

Reference

Reference Type:

study report

Title:

Unnamed

Year:

2007

Report date:

2007

Materials and methods

Test guideline

Test guideline 1

Qualifier:

according to guideline

Guideline:

OECD Guideline 405 (Acute Eye Irritation / Corrosion)

Version / remarks:

04-2002

Deviations:

no

Test guideline 2

Qualifier:

according to guideline

Guideline:

EU Method B.5 (Acute Toxicity: Eye Irritation / Corrosion)

Version / remarks:

Official Journal of the European Communities L383 A, Vol. 15, 29. December 1992.

Deviations:

no

GLP compliance:

yes (incl. QA statement)

Test material

Test material information

Constituent 1

Reference substance name:

4'-Ethyl-3-fluorbiphenyl-4-boronic acid

EC Number:

618-440-2

Cas Number:

900796-46-5

Molecular formula:

C14 H14 B F O2

IUPAC Name:

4'-Ethyl-3-fluorbiphenyl-4-boronic acid

Test animals / tissue source

Species:

rabbit

Strain:

New Zealand White

Remarks:

Crl:KBL

Details on test animals or tissues and environmental conditions:

TEST ANIMALS
- Source: Charles River Wiga GmbH, Kißlegg
- Age at study initiation: about 18 weeks
- Weight at study initiation: 3.34 KG
- Housing: separately in special rabbit cages (manufacturer: Becker, type K99/30 KU)
- Diet: ad libitum
- Water: ad libitum
- Acclimation period: more than 7 days

ENVIRONMENTAL CONDITIONS
- Temperature (°C): 16 - 18
- Humidity (%): 47 - 63
- Photoperiod (hrs dark / hrs light): 12 / 12

IN-LIFE DATES: Days 1 to 15

Test system

Vehicle:

unchanged (no vehicle)

Controls:

not required

Amount / concentration applied:

100 mg

Duration of treatment / exposure:

Single application into the conjunctival sac of the left eye, the right eye remained untreated and served as control. The eyelids were closed for 30 sec after installation.

Observation period (in vivo):

24, 48, and 72 hours, then daily up to day 15 of the experimental part

Number of animals or in vitro replicates:

1 f

Details on study design:

REMOVAL OF TEST SUBSTANCE
- Washing: no

SCORING SYSTEM: according OECD GL 405

TOOL USED TO ASSESS SCORE: hand-slit lamp / fluorescein

Results and discussion

In vivo

Results

Results 1

Irritation parameter:

cornea opacity score

Basis:

animal #1

Time point:

24/48/72 h

Score:

0.67

Max. score:

4

Reversibility:

fully reversible within: 2 days

Results 2

Irritation parameter:

iris score

Basis:

animal #1

Time point:

24/48/72 h

Score:

1

Max. score:

2

Reversibility:

fully reversible within: 4 days

Results 3

Irritation parameter:

conjunctivae score

Remarks:

Redness

Basis:

animal #1

Time point:

24/48/72 h

Score:

1.67

Max. score:

3

Reversibility:

fully reversible within: 9 days

Results 4

Irritation parameter:

chemosis score

Basis:

animal #1

Time point:

24/48/72 h

Score:

0.67

Max. score:

4

Reversibility:

fully reversible within: 3 days

Irritant / corrosive response data:

The cornea developed diffuse areas of opacity from the first reading up to day 3 of the experimental part. At the iris signs of irritation were observed from the first reading up to day 4. The conjunctivae showed redness and chemosis from the first reading up to experimental day 8. Thereafter no signs of irritation were observed. The untreated eye was unchanged.

Other effects:

none

Any other information on results incl. tables

Study design

The test item was tested for its eye irritating potential with one rabbit in a GLP study according to OECD GL 405. Prior to testing, a hen's egg test on the chorioallantoic membrane was performed and no irritating potential could be detected. For the test of primary eye irritation, 100 mg of the test material was applied into the conjunctival sac. The first examination of the eyes followed 1 hour after instillation and the other examinations were performed daily for a further 14 days.

Results

There were no signs of pain immediately after instillation. The cornea developed diffuse areas of opacity (scores 1) from the first reading up to day 3 of the experimental part. At the iris signs of irritation were observed (score 1) from the first reading up to day 4. The conjunctivae showed redness (scores 1 and 2) and chemosis (score 1) from the first reading up to experimental day 8. Thereafter no signs of irritation were observed. The untreated eye was unchanged.

Conclusion

Based on the observed results the test item should be regarded as an irritant to the eyes.

Applicant's summary and conclusion

Interpretation of results:

Category 2A (irritating to eyes) based on GHS criteria

Conclusions:

The test item possess an irritating potential to eye.

Executive summary:

This GLP study was performed according to OECD GL 405. A eye irritating potential was noted and the test item should be regarded as an irritant to the eyes.