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Diss Factsheets
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EC number: - | CAS number: -
- Life Cycle description
- Uses advised against
- Endpoint summary
- Appearance / physical state / colour
- Melting point / freezing point
- Boiling point
- Density
- Particle size distribution (Granulometry)
- Vapour pressure
- Partition coefficient
- Water solubility
- Solubility in organic solvents / fat solubility
- Surface tension
- Flash point
- Auto flammability
- Flammability
- Explosiveness
- Oxidising properties
- Oxidation reduction potential
- Stability in organic solvents and identity of relevant degradation products
- Storage stability and reactivity towards container material
- Stability: thermal, sunlight, metals
- pH
- Dissociation constant
- Viscosity
- Additional physico-chemical information
- Additional physico-chemical properties of nanomaterials
- Nanomaterial agglomeration / aggregation
- Nanomaterial crystalline phase
- Nanomaterial crystallite and grain size
- Nanomaterial aspect ratio / shape
- Nanomaterial specific surface area
- Nanomaterial Zeta potential
- Nanomaterial surface chemistry
- Nanomaterial dustiness
- Nanomaterial porosity
- Nanomaterial pour density
- Nanomaterial photocatalytic activity
- Nanomaterial radical formation potential
- Nanomaterial catalytic activity
- Endpoint summary
- Stability
- Biodegradation
- Bioaccumulation
- Transport and distribution
- Environmental data
- Additional information on environmental fate and behaviour
- Ecotoxicological Summary
- Aquatic toxicity
- Endpoint summary
- Short-term toxicity to fish
- Long-term toxicity to fish
- Short-term toxicity to aquatic invertebrates
- Long-term toxicity to aquatic invertebrates
- Toxicity to aquatic algae and cyanobacteria
- Toxicity to aquatic plants other than algae
- Toxicity to microorganisms
- Endocrine disrupter testing in aquatic vertebrates – in vivo
- Toxicity to other aquatic organisms
- Sediment toxicity
- Terrestrial toxicity
- Biological effects monitoring
- Biotransformation and kinetics
- Additional ecotoxological information
- Toxicological Summary
- Toxicokinetics, metabolism and distribution
- Acute Toxicity
- Irritation / corrosion
- Sensitisation
- Repeated dose toxicity
- Genetic toxicity
- Carcinogenicity
- Toxicity to reproduction
- Specific investigations
- Exposure related observations in humans
- Toxic effects on livestock and pets
- Additional toxicological data
![](https://echa.europa.eu/o/diss-blank-theme/images/factsheets/A-REACH/factsheet/print_toxicological-information.png)
Specific investigations: other studies
Administrative data
- Endpoint:
- biochemical or cellular interactions
- Type of information:
- experimental study
- Adequacy of study:
- supporting study
- Reliability:
- 2 (reliable with restrictions)
- Rationale for reliability incl. deficiencies:
- study well documented, meets generally accepted scientific principles, acceptable for assessment
Data source
Reference
- Reference Type:
- study report
- Title:
- Unnamed
- Year:
- 2 015
- Report date:
- 2015
Materials and methods
Test guideline
- Qualifier:
- according to guideline
- Guideline:
- other: Please see below
- Principles of method if other than guideline:
- Several different in vitro Pharmacology studies were performed according to methods described in the following publications:
Test 1: Binding Assay according to Pristupa, Z.B. et al. (1994), Mol. Pharmacol., 45 : 125-135.
Test 2: Cellular and Nuclear Receptor Functional Assay according to Zhou, Q.Y. et al. (1990), Nature, 347 : 76-80.
Test 3 and 4: Tissue Bioassay according to Zanzottera, D. et al. (1998), Brit. J. Pharmacol., 123 : 730-736 and Steins and, O.S. and Hieble, J.P. (1978), Science, 199 : 443-445.
Test 5: Enzyme and Uptake Assay according to Janowsky, A. et al. (1986), J. Neurochem., 46 : 1272-1276. - GLP compliance:
- no
- Type of method:
- in vitro
- Endpoint addressed:
- not applicable
Test material
- Test material form:
- solid
Constituent 1
- Specific details on test material used for the study:
- SOURCE OF TEST MATERIAL
- Batch No.of test material: L82-66
TREATMENT OF TEST MATERIAL PRIOR TO TESTING
- Final dilution of a stock liquid: 1.E-02 M DMSO
FORM AS APPLIED IN THE TEST (if different from that of starting material)
Liquid
Administration / exposure
- Vehicle:
- DMSO
- Analytical verification of doses or concentrations:
- not specified
- Duration of treatment / exposure:
- Test 1: 120 min
Test 2: 30 min
Test 3 and 4: no treatment duration
Test 5: 15 min
Doses / concentrations
- Dose / conc.:
- 0 other: M
- Remarks:
- All assays were performed with this concentration.
Results and discussion
Any other information on results incl. tables
Test 1 Binding assay
Test concentration (M) |
% Inhibition of Control Specific Binding |
||
1st |
2nd |
Mean |
|
1.0E-05 |
0.9 |
7.4 |
4.1 |
Reference compound results
Compound |
IC50 (M) |
Ki(M) |
nH |
BTCP |
1.3E-08 |
6.7E-09 |
1.3 |
Test 2 Cellular and Nuclear Receptor Functional Assay
Agonist effect
Test concentration (M) |
% Inhibition of Control Agonist response |
||
1st |
2nd |
Mean |
|
1.0E-05 |
0.2 |
0.3 |
0.3 |
Reference compound results
Compound |
EC50 (M) |
nH |
Dopamine |
4.4E-08 |
n/a |
Antagonist effect
Test concentration (M) |
% Inhibition of Control Antagonist response |
||
1st |
2nd |
Mean |
|
1.0E-05 |
-2.1 |
-14.7 |
-8.4 |
Reference compound results
Compound |
IC50 (M) |
KB (M) |
nH |
SCH 23390 |
4.0E-09 |
6.4E-10 |
n/a |
Test 3 and 4: Tissue Bioassay
D1 receptor
In the rabbit splenic artery pre-contracted with U-46619, the D1 receptor agonist SKF 82958 induced a concentration-dependent relaxation which was inhibited by the antagonist R(+)SCH 23390 in a concentration-dependent manner.
The test substance did not affect twitch contraction amplitude at the tested concentration.
In the tissues previously exposed to SKF 82958, the test substance did not significantly reverse the SKF 82958 induced decrease in the twitch contraction amplitude.
These results indicate that test compound does not have an activity at D1 receptors in this tissue.
Agonist effect
Compound |
Test concentration (M) |
% of control SKF 82958 Response |
||
1st |
2nd |
Mean |
||
Test substance |
1.0E-07 |
0 |
0 |
0 |
1.0E-06 |
0 |
0 |
0 |
|
1.0E-05 |
0 |
-3 |
2 |
|
SKF 82958 |
1.0E-07 |
13 |
14 |
14 |
3.0E-07 |
69 |
64 |
67 |
|
1.0E-06 |
106 |
98 |
102 |
|
+ R(+)SCH 23390 |
1.0E-05 |
-3 |
-2 |
-2 |
Antagonist effect
Compound |
Test concentration (M) |
% of control SKF 82958 Response |
||
1st |
2nd |
Mean |
||
Test substance |
1.0E-07 |
100 |
100 |
100 |
1.0E-06 |
101 |
104 |
103 |
|
1.0E-05 |
102 |
104 |
103 |
|
R(+)SCH 23390 |
1.0E-06 |
84 |
88 |
86 |
3.0E-06 |
50 |
45 |
48 |
|
1.0E-05 |
-4 |
-6 |
-5 |
The results are expressed as a percent of the control response to SKF 82958 (relaxation) (mean values; n=2)
D2 receptor
In the field-stimulated rabbit ear artery, the D2 receptor agonist (-)quinpirole induced a concentration-dependent decrease in the twitch contraction amplitude which was inhibited by the antagonist (-)sulpiride.
The test substance did not affect twitch contraction amplitude at the tested concentrations.
In the tissues previously exposed to (-)quinpirole, the test substance did not significantly reverse the (-)quinpirole-induced decrease in the twitch contraction amplitude.
These results indicate that the test substance does not have an activity at the D2 receptor in this tissue.
Agonist effect
Compound |
Test concentration (M) |
% of control (-) Quinpirole Response |
||
1st |
2nd |
Mean |
||
Test substance |
1.0E-07 |
0 |
0 |
0 |
1.0E-06 |
-3 |
-1 |
-2 |
|
1.0E-05 |
-12 |
-11 |
-12 |
|
(-)Quinpirole |
3.0E-08 |
12 |
24 |
18 |
1.0E-07 |
58 |
69 |
64 |
|
3.0E-07 |
101 |
99 |
100 |
|
+ (-)Sulpiride |
3.0E-06 |
16 |
20 |
18 |
Antagonist effect
Compound |
Test concentration (M) |
% of control (-)Quinpirole Response |
||
1st |
2nd |
Mean |
||
Test substance |
1.0E-07 |
97 |
97 |
97 |
1.0E-06 |
90 |
82 |
8 |
|
1.0E-05 |
82 |
74 |
78 |
|
(-)Sulpiride |
3.0E-08 |
85 |
85 |
85 |
3.0E-07 |
42 |
51 |
47 |
|
3.0E-06 |
1 |
-1 |
0 |
The results are expressed as a percent of the control response to (-)Quinpirole (decrease in twitch contraction amplitude) (mean values; n=2)
Test 5: Enzyme and Uptake assay
Test concentration |
% Inhibition of Control Values |
||
1st |
2nd |
Mean |
|
1.0E-05 M |
-3.2 |
-2.2 |
-2.7 |
Reference compound results
Compound |
IC50 (M) |
nH |
GBR 12909 |
2.2E-09 |
n/a |
Applicant's summary and conclusion
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice.
Reproduction or further distribution of this information may be subject to copyright protection. Use of the information without obtaining the permission from the owner(s) of the respective information might violate the rights of the owner.
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