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64490-92-2

64490-92-2 structure
64490-92-2 structure
  • Name: Tolmetin (sodium dihydrate)
  • Chemical Name: Tolmetin Sodium Salt Dihydrate
  • CAS Number: 64490-92-2
  • Molecular Formula: C15H18NNaO5
  • Molecular Weight: 315.30
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2018-09-27 12:40:40
  • Modify Date: 2024-01-05 12:50:31
  • Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent, and acts as a non-selective COX inhibitor.
Name Tolmetin Sodium Salt Dihydrate
Synonyms EINECS 252-687-3
sodium,2-[1-methyl-5-(4-methylbenzoyl)pyrrol-2-yl]acetate,dihydrate
1H-Pyrrole-2-acetic acid, 1-methyl-5-(4-methylbenzoyl)-, sodium salt, hydrate (1:1:2)
MFCD00079607
Tolmetin (sodium dihydrate)
Description Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent, and acts as a non-selective COX inhibitor.
Related Catalog
Target

COX

In Vitro Tolmetin sodium dihydrate is a non-steroidal antiinflammatory agent. Tolmetin (0-100 μM) shows no effect on osteoblast growth[2]. Tolmetin (0.25 mM) dose not attenuate lipid peroxidation in rat brain homogenate. Tolmetin (0.25, 0.5, 0.75, 1 mM) shows radical scavenging properties but without superoxide anion generation in rat brain homogenat[3].
In Vivo Tolmetin (100 mg/kg) causes gastric lesions, and shows maximal ulcerogenic effect 4 h after the single dose, while potently decreases after 3 and 14 days of repeated administration. Tolmetin produces obvious endothelial damage and inflammatory cell infiltration[1]. Tolmetin (5 mg/kg, i.p., twice a day for 5 days) has no effect on n NMDA receptor binding in rats[3].
Animal Admin Rats[1] After 2 weeks of acclimatization, rats are randomized to different groups and given the non-selective COX inhibitors, amtolmetin guacyl (AMG) (50 and 150 mg/kg) and Tolmetin (30 and 100 mg/kg) as well as the selective COX-2 inhibitor, celecoxib (CXIB; 20 and 60 mg/kg). The compounds are suspended in 1% carboxymethylcellulose (CMC) immediately before use and administered by gavage in a 10-mL/kg volume. Control groups receive CMC in the same volume. Rats from each group are divided into 3 subgroups, consisting each of at least 10 animals. Subgroups are dosed either with a single dose (acute treatment group) or twice daily for 3 and 14 days (chronic treatment groups). To ensure that all groups are dosed for the same period of time, those receiving less than 14 days of NSAIDs are given CMC until they are due to start the assigned treatment. Rats are killed by cervical dislocation 4 h after the last administration. Stomachs are immediately removed, opened along the lesser curvature and gently rinsed[1].
References

[1]. Morini G, et al. Morphological features of rat gastric mucosa after acute and chronic treatment with amtolmetin guacyl: comparison with non-selective and COX-2-selective NSAIDs. Digestion. 2003;68(2-3):124-32. Epub 2003 Nov 7.

[2]. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100.

[3]. Dairam A, et al. Non-steroidal anti-inflammatory agents, tolmetin and sulindac, attenuate oxidative stress in rat brain homogenate and reduce quinolinic acid-induced neurodegeneration in rat hippocampal neurons. Metab Brain Dis. 2006 Sep;21(2-3):221-33.
Boiling Point 483.2ºC at 760 mmHg
Melting Point 155-157 (dec.)
Molecular Formula C15H18NNaO5
Molecular Weight 315.30
Flash Point 246ºC
PSA 80.59000
LogP 0.72830
Storage condition -20°C Freezer

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UX9280000
CHEMICAL NAME :
1H-Pyrrole-2-acetic acid, 1-methyl-5-(4-methylbenzoyl)-, sodium salt, dihydrate
CAS REGISTRY NUMBER :
64490-92-2
LAST UPDATED :
199603
DATA ITEMS CITED :
15
MOLECULAR FORMULA :
C15-H14-N-O3.Na.2H2-O
MOLECULAR WEIGHT :
315.33
WISWESSER LINE NOTATION :
T5NJ A1 BVR D1& E1VO &-NA- &QH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
914 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #134763
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
612 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #134763
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1050 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - hypermotility, diarrhea
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1099,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>724 mg/kg
TOXIC EFFECTS :
Gastrointestinal - ulceration or bleeding from stomach Blood - changes in spleen
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1099,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
899 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #134763
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
550 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #134763
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
670 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - ulceration or bleeding from stomach
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1099,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>622 mg/kg
TOXIC EFFECTS :
Gastrointestinal - ulceration or bleeding from large intestine Blood - changes in spleen
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1099,1977 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9360 mg/kg/26W-I
TOXIC EFFECTS :
Gastrointestinal - other changes Endocrine - adrenal cortex hyperplasia Blood - changes in cell count (unspecified)
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1117,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3720 mg/kg/31D-I
TOXIC EFFECTS :
Endocrine - changes in spleen weight Blood - pigmented or nucleated red blood cells Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 11,1107,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
43800 mg/kg/2Y-I
TOXIC EFFECTS :
Gastrointestinal - ulceration or bleeding from stomach Blood - normocytic anemia
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,557,1979
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
33306 mg/kg/78W-I
TOXIC EFFECTS :
Gastrointestinal - ulceration or bleeding from stomach Blood - normocytic anemia
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,557,1979
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
134 gm/kg/1Y-I
TOXIC EFFECTS :
Gastrointestinal - ulceration or bleeding from stomach Blood - normocytic anemia
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 30,557,1979 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
163 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 8,158,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1300 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 8,158,1977
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H315
Precautionary Statements P301 + P312 + P330
Hazard Codes Xn: Harmful;
Risk Phrases R22;R38
Safety Phrases S36
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS UX9280000

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