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86-34-0

86-34-0 structure
86-34-0 structure
  • Name: Phensuximide
  • Chemical Name: phensuximide
  • CAS Number: 86-34-0
  • Molecular Formula: C11H11NO2
  • Molecular Weight: 189.21100
  • Catalog: Pharmaceutical intermediate Heterocyclic compound Pyridine compound Iodopyridine
  • Create Date: 2018-03-22 08:00:00
  • Modify Date: 2024-01-08 11:13:36
  • Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal[1][3].
Name phensuximide
Synonyms 1-methyl-3-phenyl-pyrrolidine-2,5-dione
1-methyl-3-phenylsuccinimide
Milontin
Lifen
Mirotin
Lifene
Mirontin
1-Methyl-3-phenyl-pyrrolidin-2,5-dion
Milonton
Epimal
Epimid
N-methylphenylsuccinimide
PM 334
Description Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal[1][3].
Related Catalog
Target

IC50: cyclic AMP and cyclic GMP accumulation[2]

In Vitro Phensuximide produce depolarization-induced accumulation of cyclic GMP or cyclic AMP levels with ID50 values of 8.00 mM or 6.20 mM in incubated slices of mouse cerebral cortex[2]. Phensuximide (0.5-2.0 mM) has the ability to competitively inhibit mephenytoin 4-hydroxylase activity in human liver microsomes, the Ki and Km values are 559 μM and 235 μM, respectively[4].
In Vivo Phensuximide (intraperitoneal injection; 1.25 mmol/kg; single dose) induces mild changes in renal function, including: trace hematuria, increased proteinuria and decreased paminohippurate uptake in Sprague-Dawley rats[1]. Phensuximide (intraperitoneal injection; 0.3 or 0.6 mmol/kg; 5-7 days) results in transient hematuria and proteinuria, but no change in the other renal function parameters studied. It is concluded that phensuximide produces mild, transient renal effects in Fischer 344 rats, and that the Fischer 344 rat is a suitable model for studying phensuximide-induced toxicity to the urinary tract[1]. Animal Model: Fischer 344 rats[1] Dosage: 0.3 or 0.6 mmol/kg Administration: Intraperitoneal injection; 5-7 days Result: Induced urotoxicity following daily administration for 5-7 days in Fischer 344 rats.
References

[1]. G O Rankin, et al. Urinary Tract Effects of Phensuximide in the Sprague-Dawley and Fischer 344 Rat. J Appl Toxicol. . 1986 Oct;6(5):349-56.

[2]. J A Ferrendelli, et al. Inhibitory Effects of Anticonvulsant Drugs on Cyclic Nucleotide Accumulation in Brain. Ann Neurol. 1979 Jun;5(6):533-8.

[3]. J G MILLICHAP, et al. Milontin: A New Drug in the Treatment of Petit Mal.Lancet. 1952 Nov 8;2(6741):907-10.

[4]. S D Hall,et al. Characterization and inhibition of mephenytoin 4-hydroxylase activity in human liver microsomes. The JOURNAL OP PHARMAcOLOGY AND EXPERIMENTAL THERAPEUTICS
Density 1.1596 (rough estimate)
Boiling Point 324.47°C (rough estimate)
Melting Point 71-73°
Molecular Formula C11H11NO2
Molecular Weight 189.21100
Exact Mass 189.07900
PSA 37.38000
LogP 1.09680
Index of Refraction 1.5012 (estimate)
Storage condition 2-8°C

CHEMICAL IDENTIFICATION

RTECS NUMBER :
WN3325000
CHEMICAL NAME :
Succinimide, N-methyl-2-phenyl-
CAS REGISTRY NUMBER :
86-34-0
BEILSTEIN REFERENCE NO. :
0155329
LAST UPDATED :
199612
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C11-H11-N-O2
MOLECULAR WEIGHT :
189.23
WISWESSER LINE NOTATION :
T5VNVTJ B1 DR

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
700 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
485 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
795 mg/kg/7D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - proteinuria Kidney, Ureter, Bladder - hematuria Kidney, Ureter, Bladder - inflammation, necrosis, or scarring of bladder
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
666 mg/kg
SEX/DURATION :
female 8-10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
DOSE :
1533 mg/kg
SEX/DURATION :
female 8-10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system

MUTATION DATA

TYPE OF TEST :
Cytogenetic analysis
TEST SYSTEM :
Human Leukocyte
DOSE/DURATION :
100 ug/L
REFERENCE :
AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 116,867,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4457 No. of Facilities: 46 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 279 (estimated) No. of Female Employees: 46 (estimated)
RIDADR NONH for all modes of transport
HS Code 2925190090
HS Code 2925190090
Summary 2925190090 other imides and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

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